Prostatic Neoplasms: Tumors or cancer of the PROSTATE.Prostate: A gland in males that surrounds the neck of the URINARY BLADDER and the URETHRA. It secretes a substance that liquefies coagulated semen. It is situated in the pelvic cavity behind the lower part of the PUBIC SYMPHYSIS, above the deep layer of the triangular ligament, and rests upon the RECTUM.Androgens: Compounds that interact with ANDROGEN RECEPTORS in target tissues to bring about the effects similar to those of TESTOSTERONE. Depending on the target tissues, androgenic effects can be on SEX DIFFERENTIATION; male reproductive organs, SPERMATOGENESIS; secondary male SEX CHARACTERISTICS; LIBIDO; development of muscle mass, strength, and power.Receptors, Androgen: Proteins, generally found in the CYTOPLASM, that specifically bind ANDROGENS and mediate their cellular actions. The complex of the androgen and receptor migrates to the CELL NUCLEUS where it induces transcription of specific segments of DNA.Tumor Cells, Cultured: Cells grown in vitro from neoplastic tissue. If they can be established as a TUMOR CELL LINE, they can be propagated in cell culture indefinitely.Cell Line, Tumor: A cell line derived from cultured tumor cells.Finasteride: An orally active 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE inhibitor. It is used as a surgical alternative for treatment of benign PROSTATIC HYPERPLASIA.Vitamin E: A generic descriptor for all TOCOPHEROLS and TOCOTRIENOLS that exhibit ALPHA-TOCOPHEROL activity. By virtue of the phenolic hydrogen on the 2H-1-benzopyran-6-ol nucleus, these compounds exhibit varying degree of antioxidant activity, depending on the site and number of methyl groups and the type of ISOPRENOIDS.Prostate-Specific Antigen: A glycoprotein that is a kallikrein-like serine proteinase and an esterase, produced by epithelial cells of both normal and malignant prostate tissue. It is an important marker for the diagnosis of prostate cancer.Scoliosis: An appreciable lateral deviation in the normally straight vertical line of the spine. (Dorland, 27th ed)Androgen Receptor Antagonists: Compounds that bind to and inhibit the activation of ANDROGEN RECEPTORS.Flutamide: An antiandrogen with about the same potency as cyproterone in rodent and canine species.Androgen Antagonists: Compounds which inhibit or antagonize the biosynthesis or actions of androgens.Tosyl CompoundsThiohydantoinsDihydrotestosterone: A potent androgenic metabolite of TESTOSTERONE. It is produced by the action of the enzyme 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE.AnilidesHeptanes: Seven-carbon saturated hydrocarbon group of the methane series. Include isomers and derivatives.Androgen-Insensitivity Syndrome: A disorder of sexual development transmitted as an X-linked recessive trait. These patients have a karyotype of 46,XY with end-organ resistance to androgen due to mutations in the androgen receptor (RECEPTORS, ANDROGEN) gene. Severity of the defect in receptor quantity or quality correlates with their phenotypes. In these genetic males, the phenotypic spectrum ranges from those with normal female external genitalia, through those with genital ambiguity as in Reifenstein Syndrome, to that of a normal male with INFERTILITY.Orchiectomy: The surgical removal of one or both testicles.Androstenols: Unsaturated androstanes which are substituted with one or more hydroxyl groups in any position in the ring system.Phenylthiohydantoin: Thiohydantoin benzene derivative.Serine Endopeptidases: Any member of the group of ENDOPEPTIDASES containing at the active site a serine residue involved in catalysis.Hydroxamic Acids: A class of weak acids with the general formula R-CONHOH.Histone Deacetylase Inhibitors: Compounds that inhibit HISTONE DEACETYLASES. This class of drugs may influence gene expression by increasing the level of acetylated HISTONES in specific CHROMATIN domains.Apoptosis: One of the mechanisms by which CELL DEATH occurs (compare with NECROSIS and AUTOPHAGOCYTOSIS). Apoptosis is the mechanism responsible for the physiological deletion of cells and appears to be intrinsically programmed. It is characterized by distinctive morphologic changes in the nucleus and cytoplasm, chromatin cleavage at regularly spaced sites, and the endonucleolytic cleavage of genomic DNA; (DNA FRAGMENTATION); at internucleosomal sites. This mode of cell death serves as a balance to mitosis in regulating the size of animal tissues and in mediating pathologic processes associated with tumor growth.Glycyrrhetinic Acid: An oleanolic acid from GLYCYRRHIZA that has some antiallergic, antibacterial, and antiviral properties. It is used topically for allergic or infectious skin inflammation and orally for its aldosterone effects in electrolyte regulation.17-alpha-Hydroxyprogesterone: A metabolite of PROGESTERONE with a hydroxyl group at the 17-alpha position. It serves as an intermediate in the biosynthesis of HYDROCORTISONE and GONADAL STEROID HORMONES.Hydroxyprogesterones: Metabolites or derivatives of PROGESTERONE with hydroxyl group substitution at various sites.Encyclopedias as Topic: Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)Carbenoxolone: An agent derived from licorice root. It is used for the treatment of digestive tract ulcers, especially in the stomach. Antidiuretic side effects are frequent, but otherwise the drug is low in toxicity.Hydroxysteroid Dehydrogenases: Enzymes of the oxidoreductase class that catalyze the dehydrogenation of hydroxysteroids. (From Enzyme Nomenclature, 1992) EC 1.1.-.Glycyrrhizic Acid: A widely used anti-inflammatory agent isolated from the licorice root. It is metabolized to GLYCYRRHETINIC ACID, which inhibits 11-BETA-HYDROXYSTEROID DEHYDROGENASES and other enzymes involved in the metabolism of CORTICOSTEROIDS. Therefore, glycyrrhizic acid, which is the main and sweet component of licorice, has been investigated for its ability to cause hypermineralocorticoidism with sodium retention and potassium loss, edema, increased blood pressure, as well as depression of the renin-angiotensin-aldosterone system.Glycyrrhiza: A genus of leguminous herbs or shrubs whose roots yield GLYCYRRHETINIC ACID and its derivative, CARBENOXOLONE.Adrenal Hyperplasia, Congenital: A group of inherited disorders of the ADRENAL GLANDS, caused by enzyme defects in the synthesis of cortisol (HYDROCORTISONE) and/or ALDOSTERONE leading to accumulation of precursors for ANDROGENS. Depending on the hormone imbalance, congenital adrenal hyperplasia can be classified as salt-wasting, hypertensive, virilizing, or feminizing. Defects in STEROID 21-HYDROXYLASE; STEROID 11-BETA-HYDROXYLASE; STEROID 17-ALPHA-HYDROXYLASE; 3-beta-hydroxysteroid dehydrogenase (3-HYDROXYSTEROID DEHYDROGENASES); TESTOSTERONE 5-ALPHA-REDUCTASE; or steroidogenic acute regulatory protein; among others, underlie these disorders.17-alpha-Hydroxypregnenolone: A 21-carbon steroid that is converted from PREGNENOLONE by STEROID 17-ALPHA-HYDROXYLASE. It is an intermediate in the delta-5 pathway of biosynthesis of GONADAL STEROID HORMONES and the adrenal CORTICOSTEROIDS.Research Support, U.S. Gov't, Non-P.H.S.Research Support, U.S. Gov't, P.H.S.Research Support, Non-U.S. Gov'tResearch Support, U.S. GovernmentIchthyosis, Lamellar: A chronic, congenital ichthyosis inherited as an autosomal recessive trait. Infants are usually born encased in a collodion membrane which sheds within a few weeks. Scaling is generalized and marked with grayish-brown quadrilateral scales, adherent at their centers and free at the edges. In some cases, scales are so thick that they resemble armored plate.Ichthyosis: Any of several generalized skin disorders characterized by dryness, roughness, and scaliness, due to hypertrophy of the stratum corneum epidermis. Most are genetic, but some are acquired, developing in association with other systemic disease or genetic syndrome.Acitretin: An oral retinoid effective in the treatment of psoriasis. It is the major metabolite of ETRETINATE with the advantage of a much shorter half-life when compared with etretinate.Emollients: Oleagenous substances used topically to soothe, soften or protect skin or mucous membranes. They are used also as vehicles for other dermatologic agents.Paracentesis: A procedure in which fluid is withdrawn from a body cavity or organ via a trocar and cannula, needle, or other hollow instrument.Transglutaminases: Transglutaminases catalyze cross-linking of proteins at a GLUTAMINE in one chain with LYSINE in another chain. They include keratinocyte transglutaminase (TGM1 or TGK), tissue transglutaminase (TGM2 or TGC), plasma transglutaminase involved with coagulation (FACTOR XIII and FACTOR XIIIa), hair follicle transglutaminase, and prostate transglutaminase. Although structures differ, they share an active site (YGQCW) and strict CALCIUM dependence.Ichthyosiform Erythroderma, Congenital: Designation for several severe forms of ichthyosis, present at birth, that are characterized by hyperkeratotic scaling. Infants may be born encased in a collodion membrane which begins shedding within 24 hours. This is followed in about two weeks by persistent generalized scaling. The forms include bullous (HYPERKERATOSIS, EPIDERMOLYTIC), non-bullous (ICHTHYOSIS, LAMELLAR), wet type, and dry type.Retinoids: A group of tetraterpenes, with four terpene units joined head-to-tail. Biologically active members of this class are used clinically in the treatment of severe cystic ACNE; PSORIASIS; and other disorders of keratinization.Keratolytic Agents: Agents that soften, separate, and cause desquamation of the cornified epithelium or horny layer of skin. They are used to expose mycelia of infecting fungi or to treat corns, warts, and certain other skin diseases.Ichthyosis Vulgaris: Most common form of ICHTHYOSIS characterized by prominent scaling especially on the exterior surfaces of the extremities. It is inherited as an autosomal dominant trait.

The effects of androgens and antiandrogens on hormone-responsive human breast cancer in long-term tissue culture. (1/1203)

We have examined five human breast cancer cell lines in continuous tissue culture for androgen responsiveness. One of these cell lines shows a 2- to 4-fold stimulation of thymidine incorporation into DNA, apparent as early as 10 hr following androgen addition to cells incubated in serum-free medium. This stimulation is accompanied by an acceleration in cell replication. Antiandrogens [cyproterone acetate (6-chloro-17alpha-acetate-1,2alpha-methylene-4,6-pregnadiene-3,20-dione) and R2956 (17beta-hydroxy-2,2,17alpha-trimethoxyestra-4,9,11-triene-1-one)] inhibit both protein and DNA synthesis below control levels and block androgen-mediated stimulation. Prolonged incubation (greater than 72 hr) in antiandrogen is lethal. The MCF- cell line contains high-affinity receptors for androgenic steroids demonstrable by sucrose density gradients and competitive protein binding analysis. By cross-competition studies, androgen receptors are distinguishable from estrogen receptors also found in this cell line. Concentrations of steroid that saturate androgen receptor sites in vitro are about 1000 times lower than concentrations that maximally stimulate the cells. Changes in quantity and affinity of androgen binding to intact cells at 37 degrees as compared with usual binding techniques using cytosol preparation at 0 degrees do not explain this difference between dissociation of binding and effect. However, this difference can be explained by conversion of [3H]-5alpha-dihydrotestosterone to 5alpha-androstanediol and more polar metabolites at 37 degrees. An examination of incubation media, cytoplasmic extracts and crude nuclear pellets reveals probable conversion of [3H]testosterone to [3H]-5alpha-dihydrotestosterone. Our data provide compelling evidence that some human breast cancer, at least in vitro, may be androgen dependent.  (+info)

Pharmacokinetics of flutamide in patients with renal insufficiency. (2/1203)

AIMS: The aim of this study was to determine the pharmacokinetic parameters of flutamide, a nonsteroidal antiandrogenic compound, and its pharmacologically active metabolite, hydroxyflutamide, in renal insufficiency. Haemodialysis (HD) clearance of flutamide and hydroxyflutamide was also determined. METHODS: Pharmacokinetic parameters were assessed for flutamide and hydroxyflutamide in 26 male subjects with normal renal function (creatinine clearance by 24 h urine collection, CLcr, greater than 80 ml min(-1) 1.73 m(-2); n=6) or reduced renal function; CLcr=50-80 (n=7), 30-49 (n=3), 5-29 (n=4), and <5 ml min(-1) 1.73 m(-2)-HD (n=6), following a single, oral 250 mg flutamide dose. Subjects undergoing HD received a second 250 mg dose of flutamide 4 h prior to HD; blood and dialysate were collected during HD to determine dialysability of flutamide and hydroxyflutamide. RESULTS: Cmax, tmax, AUC, t1/2, and renal clearance of flutamide and hydroxyflutamide did not differ between groups. Less than 1% of the dose appeared in dialysate as hydroxyflutamide. No serious adverse events were observed. CONCLUSIONS: Renal function did not affect flutamide nor hydroxyflutamide disposition. HD did not alter hydroxyflutamide pharmacokinetics. Dosing adjustments for renal impairment or HD are not indicated for flutamide.  (+info)

Androgen-independent induction of prostate-specific antigen gene expression via cross-talk between the androgen receptor and protein kinase A signal transduction pathways. (3/1203)

Transcription of the prostate-specific antigen (PSA) gene escapes regulation by androgens in advanced prostate cancer. To determine the molecular mechanism(s) of androgen-independent regulation of the PSA gene, the possibility that the androgen receptor (AR) is activated in the absence of androgen by stimulation of protein kinase A (PKA) was investigated. Activation of PKA by forskolin resulted in elevated expression of the PSA gene in androgen-depleted LNCaP cells, an effect that was blocked by the antiandrogen, bicalutamide. Further evidence that induction of PSA gene expression was dependent on AR was obtained from experiments using PC3 cells devoid of AR. Neither PSA, PB, nor ARR3 androgen-responsive reporters could be induced by activation of PKA in the absence of transfected AR. In addition, when nuclear AR from forskolin-treated LNCaP cells was incubated with oligonucleotides encoding an androgen response element of the PSA promoter and examined by electromobility shift assay, an increase in AR-androgen response element complex formation was observed. Lastly, cotransfection of an expression vector for a chimeric protein encoding the amino-terminal domain of the human AR linked to Gal4 and a 5xGal4UAS reporter gene construct resulted in activation of the amino-terminal domain of the AR by stimulation of PKA activity. These results demonstrate androgen-independent induction of PSA gene expression in prostate cancer cells by an AR-dependent pathway.  (+info)

Does androgen insufficiency cause lacrimal gland inflammation and aqueous tear deficiency? (4/1203)

PURPOSE: The current investigators have shown that androgen treatment suppresses inflammation and stimulates the function of lacrimal glands in mouse models of Sjogren's syndrome. Recently, others have hypothesized that androgen insufficiency induces an autoimmune process in lacrimal tissue, leading to inflammation, a Sjogren's syndrome-like pathology, and aqueous tear deficiency. The purpose of the present study was to test this hypothesis. METHODS: Lacrimal glands were obtained from adult testicular feminized (Tfm) and control mice; castrated rats, guinea pigs, and rabbits; and castrated rats without anterior or whole pituitary glands and were processed for histology and image analysis. Tear volumes were measured in mice, in patients taking antiandrogen medications, and in age-matched human control subjects. RESULTS: Tfm mice, which are completely resistant to classical androgen action, did not have increased lymphocyte infiltration in their lacrimal glands or decreased tear volumes. No inflammation was evident in lacrimal tissues of male or female rats, guinea pigs, or rabbits 12 to 31 days after castration, no inflammation existed in rat lacrimal glands 15 to 31 days after orchiectomy and pituitary removal, and no aqueous tear deficiency was apparent in patients receiving antiandrogen therapy. CONCLUSIONS: Androgen deficiency may promote the progression of Sjogren's syndrome and its associated lacrimal gland inflammation, meibomian gland dysfunction, and severe dry eye. However, androgen insufficiency alone does not cause lacrimal gland inflammation, a Sjogren's syndrome-like pathology in lacrimal tissue, or aqueous tear deficiency in nonautoimmune animals and humans.  (+info)

From HER2/Neu signal cascade to androgen receptor and its coactivators: a novel pathway by induction of androgen target genes through MAP kinase in prostate cancer cells. (5/1203)

Overexpression of the HER2/Neu protooncogene has been linked to the progression of breast cancer. Here we demonstrate that the growth of prostate cancer LNCaP cells can also be increased by the stable transfection of HER2/Neu. Using AG879, a HER2/Neu inhibitor, and PD98059, a MAP kinase inhibitor, as well as MAP kinase phosphatase-1 (MPK-1), in the transfection assay, we found that HER2/Neu could induce prostate-specific antigen (PSA), a marker for the progression of prostate cancer, through the MAP kinase pathway at a low androgen level. Reporter assays and mammalian two-hybrid assays further suggest this HER2/Neu-induced androgen receptor (AR) transactivation may function through the promotion of interaction between AR and AR coactivators, such as ARA70. Furthermore, we found this HER2/Neu --> MAP kinase --> AR-ARAs --> PSA pathway could not be blocked completely by hydroxyflutamide, an antiandrogen used in the treatment of prostate cancer. Together, these data provide a novel pathway from HER2/Neu to AR transactivation, and they may represent one of the reasons for the PSA re-elevation and hormone resistance during androgen ablation therapy in prostate cancer patients.  (+info)

Differentially expressed genes in hormone refractory prostate cancer: association with chromosomal regions involved with genetic aberrations. (6/1203)

Differential gene expression between the androgen sensitive human prostate cancer cell line LNCaP and an insensitive clonal variant, LNCaP-r, was demonstrated by suppression subtractive hybridization. Twenty-one sequences were identified of which 9 are homologous to known genes, 11 are represented by expressed sequence tags (ESTs), and 1 is novel. We present data for 5 of 7 sequences confirmed to be differentially expressed by Northern blot analysis and semiquantitative RT-PCR. Only one gene, fibronectin (FN), was highly overexpressed (>60-fold) in LNCaP-r cells, consistent with previously reported overexpression of FN in prostate cancer. Four sequences were down-regulated in LNCaP-r cells, including an inactive variant of the E2 ubiquitin conjugating enzyme (UEV-1), a novel metalloproteinase-related collagenase (PM5), and a potential tumor suppressor gene (breast basic conserved gene, BBC1). UEV-1 is multifunctional, regulates the cell cycle via cdk1, has homology to MMS2 and likewise functions as a DNA protection protein, and also has homology to TSG101. Aberrant splice variants of TSG101 occur frequently in both breast and prostate cancer, but its mechanism of action is unknown. FN, BBC1, and UEV-1 localize to regions of chromosomal aberration (2q3.4, 16q24.3, and 20q13.2, respectively) associated with advanced prostate cancer and thus may be highly relevant to disease progression.  (+info)

Overexpression of the cyclin-dependent kinase inhibitor p16 is associated with tumor recurrence in human prostate cancer. (7/1203)

The INK4A gene maps to the 9p21 region and was initially described [M. Serrano et al., Nature (Lond.), 366: 704-707, 1993; A. Kamb et al., Science (Washington DC), 264: 436-440, 1994] as encoding a 148-amino-acid protein termed p16. The p16 protein associates exclusively with Cdk4 and Cdk6, inhibiting their complexation with D-type cyclins and the consequent phosphorylation of pRb. This contributes to cell cycle arrest. The purpose of the present study was to evaluate patterns of p16 expression in a well-characterized cohort of prostatic adenocarcinomas while exploring potential associations between alterations of p16 and clinicopathological variables. Normal and malignant tissues from 88 patients with prostate carcinoma were examined. In situ hybridization and immunohistochemistry assays were used to determine the status of the INK4A exon 1alpha transcripts and levels of p16 protein, respectively. Associations between altered patterns of expression and clinicopathological variables, including pretreatment prostate-specific antigen (PSA) level, Gleason grade, pathological stage, and hormonal status, were evaluated using the Mantel-Haenszel chi2 test. Biochemical (PSA) relapse after surgery was evaluated using the Kaplan-Meier method and the log-rank test. Levels of p16 expression and INK4A exon 1alpha transcripts in normal prostate and benign hyperplastic tissues were undetectable. However, p16 nuclear overexpression was observed in 38 (43%) prostate carcinomas, whereas the remaining 50 (57%) cases showed undetectable p16 levels. Overexpression of p16 protein was found to correlate with increased INK4A exon 1alpha transcripts. Moreover, p16 overexpression was associated with a higher pretreatment PSA level (P = 0.018), the use of neoadjuvant androgen ablation (P = 0.001), and a sooner time to PSA relapse after radical prostatectomy (P = 0.002). These data suggest that p16 overexpression is associated with tumor recurrence and a poor clinical course in patients with prostate cancer.  (+info)

Selection for androgen receptor mutations in prostate cancers treated with androgen antagonist. (8/1203)

The role of androgen receptor (AR) mutations in androgen-independent prostate cancer (PCa) was determined by examining AR transcripts and genes from a large series of bone marrow metastases. Mutations were found in 5 of 16 patients who received combined androgen blockade with the AR antagonist flutamide, and these mutant ARs were strongly stimulated by flutamide. In contrast, the single mutant AR found among 17 patients treated with androgen ablation monotherapy was not flutamide stimulated. Patients with flutamide-stimulated AR mutations responded to subsequent treatment with bicalutamide, an AR antagonist that blocks the mutant ARs. These findings demonstrate that AR mutations occur in response to strong selective pressure from flutamide treatment.  (+info)

*Abiraterone acetate

... prostate cancer not responding to androgen deprivation or treatment with androgen receptor antagonists. It is a prodrug to the ... is a steroidal CYP17A1 inhibitor and by extension androgen synthesis inhibitor which is used in combination with prednisone in ...

*11α-Hydroxyprogesterone

Tindall, D.J.; Chang, C.H.; Lobl, T.J.; Cunningham, G.R. (1984). "Androgen antagonists in androgen target tissues". ... Lerner, Leonard J. (1975). "Androgen antagonists". Pharmacology & Therapeutics. Part B: General and Systematic Pharmacology. 1 ... It was investigated as a topical antiandrogen for the treatment of androgen-dependent skin conditions in the early 1950s, and ...

*RU-22930

"Androgen antagonists in androgen target tissues". Pharmacol. Ther. 24 (3): 367-400. PMID 6205409. Singh SM, Gauthier S, Labrie ... It is a selective antagonist of the androgen receptor and consequently has progonadotropic effects by increasing gonadotropin ... "Androgen receptor antagonists (antiandrogens): structure-activity relationships". Curr. Med. Chem. 7 (2): 211-47. PMID 10637363 ... Thomson, D. S. (1989). "Pharmacology of Anti-androgens in the Skin". 87 / 2: 483-493. doi:10.1007/978-3-642-74054-1_36. ISSN ...

*Somatic evolution in cancer

June 1999). "Selection for androgen receptor mutations in prostate cancers treated with androgen antagonist". Cancer Res. 59 ( ... Mutations in the androgen receptor (AR) have been observed in anti-androgen resistant prostate cancer that makes the AR ... These additional copies of the gene are thought to make the cell hypersensitive to low levels of androgens and so allow them to ... Most prostate cancers derive from cells that are stimulated to proliferate by androgens. Most prostate cancer therapies are ...

*Side effects of bicalutamide

Apoptosis induced by the androgen antagonist bicalutamide is receptor mediated (Lin et al., 2006), and hence a dominant effect ... Androgens are known to stimulate the formation of red blood cells and increase the red blood cell count and circulating ... Androgens are involved in regulation of the skin (e.g., sebum production), and antiandrogens are known to be associated with ... It is thought that this is due to the suppression of estrogen levels (in addition to androgen levels) by GnRH analogues, as ...

*Spectinabilin

Isolation and structure elucidation of a novel androgen antagonist, arabilin, produced by Streptomyces sp. MK756-CF1 - Journal ...

*Antiandrogens in the environment

... have shown irregular reproductive development due to their function as androgen receptor antagonists that inhibit androgen- ... "Plant-derived 3,3'-Diindolylmethane is a strong androgen antagonist in human prostate cancer cells". J Biol Chem. 278: 21136-45 ... Paraben esters, such as butylparaben, have been found to mimic androgen antagonist activity. Antiandrogenic endocrine ... is a specific androgen antagonist and has been used as alternative medicine in benign prostatic hyperplasia. Licorice, or ...

*Cruciferous vegetables

Diindolylmethane is a strong androgen antagonist in human prostate cancer cells". The Journal of Biological Chemistry. 278 (23 ...

*Brassica

Diindolylmethane Is a Strong Androgen Antagonist in Human Prostate Cancer Cells". Journal of Biological Chemistry. 278 (23): ... Diindolylmethane induces a G1 arrest in human prostate cancer cells irrespective of androgen receptor and p53 status". ...

*Cortexolone 17α-propionate

... an androgen receptor antagonist - that is under development by Cassiopea and Intrepid Therapeutics for use as a topical ... a new topical and peripherally selective androgen antagonist". Arzneimittelforschung. 54 (12): 881-6. doi:10.1055/s-0031- ... medication in the treatment of androgen-dependent conditions including acne vulgaris and androgenic alopecia (male-pattern hair ...

*9,11-Dehydrocortexolone 17α-butyrate

... a new androgen antagonist with antigonadotropic activity". Arzneimittelforschung. 55 (10): 581-7. doi:10.1055/s-0031-1296908. ...

*Flutamide

... acts as a selective antagonist of the androgen receptor (AR), competing with androgens like testosterone and ... Helsen C, Van den Broeck T, Voet A, Prekovic S, Van Poppel H, Joniau S, Claessens F (Aug 2014). "Androgen receptor antagonists ... Sundblad C, Landén M, Eriksson T, Bergman L, Eriksson E (2005). "Effects of the androgen antagonist flutamide and the serotonin ... In contrast to GnRH agonists, GnRH antagonists don't cause an initial androgen surge, and are gradually replacing GnRH agonists ...

*RU-59063

Ran F, Xing H, Liu Y, Zhang D, Li P, Zhao G (2015). "Recent Developments in Androgen Receptor Antagonists". Arch. Pharm. ( ... RU-59063 is a nonsteroidal androgen or selective androgen receptor modulator (SARM) which was first described in 1994 and was ... RU-59063 has high affinity for the human androgen receptor (AR) (Ki = 2.2 nM; Ka = 5.4 nM) and 1,000-fold selectivity for the ... Liu B, Su L, Geng J, Liu J, Zhao G (2010). "Developments in nonsteroidal antiandrogens targeting the androgen receptor". ...

*Nonsteroidal antiandrogen

They are typically selective and full or silent antagonists of the androgen receptor (AR) and act by directly blocking the ... Singh SM, Gauthier S, Labrie F (2000). "Androgen receptor antagonists (antiandrogens): structure-activity relationships". Curr ... "Androgen receptor antagonists (antiandrogens): structure-activity relationships". Curr. Med. Chem. 7 (2): 211-47. doi:10.2174/ ... An over-the-counter histamine H2 receptor antagonist that also shows very weak activity as an AR antagonist. Also inhibits ...

*Pharmacology of bicalutamide

Masiello D, Cheng S, Bubley GJ, Lu ML, Balk SP (July 2002). "Bicalutamide functions as an androgen receptor antagonist by ... Bicalutamide acts as a highly selective competitive silent antagonist of the androgen receptor (AR) (IC50 = 159-243 nM), the ... Antigonadotropic agents like high-dose CPA, high-dose androgens (e.g., testosterone esters), and GnRH antagonists (though ... Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): structure-activity ...

*Steroidal antiandrogen

They are typically antagonists of the androgen receptor (AR) and act both by blocking the effects of androgens like ... Specifically acts as an AR antagonist, weak antigonadotropin, and weak steroidogenesis inhibitor. Used for androgen-dependent ... 99-. ISBN 978-1-60327-829-4. Singh SM, Gauthier S, Labrie F (2000). "Androgen receptor antagonists (antiandrogens): structure- ... Due to their antigonadotropic effects, SAAs lower androgen levels in addition to directly blocking the actions of androgens at ...

*Azasteroid

321-. ISBN 978-1-901865-55-4. Singh, Shankar; Gauthier, Sylvain; Labrie, Fernand (2000). "Androgen Receptor Antagonists ( ...

*AA560

Similarly to flutamide, AA560 is a selective antagonist of the androgen receptor (AR) and consequently shows progonadotropic ... Singh SM, Gauthier S, Labrie F (2000). "Androgen receptor antagonists (antiandrogens): structure-activity relationships". Curr ...

*Metribolone

Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): structure-activity ... ISBN 978-1-4831-4566-2. R-2956 [41-43], a dimethyl derivative of an extremely potent androgen, R 1881 [44], is a powerful ... Brueggemeier, Robert W. (2006). "Sex Hormones (Male): Analogs and Antagonists". doi:10.1002/3527600906.mcb.200500066. ... derivative which was never marketed for medical use but has been widely used in scientific research as a hot ligand in androgen ...

*Dienogest

In fact, it is actually an antagonist of the androgen receptor (AR) and hence has antiandrogenic activity, said to be about 30 ... 63-. ISBN 978-3-319-20185-6. Singh SM, Gauthier S, Labrie F (2000). "Androgen receptor antagonists (antiandrogens): structure- ... It shows antagonist activity by binding to the AR, and hence produces an antiandrogenic action equivalent to ca. 40% of the ... Ojasoo T, Delettré J, Mornon JP, Turpin-VanDycke C, Raynaud JP (1987). "Towards the mapping of the progesterone and androgen ...

*Nilutamide

... acts as a selective antagonist of the androgen receptor (AR), preventing the effects of androgens like testosterone ... Nilutamide acts as a selective competitive silent antagonist of the AR (IC50 = 412 nM), which prevents androgens like ... 11-. ISBN 978-981-256-920-2. Singh, Shankar; Gauthier, Sylvain; Labrie, Fernand (2000). "Androgen Receptor Antagonists ( ... De Voogt, H. J.; Rao, B. R.; Geldof, A. A.; Gooren, L. J. G.; Bouman, F. G. (1987). "Androgen action blockade does not result ...

*Comparison of bicalutamide with other antiandrogens

Rathkopf D, Scher HI (2013). "Androgen receptor antagonists in castration-resistant prostate cancer". Cancer Journal. 19 (1): ... ISBN 978-1-60327-829-4. Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): ... "Androgen receptor antagonists for prostate cancer therapy". Endocrine-Related Cancer. 21 (4): T105-18. doi:10.1530/ERC-13-0545 ... "Drug safety is a barrier to the discovery and development of new androgen receptor antagonists". The Prostate. 71 (5): 480-8. ...

*Hydroxyflutamide

Singh, Shankar; Gauthier, Sylvain; Labrie, Fernand (2000). "Androgen Receptor Antagonists (Antiandrogens) Structure-Activity ... Differential effects on high-androgen responder and low-androgen responder muscle groups". Endocrinology. 154 (12): 4594-606. ... It is reported to possess an IC50 of 700 nM for the androgen receptor (AR), about 4-fold less than that of bicalutamide. ...

*Cyproterone acetate

CPA is a potent androgen receptor (AR) competitive antagonist. It directly blocks endogenous androgens such as testosterone and ... CPA is known to possess the following pharmacological activity: Androgen receptor (AR) antagonist/very weak partial agonist ( ... ISBN 978-1-84076-013-2. Singh, Shankar; Gauthier, Sylvain; Labrie, Fernand (2000). "Androgen Receptor Antagonists ( ... In addition, although CPA reduces androgen production in the gonads, it can increase the production of adrenal androgens, in ...

*Delanterone

ISBN 978-3-527-30247-5. Singh, Shankar; Gauthier, Sylvain; Labrie, Fernand (2000). "Androgen Receptor Antagonists ( ...

*7α-Thioprogesterone

Cutler GB, Pita JC, Rifka SM, Menard RH, Sauer MA, Loriaux DL (1978). "SC 25152: A potent mineralocorticoid antagonist with ... as that of spironolactone and its active metabolites like 7α-thiomethylspironolactone for the rat ventral prostate androgen ...

*Medical uses of bicalutamide

Gauthier S, Martel C, Labrie F (October 2012). "Steroid derivatives as pure antagonists of the androgen receptor". The Journal ... Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): structure-activity ... In the cortex and pituitary, androgens do not undergo significant aromatization, and it appears that the effects of androgens ... Balk SP (September 2002). "Androgen receptor as a target in androgen-independent prostate cancer". Urology. 60 (3 Suppl 1): 132 ...
The trial follow-up period was stopped early (median follow-up, 6.9 years) because a planned interim analysis, reviewed by an independent data and safety monitoring committee, unequivocally demonstrated no difference in survival outcome between the two treatment groups. Median overall survival was 8.8 years on intermittent androgen suppression vs 9.1 years on continuous androgen deprivation (HR = 1.02; 95% CI = 0.86-1.21; P = .009 for noninferiority [HR ≥ 1.25 for intermittent androgen suppression vs continuous androgen deprivation]). Patients on the intermittent androgen suppression arm had more disease-related deaths (122 vs 97) and fewer disease-unrelated deaths (134 vs 146).. Patients receiving intermittent androgen suppression therapy had a reduced incidence of hot flashes, but rates of other adverse events, including myocardial events and osteoporotic fractures, were similar between the two groups. Full testosterone recovery was noted in 35% of men on the intermittent androgen ...
In locally advanced prostate cancer, the results of radiotherapy are improved by combination with androgen deprivation therapy. Prostate volume reduction by neoadjuvant hormonal treatment can facilitate dose escalation without increasing the toxicity. The aim of this study is to decide the optimal duration of neoadjuvant androgen deprivation therapy for prostate volume reduction in locally advanced prostate cancer patients scheduled for external beam radiotherapy (EBRT). ...
RATIONALE: Radiation therapy uses high-energy x-rays and other types of radiation to kill tumor cells and shrink tumors. Androgens can cause the growth of prostate cancer cells. Androgen-deprivation therapy may lessen the amount of androgens made by the body. It is not yet known whether radiation therapy is more effective with or without androgen-deprivation therapy in treating patients with prostate cancer.. PURPOSE: This randomized phase III trial is studying radiation therapy to see how well it works compared with radiation therapy given together with androgen-deprivation therapy in treating patients with prostate cancer. ...
RATIONALE: Radiation therapy uses high-energy x-rays and other types of radiation to kill tumor cells and shrink tumors. Androgens can cause the growth of prostate cancer cells. Androgen-deprivation therapy may lessen the amount of androgens made by the body. It is not yet known whether radiation therapy is more effective with or without androgen-deprivation therapy in treating patients with prostate cancer.. PURPOSE: This randomized phase III trial is studying radiation therapy to see how well it works compared with radiation therapy given together with androgen-deprivation therapy in treating patients with prostate cancer. ...
Health, ...WASHINGTON A study of more than 15000 men with early stage prostate ...The research team led by scientists at Georgetown Lombardi Comprehens...The findings reported Monday in the Journal of Clinical Oncology/...Androgen deprivation therapy suppresses the production of testosterone...,Primary,androgen,deprivation,therapy,ineffective,for,most,men,with,early,prostate,cancer,medicine,medical news today,latest medical news,medical newsletters,current medical news,latest medicine news
Background: Many elderly men with high-risk nonmetastatic prostate cancer (HRnMPCa) do not receive radical treatment, despite the high mortality associated with conservative management. Objective: To investigate how age and comorbidity affect treatment of men with HRnMPCa. Design, setting, and participants: This was an observational nationwide register study during 2001-2012. We identified 19 190 men of ,80 yr of age diagnosed with HRnMPCa in the National Prostate Cancer Register of Sweden and 95 948 age-matched men without prostate cancer in the register of the total population. Outcome measurements and statistical analysis: The outcome was the proportion of men with HRnMPCa receiving radical treatment (radical prostatectomy or radiotherapy). Vital status and the Charlson comorbidity index (CCI) were obtained from nationwide registers. The 10-yr survival of men without prostate cancer, stratified by age and CCI, was used as a measure of the life expectancy of the men with prostate cancer. ...
1 Introduction Treatment of metastatic prostate cancer with androgen deprivation therapy (ADT) is effective, but can be associated with debilitating side effects. Oligometastasis describes a state of limited metastatic capacity (Weichselbaum 2011). This may represent an intermediate disease state that is amenable to aggressive local therapy, allowing deferral of ADT. In practice oligometastasis usually refers to five or fewer metastases. These early metastatic lesions may seed further metastases. Therefore, eradication of oligometastases may alter the progression of disease and potentially offer cure in select cases. Surgery or radiation therapy are the two treatment options in this setting. Stereotactic body radiotherapy (SBRT) is relatively non-invasive. It delivers an ablative dose of radiotherapy to target tissues, minimising scatter to adjacent structures. Early evidence in other cancers suggests SBRT is a safe and effective treatment for oligometastatic disease (Tree 2013). Conclusions ...
Evidence-based recommendations on enzalutamide (Xtandi) for treating high-risk hormone-relapsed non-metastatic prostate cancer in adults
CTLA-4 blockade has demonstrated antitumor efficacy in human clinical trials. The antitumor mechanism is presumably mediated in part by the expansion of tumor-specific T cells. Androgen deprivation, t
In a Phase III clinical trial among men receiving androgen-deprivation therapy for nonmetastatic prostate cancer, treatment with investigational drug denosumab improved bone density and reduced the risk of vertebral fractures.. Prostate cancer is the most commonly diagnosed cancer (other than skin cancer) among men in the United States. One common approach to treatment of prostate cancer is androgen deprivation therapy (ADT), also referred to as hormonal therapy. ADT interferes with the growth of prostate cancer by reducing circulating testosterone levels.. A significant side effect associated with ADT is loss of bone density or bone mass. Bone loss increases the risk of osteoporosis, bone fracture, pain, hospitalization, and immobility, and increases medical costs.. Denosumab is an investigational drug that targets a protein known as the RANK ligand. This protein regulates the activity of osteoclasts (cells that break down bone). Denosumab is being evaluated for the management of bone loss ...
Some men receiving Androgen Deprivation Therapy (ADT; also called hormone therapy) report a decline in their thinking skills (eg.memory). But some men may experience more of a change than others. This suggests that there may be factors that make some men more, or less, at risk of a drop in thinking skills after ADT than others. These researchers aim to identify these factors so that men can be given evidence based information before making treatment decisions around hormone therapy. Population based studies like this will give us knew information that might help in developing interventions to manage the side-effects of treatment. ...
Immune Responses Enhanced and Sustained When PROVENGE® (sipuleucel-T) is Given After Androgen Deprivation Therapy in Biochemically-Recurrent Prostate Cancer
The paper, titled "Enhancing the effectiveness of androgen deprivation in prostate cancer by inducing Filamin A nuclear localization," shows for the first time that GCP keeps filamin A in the nucleus. As long as this protein remains attached to the androgen receptor, the cancerous cells need androgens to survive and grow. They die off when starved of androgens, thus prolonging the effects of androgen deprivation, which ultimately prolongs the patients life.. The teams hypothesis is that metastatic prostate cancer patients with the weakest response to androgen-deprivation therapy could be given GCP concurrently with androgen deprivation therapy to retain Filamin A in the nucleus, thereby allowing cancer cells to die off. De Vere White is now pursuing funding to begin GCP human clinical trials. Because GCP is a natural product rather than a drug, and requires fewer government approvals, its expected that these trials will proceed rapidly once funded.. "We should know within the first eight ...
August 12, 2009 - There are higher rates of both osteoporosis and nonpathologic fractures for men with nonmetastatic prostate cancer using androgen-deprivation therapy (ADT). The role of ADT in men with metastatic prostate cancer - especially patients who receive external beam radiotherapy or who have node-positive disease - has been prospectively established. However, the most common use of ADT in the U.S. is for nonmetastatic prostate-specific antigen failure, for which prospective evidence of benefit is lacking.. Bisphosphonates have been widely used to lower incidence of skeletal events (e.g., pathologic fractures in patients with metastatic disease) and to attenuate development of osteoporosis. However, use of this class of drugs carries a small but real risk for development of renal insufficiency and osteonecrosis. A novel compound that might be used in this setting is denosumab, a human monoclonal antibody that binds to the receptor activator of nuclear factor-B ligand (a key mediator of ...
At a median follow-up of 29 months, median OS was 44 months in the ADT group versus 57.6 months in the ADT-docetaxel group, or a 39% higher likelihood of survival in the combination arm at any time point during the study (haz-ard ratio 0.61, P = .0003).. Among 520 patients with high-volume disease (visceral metastases and/or 4 or more bone metastases), adding docetaxel to ADT improved median OS by 17 months (32.2 months in the ADT-only group vs 49.2 months in the combi-nation group). The median OS in patients with low-volume disease has not yet been reached.. Combination therapy favored all subgroups. Patients were stratified according to age, volume of disease, bone and vis-ceral metastases, race, Gleason score, prior local therapy, use of anti-androgen therapy beyond 30 days, and skeletal-related events.. Docetaxel also delayed disease progression. At 1 year, the percentage of patients with prostate-specific antigen (PSA) levels less than 0.2 ng/mL was 11.7% in the ADT group versus 22.7% in ...
Purpose: To initiate a phase 1/2 trial to examine the tolerability of a condensed combined-modality protocol for high-risk prostate cancer. Methods and Materials: Men scoring ≥3 on the Vulnerable Elderly Scale (VES) or refusing conventionally fractionated treatment for high-risk prostate cancer were eligible to participate. Androgen suppression was delivered for 12 months, and radiation therapy was delivered using 25 Gy to pelvic nodes delivered synchronously with 40 Gy to the prostate given as 1 fraction per week over 5 weeks. The phase 1 component included predetermined stopping rules based on 6-month treatment-related toxicity, with trial suspension specified if there were ≥6 of 15 patients (40%) or ≥3 of 15 (20%) who experienced grade ≥2 or ≥3 gastrointestinal (GI) or genitourinary (GU) toxicity, respectively. Results: Sixteen men were enrolled, with 7 men meeting the criteria of VES ≥3 and 9 men having a VES ,3 but choosing the condensed treatment. One man was not treated owing ...
RATIONALE: Zoledronate may prevent bone loss in patients with prostate cancer undergoing radiation therapy and hormone therapy. It is not yet known whet
This study investigated the feasibility of using degarelix as intermittent androgen deprivation (IAD) therapy in the treatment of prostate cancer.
When LAPC patients are treated with RT+ADT, LT-ADT is generally defined as the administration of ADT over 2 years, usually prescribed as an adjuvant. A total of five phase III trials have reported long-term follow-up results from approximately 2,500 patients [4-7,10,12-16] (Table 4). As described previously, the purposes of those five studies were to compare the clinical outcomes of LT-ADT+RT with RT alone (RTOG 8531 and EORTC 22863) [4-7,10], or with ADT alone (NCIC CTG/MRC and SPCG-7/SFUO-3) [12-14] or with ST-ADT (RTOG 9202) [15,16] in LAPC patients. In most studies, the median age was around 70 years but, in SPCG-7/SFUO-3, it was 66 years [14]. RTOG 8531 enrolled a larger proportion of node-positive disease (29%) cases than the others (3%-4%) [4,6,7]. Patients with locally advanced stage (cT3-4) accounted for over 70% of the cohort, except for RTOG 9202 (cT2c 45%, cT3-4 55%). A total dose of 65-70 Gy was delivered to the prostate target (approximately 45-50 Gy of pelvic RT followed by 20-25 ...
Based on the controversial nature of the SWOG 9346 findings, presented at the 2012 Annual Meeting Plenary Session, ASCO intiated a pilot program at the meeting for a "town hall" type of discussion, where attendees could voice their concerns and questions, and where presenter Maha Hussain, MD, University of Michigan Comprehensive Cancer Center, Ann Arbor, and discussant William K. Oh, MD, Mount Sinai School of Medicine, New York, could respond.. At the post-plenary discussion, Dr. Hussain recapped the results of the study and acknowledged that the study was not designed to look at extensive vs minimal disease prospectively.. "I was surprised at the data. Intermittent androgen deprivation is thought to be most appropriate in patients with less metastatic disease burden, yet our results based on the secondary analysis suggest that intermittent therapy was especially inferior in the minimal disease group of patients. However, based on the primary results of the study, continuous therapy is the ...
Background:Hormone therapy is commonly used with radiotherapy in the treatment of prostate cancer. Aim:To provide a single-institution analysis of the benefits of hormone therapy with radiotherapy in...
The present analysis is to our knowledge the first one that addresses the role of PMRT as a potential cause of cardiac morbidity in prostate cancer patients receiving androgen suppression therapy. It was performed both in cancer patients and randomly selected individuals having had CT examinations for other medical reasons. The results in these groups were largely comparable. We used 3-D treatment planning with display of isodose distributions and dose-volume histograms only in those patients whose CT scans already were entered into the treatment planning system, i.e. prostate cancer patients, and only if the LAD could be identified. Data from these patients suggest that parts of the left ventricle might be exposed to 50-80% of the prescription dose, even if the mean doses in general are low. Studies in electron boost treatment for breast cancer have also shown that the heart might be exposed to unexpected radiation doses in a proportion of these patients [12]. The present data suggest that ...
The purpose of this study is to describe the safety and tolerability of up to 5 years (ie, 3 years under the 20040138 Amgen study and 2 years on this s
Given the positive-feedback circuit linking AR axis stimulation and DNA repair, it would suggest, in principle, that targeting the AR axis represents a very sound and attractive strategy for potentiating the DNA-damaging effects of cytotoxic therapies in prostate cancer. Importantly, it was observed in primary prostate cancer specimens undergoing neoadjuvant androgen deprivation therapy (ADT), that inhibition of the AR axis leads to a reduction of Ku protein expression in post-ADT prostate biopsies (5). In this first-in-human proof-of-mechanism study, Tarish and colleagues demonstrated longitudinally that castration primarily affected both Ku and DNA-PKcs expression in response to radiotherapy, leading to significant impairment of the nonhomologous end-joining (NHEJ) pathway of DSB (5). In parallel, Polkinghorn and colleagues and Goodwin and colleagues also observed a radiosensitization effect as a consequence of androgen blockade, and attributed this to the transcriptional downregulation of DNA ...
In our cohort of 80 844 patients, ADT was associated with an increased rate of fracture in both non-metastatic patients (aHR = 1.34; 95% confidence interval [CI] = 1.29-1.39) and metastatic patients (aHR = 1.51; 95%CI = 1.36-1.67). Fracture rates increased with increasing cumulative GnRH dose but decreased with increasing number of months since last use in each dose category. The mortality rate doubled for men experiencing a fracture after their diagnosis compared with that for men who did not experience a fracture (aHR = 2.05; 95%CI = 1.98-2.12). ...
OncoLink, the Webs first cancer resource,provides comprehensive information on coping with cancer, cancer treatments, cancer research advances, continuing medical education, cancer prevention, and clinical trials
Radical prostatectomy reduces mortality among men with localized prostate cancer; however, important questions regarding long-term benefit remain. Between 1989 and 1999,.... ...
J Clin Oncol. 2003 May 1;21(9):1653-9. Clinical Trial; Multicenter Study; Randomized Controlled Trial; Research Support, Non-U.S. Govt
For men with bladder cancer, androgen suppression therapy may be prophylactic for intravesical recurrence, according to a study published in the February issue of The Journal of Urology.
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Peripheral androgen blockade is feasible for prostate cancer patients who experience biochemical failure after definitive local therapy.
WASHINGTON - The cardiovascular effects of androgen deprivation therapy (ADT) for men with advanced prostate cancer are less severe than once feared, but there
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Background: There has been substantial increase in use of androgen deprivation therapy as adjuvant management of prostate cancer. However, this leads to a range of musculoskeletal toxicities including reduced bone mass and increased skeletal fractures compounded with rapid metabolic alterations, including increased body fat, reduced lean mass, insulin resistance and negative lipoprotein profile, increased incidence of cardiovascular and metabolic morbidity, greater distress and reduced quality of life. Numerous research studies have demonstrated certain exercise prescriptions to be effective at preventing or even reversing these treatment toxicities. However, all interventions to date have been of rehabilitative intent being implemented after a minimum of 3 months since initiation of androgen deprivation, by which time considerable physical and psychological health problems have manifested. The pressing question is whether it is more efficacious to commence exercise therapy at the same time as
There has been substantial increase in use of androgen deprivation therapy as adjuvant management of prostate cancer. However, this leads to a range of musculoskeletal toxicities including reduced bone mass and increased skeletal fractures compounded
A regimen found useful for treating hot flashes in female cancer patients failed to relieve vasomotor symptoms in prostate cancer patients treated with androgen deprivation therapy, according to a ran
BACKGROUND: Strategies to improve bone health care in men receiving androgen deprivation therapy (ADT) are not consistently implemented. The authors conducted a phase 2 randomized controlled trial of 2 education-based models-of-care interventions to determine their feasibility and ability to improve bone health care. METHODS: A single-center parallel-group randomized controlled trial of men with prostate cancer who were receiving ADT was performed. Participants were randomized 1:1:1 to 1) a patient bone health pamphlet and brief recommendations for their family physician (BHP+FP); 2) a BHP and support from a bone health care coordinator (BHP+BHCC); or 3) usual care ...
Statin use may slow prostate cancer progression in patients receiving androgen deprivation therapy, but more trials are needed to confirm benefits, researchers say
Background: Although androgen deprivation therapy initially decreases PC tumor burden, resistance to further androgen receptor (AR)-directed treatments or chemotherapy is inevitable once CRPC is established. We postulated that the stress of ADT triggers widespread alterations in expression that renders a metastable physiologic state conditioned by epigenetic changes that might be initially reversible by targeting non-androgen pathways. We conducted a pilot study to explore genome-wide expression alterations in PC foci surviving 3 months ADT (eADT).. Methods: mRNA from 7 frozen microdissected PC foci and normal counterparts (NC) were processed for RNA-seq. RNA-seq changes in eADT specimens were compared first with NC and the untreated PC in the TCGA PRAD (TCGA) database to castrate resistant (mCRPC) specimens in the dbGAP study phs000915.v1.p1database. The raw data (fastq files) was quantified using kallisto, normalized by TMM using R package edgeR, batch effects corrected using R package SVA. ...
Prostate cancer hormone therapy, also called androgen deprivation therapy (ADT), is used to suppress the amount of testosterone produced by the body.
Antiandrogens Definition - Anti-androgens are a diverse group of medicines that counteract the effects of excess amounts of androgens or male sex...
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Purpose: Prostate cancer survivors (PCS) on androgen deprivation therapy (ADT) experience adverse side effects such as skeletal muscle loss and adiposity gain, together called sarcopenic obesity, and changes in cardiometabolic factors that increase risk of metabolic syndrome (MetS). Resistance exercise can increase skeletal muscle mass, but no exercise interventions to date in PCS on ADT have concomitantly improved sarcopenic obesity and cardiometabolic risk factors. Utilizing a 12-week intervention of progressive resistance exercise designed to target skeletal muscle mass, this ongoing pilot trial investigates sarcopenic obesity and as a secondary analyses, MetS components, in PCS on ADT.. Methods: Eighteen PCS (65.6±8.8 yr) on current or previous ADT were recruited from the USC Norris Comprehensive Cancer Center and randomized to resistance training (RT; n=9) or a control stretching program (CS; n=9). Body composition, measured through dual-x-ray absorptiometry, and MetS outcomes, including ...
A combination regimen plus androgen-deprivation therapy prolongs overall survival (OS) and radiographic progression-free survival (PFS) in newly diagnosed patients with metastatic, castration-sensitive prostate cancer, according to a recent study published in the New England Journal of Medicine (July 27, 2017;377:352-360).. -----. Related Content. Metastatic Hormone-Naïve Prostate Cancer Effectively Treated With Combination Therapy. Lower Dosage of Prostate Cancer Drug Equally Effective When Taken With Low-Fat Meal. -----. Abiraterone acetate in combination with prednisone has demonstrated effectiveness in patients with metastatic, castration-resistant prostate cancer who have not received prior chemotherapy or in those who have received previous docetaxel. Including androgen-deprivation therapy in this regimen has been shown to reduce tumor burden in men with high-risk, localized prostate cancer who are receiving neoadjuvant therapy.. Karim Fizazi, MD, PhD, and colleagues conducted a study to ...
Prostate cancer is the most commonly diagnosed non-cutaneous malignancy in U.S. men. While tumors initially respond to androgen-deprivation therapy, the standard care for advanced or metastatic disease, tumors eventually recur as castration-resistant prostate cancer. Upregulation of the insulin-like growth factor signaling axis drives growth and progression of prostate cancer by promoting proliferation, survival, and angiogenesis. Ganitumab (formerly AMG 479) is a fully human antibody that inhibits binding of IGF-1 and IGF-2 to IGF-1R. Ganitumab decreased IGF-1 induced phosphorylation of the downstream effector AKT and reduced proliferation of multiple androgen-dependent and castration-resistant human prostate cancer cell lines in vitro albeit to varying extents. We evaluated the therapeutic value of ganitumab in several pre-clinical settings including androgen-dependent prostate cancer, castration-resistant (recurrent) prostate cancer, and in combination with androgen-deprivation therapy.
Richman EL, Kenfield SA, Stampfer MJ, Paciorek A, Carroll PR, Chan JM. Physical Activity after Diagnosis and Risk of Prostate Cancer Progression: Data from the Cancer of the Prostate Strategic Urologic Research Endeavor. Cancer Res. 2011 May 24;71(11):3889-95. • Rosario DJ, Lane JA, Metcalfe C, Donovan JL, Doble A, Goodwin L, et al. Short term outcomes of prostate biopsy in men tested for cancer by prostate specific antigen: prospective evaluation within ProtecT study. BMJ. 2012;344:d7894 ...
Clinical Scenario. A 77-year-old man presents to his primary care physician for evaluation after a single episode of rectal bleeding, which is found to be related to his known history of hemorrhoids. At the time of examination, he is found to have a firm prostate with prominent bilateral nodularity. Due to suspicion for prostate cancer, a prostate-specific antigen (PSA) test is given, which returns at 16.2 ng/mL. He then undergoes transrectal ultrasound-guided biopsy and is found to have Gleason score 4 + 4 disease in 8 of 12 cores, with 30% to 80% involvement of each core. Staging reveals no evidence for skeletal metastasis, but shows a single enlarged right internal iliac lymph node. The patient has good urinary and sexual function, and is otherwise in excellent health. After obtaining his diagnosis of high-risk prostate cancer (cT2c, Gleason score 4+4, PSA 16.2), he consults a physician who recommends androgen-deprivation therapy (ADT) alone. He presents to you seeking a second opinion, with ...
Purpose: To evaluate the survival outcomes for patients with lymph node-positive, nonmetastatic prostate cancer undergoing definitive local therapy (radical prostatectomy [RP], external beam radiation therapy [EBRT], or both) versus no local therapy (NLT) in the US population in the modern prostate specific antigen (PSA) era. Methods and Materials: The Surveillance, Epidemiology, and End Results database was queried for patients with T1-4N1M0 prostate cancer diagnosed from 1995 through 2005. To allow comparisons of equivalent datasets, patients were analyzed in separate clinical (cN+) and pathologically confirmed (pN+) lymph node-positive cohorts. Kaplan-Meier overall survival (OS) and prostate cancer-specific survival (PCSS) estimates were generated, with accompanying univariate log-rank and multivariate Cox proportional hazards comparisons. Results: A total of 796 cN+ and 2991 pN+ patients were evaluable. Among cN+ patients, 43% underwent EBRT and 57% had NLT. Outcomes for cN+ patients favored ...
Longer Duration of Androgen Deprivation Therapy Increases Risk of Depression in Early Prostate Cancer (04-25-2016) Among men with early prostate cancer, the risk of depression is increased with the use of androgen-deprivation therapy (ADT), particularly among men who are treated with ADT for 12 months or longer. It is important for patients receiving ADT to speak... Continue Reading. ...
Red and processed meat may increase risk of advanced prostate cancer. Data on postdiagnostic diet and prostate cancer are sparse, but postdiagnostic intake of poultry with skin and eggs may increase risk of disease progression. Therefore, we prospectively examined total, unprocessed, and processed red meat, poultry, and eggs in relation to risk of lethal prostate cancer (e.g., men without cancer at baseline who developed distant organ metastases or died from prostate cancer during follow-up) among 27, 607 men followed from 1994 to 2008. We also conducted a case-only survival analysis to examine postdiagnostic consumption of these foods and risk of lethal prostate cancer among the 3,127 men initially diagnosed with nonmetastatic prostate cancer during follow-up. In the incidence analysis, we observed 199 events during 306,715 person-years. Men who consumed 2.5 or more eggs per week had an 81% increased risk of lethal prostate cancer compared with men who consumed less than 0.5 eggs per week (HR: ...
Prostate Cancer News Today is strictly a news and information website about the disease. It does not provide medical advice, diagnosis or treatment. This content is not intended to be a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition. Never disregard professional medical advice or delay in seeking it because of something you have read on this website ...
Androgen deprivation therapy, one of the standard treatments for prostate cancer, induces apoptosis as well as autophagy in androgen-responsive PCa cells. As modulation of autophagy is a new paradigm for enhancing the therapeutic efficacy of various cancer therapies, we sought to determine the functions of autophagy during androgen deprivation. In this study, we confirmed that androgen removal or inhibition induces autophagy in two different hormone sensitive prostate cancer cells. Androgen deprivation also caused depletion of lipid droplets which was abrogated on inhibition of autophagy by pharmacological means (3-methyladenine, bafilomycin A1) or using a genetic approach (Atg5 siRNA). In addition, colocalization of lipid droplets and autophagic vesicles was observed in LNCaP cells, which was further enhanced by blocking the autophagic flux. These findings suggest that autophagy mediates lipid droplet degradation and lipolysis in androgen sensitive prostate cancer cells. Furthermore, inhibition of
A new analysis has found that men diagnosed with nonmetastatic prostate cancer who consumed more than 140 μg a day of supplemental selenium had over a two-and-a-half-fold excess risk for death from prostate cancer compared with nonsupplement users. On the other hand, there was a modest 12% inverse association between selenium supplementation and the risk […]. ...
Androgen deprivation therapy (ADT) is highly effective therapy for men with advanced or metastatic prostate cancer, providing at least temporary disease control in over 80 percent of cases. However, the vast majority eventually develop progressive di
Several men with metastatic, hormone-sensitive prostate cancer live longer on constant androgen-deprivation therapy, (hormone therapy), than intermittent therapy, states a study led by SWOG.
Despite current risk stratification systems using traditional clinicopathologic factors, many localized and locally advanced prostate cancers fail radical treatment (ie, radical prostatectomy, radiation therapy with or without androgen deprivation therapy). Therefore, a pressing need exists for enhanced methods of
Following the results of the TAX-327 study, questions have been raised as to whether administering chemotherapy to patient with prostate cancer before symptomatic disease progression when receiving standard hormonal treatment can improve the duration and quality of survival. The GETUG-AFU-15 and CHAARTED studies assessed the effi cacy and tolerability of androgen deprivation therapy (ADT) with or without docetaxel in patients with metastatic hormone-naive prostate cancer. Both studies included a mix of patients with de novo metastatic disease (~75%) and patients with metastases following treatment of localized disease. A short course of ADT was allowed in both trials prior to accrual. Key differences between the two studies include the number of patients with high-volume metastases (GETUGAFU- 15: 52%; CHAARTED: 65%) and number of docetaxel cycles (GETUG-AFU-15: up to nine cycles; CHAARTED six cycles). Both studies reported an improvement in progression-free survival with docetaxel plus ADT ...
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(PRWEB) August 22, 2017 -- It is well known that men who receive androgen deprivation therapy (ADT) after diagnosis of prostate cancer can experience
There is limited evidence supporting the use of local treatment (LT) for prostate cancer (PCa) patients with clinically pelvic lymph node-positive (cN1) disease.To examine the efficacy of any form of LT±androgen deprivation therapy (ADT) in treating these individuals.
... - PHILADELPHIA-A common hormone therapy to treat prostate cancer may double a mans risk of dementia, regardless of his age, Penn Medicine researchers reported in a study published online today in JAMA Oncology.. Last year, researchers discovered a dramatic association between Alzheimers disease and androgen deprivation therapy (ADT), a mainstay of treatment for prostate cancer since the 1940s currently used in over a half million men in the United States. This new study suggests a broader neurocognitive risk associated with the testosterone-lowering therapy.. While the findings do not prove that ADT increases the risk of dementia, the analysis comparing the medical records of almost 9,500 prostate cancer patients who received ADT vs. those who did not strongly supports that possibility.. "This is not an academic question anymore; this is really a clinical question that needs to be answered," said lead author Kevin T. Nead, MD, MPhil, a resident in the department of Radiation Oncology ...
Researchers at Moffitt Cancer Center and the University of South Florida have found that men with prostate cancer who receive androgen deprivation therapy may predictably suffer from fatigue if they have single nucleotide ...
December 10, 2013: Robert Bazell - Cancer and the Media: A Troubled Marriage. December 3, 2013: Shuangge Ma, PhD - Integrative Analysis of Cancer Omic Data. December 3, 2013: Samuel Katz, MD, PhD - Dissecting and Targeting Pro-Apoptotic BIM in Mantle Cell Lymphoma. November 12, 2013: Xiaoyong Yang, PhD - Cancer as a Metabolic Disease. November 12, 2013: Brian Shuch, MD - The Omics Era and Kidney Cancer: Bringing Big Data to the Bedside. September 3, 2013: Emre Seli, MD - Options for Fertility for Cancer Survivors. September 3, 2013: Beyhan Duran, RN, MS, OCN - Posttraumatic Growth as Experienced by Childhood Cancer Survivors: A Narrative Synthesis. May 14, 2013: Kavita Dhodapkar, MD - Next Generation Targeted Cancer Vaccines. May 14, 2013: Herta Chao, MD - Effects of Androgen Deprivation on Brain Function in Prostate Cancer Patients. April 16, 2013: Murat Gunel, MD, FACS, FAHA - Nextgen Genomics for Cancer Target Discovery and Individualized Therapies. April 2, 2013: Joseph Paul Eder, MD - ...
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Principal Investigator:AKAKURA Koichiro, Project Period (FY):1997 - 1998, Research Category:Grant-in-Aid for Scientific Research (C), Section:一般, Research Field:Urology
A team of UC Davis investigators, led by Christopher P. Evans, professor and chair of the Department of Urology, has received a $660,000 grant from the U.S. Department of Defense to study a promising new approach for treating advanced prostate cancer.
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Younger men diagnosed with advanced prostate cancer don t live as long as older men facing the same diagnosis, a new study finds. Overall, young men with prosta
Hello everyone. My husband and I have joined this forum because of my husbands illness. He has advanced prostate cancer with mets all over his body but no pain and the PSA is at 11 at the moment. He...
The chemotherapy drug Jevtana (cabazitaxel) has been approved by the U.S. Food and Drug Administration to treat advanced prostate cancer that worsens despite us
Because the relationship between long-term androgen use and gynecological health is not yet fully understood, and because many trans men often experience embarrassment and/or access issues over obtaining ongoing
Resistance to anti-androgen therapy is associated with increased expression of androgen receptor (AR) mRNA, AR gene amplification or AR mutation. Increased AR levels are necessary and sufficient to promote hormone-refractory growth in models and, paradoxically, alter the cellular response to classic AR antagonists such that they function as weak agonists. Therefore, second generation antiandrogens must overcome these resistance mechanisms. We searched for novel AR antagonists that might retain function in the context of increased AR expression through a cell-based screen. Using the high affinity AR agonist RU59063 as a starting point, we synthesized and screened over 200 compounds to construct a structure/activity profile that defines features of the scaffold essential for receptor binding and for maximal antagonism. We focused our further efforts on a novel compound MDV3100, which retains potent antiandrogen activity in cells expressing increased levels of AR, blocks AR function in mice and ...
Jensen, M; Morandi, S; Prinetto, F; Sjåstad, Anja Olafsen; Olsbye, Unni & Ghiotti, G (2012). FT-IR characterization of supported Ni-catalysts: Influence of different supports on the metal phase properties. Catalysis Today. ISSN 0920-5861. 197(1), s 38- 49 . doi: 10.1016/j.cattod.2012.06.016 Show summary Supported Ni catalysts (2 wt.% Ni) were investigated by FT-IR and UV-vis-NIR spectroscopy, using CO2, CH3CN and CO as probe molecules. The supports studied range from acidic (SiO2), via amphoteric (Al2O3, Mg(Al)O) to basic oxides (MgO, CaO). CO2 adsorption experiments allowed to obtain the following qualitative scale for the basic strength of O2− sites and Mn+O2− pairs: Ni/CaO , Ni/MgO ≥ Ni/Mg(Al)O ≫ Ni/Al2O3. On Ni/SiO2 these sites are absent. CH3CN adsorption allowed to reveal acidic and strong basic Lewis sites with the following results: Ni/SiO2 does not contain basic or acidic Lewis sites. Ni/Al2O3 contains acidic Lewis sites but no strong basic Lewis sites. The ratio between the ...
Stad.com contains a database with over 7 million locations in the world. From small villages to major cities, regions and countries
Stad.com contains a database with over 7 million locations in the world. From small villages to major cities, regions and countries
Is the thought of sealing yourself in a pitch-black chamber with no sound appealing to you? It is for a growing number of Americans, and it can have physical and mental benefits as...
In rare cases clients may experience nausea. This is typically indicative of a detox reaction responding to stress-which is often held in the stomach. Ultimately, releasing this stress is beneficial (though it may be uncomfortable in the moment). Ask your Float Consultant about trying the oxygen bar if you feel nausea, as this can relieve discomfort. While this level of nausea is fairly uncommon, we do ask that guests exit the Pod if they believe they may be sick. Flotation is powerful. Please remember to drink plenty of water after your session!. ...
I have had 4 treatments with Taxotere but my PSA is still going up. MedOnco ordered a CT Scan to look at the tumors in my lymph nodes around my bladder area. After he gets the results we will...
Sigma-Aldrich offers abstracts and full-text articles by [Zun Liu, Ryan E Rebowe, Zemin Wang, Yingchun Li, Zehua Wang, John S DePaolo, Jianhui Guo, Chiping Qian, Wanguo Liu].
antiandrògēn m <G mn antiandrogéna> DEFINICIJA farm. sredstvo koje blokira androgene receptore ETIMOLOGIJA anti + v. androgeni
Comments: Revised submission to Rheol. Acta. with change of title. Corresponding author is A.D. Stickland, email: [email protected] The text has been improved substantially and there is further data analysis and modelling ...
Estrogens have long played a role in the treatment of advanced prostate cancer, however the mechanism of efficacy in men who have already developed resistance to androgen-deprivation therapies has been uncertain. Estrogens induce feedback inhibition of LH secretion in patients with an intact hypothalamic-pituitary axis, resulting in decreased testosterone production. An early VA Cooperative Urology Group study compared the estrogen diethylstilbestrol (DES) to orchiectomy, and demonstrated that DES provided better cancer specific survival than orchiectomy, but cardiovascular mortality offset the improved disease control [27]. This study raised the possibility that estrogens might inhibit cancer growth independently of simple suppression of testicular androgen production. In support of that idea, our group has previously shown that estradiol inhibits multiple castration resistant human prostate cancer xenografts in castrated animals, however the mechanism remained ambiguous. This study was carried ...
RTOG 0924: Androgen Deprivation Therapy and High Dose Radiotherapy with or without Whole-pelvic Radiotherapy in Unfavorable Intermediate or Favorable High Risk Prostate Cancer: A Phase III Randomized ...
HealthDay News) -- Because testosterone can help prostate tumors grow, men with prostate cancer are often given hormone-suppressing treatment.. But new research suggests that delivering the treatment in prostate cancers early stages may, in turn, hike a mans odds for another illness -- heart failure.. The treatment in question is known as androgen-deprivation therapy.. The take-home message from the new study is that patients with localized prostate cancer should be followed to minimize the health effects of androgen-deprivation therapy on the cardiovascular system, said study author Reina Haque. Shes a researcher with the Kaiser Permanente Southern California Department of Research & Evaluation.. Haques advice? Patients should consider [heart-healthy] lifestyle changes, and physicians should actively monitor the patients health for early signs of heart disease, she said in a Kaiser Permanente news release.. A prostate cancer expert who reviewed the study agreed.. This new data is ...
Major clinical trials using prostate-specific antigen (PSA) as the screening test to detect localized early-stage prostate cancer and to attempt to change its natural history with early intervention have yielded conflicting interpretations. The US Prostate, Lung, Colorectal, and Ovarian (US PLCO) cancer screening trial concluded that PSA-based screening conferred no meaningful survival benefit, whereas the European Randomized Study of Screening for Prostate Cancer (ERSPC) and the GOTEBORG clinical trial (GOTEBORG) trials claimed statistically significant life-saving benefits. These divergent outcomes have not provided physicians with clarity on the best evidence-based treatment. To determine the extent to which these divergent outcomes are clinically meaningful, we evaluated these data and those of a long-term prospective cohort study in the context of the clinically documented harms of androgen deprivation therapy (ADT). We noted the unheralded fact that in both European trials far more ...
Standard therapy for prostate cancer, the third-leading cause of cancer-related deaths in American men, is based on blocking androgens, the male sex hormones. However, for some men, prostate cancer recurs despite androgen-deprivation therapy. A team of scientists led by Irwin Gelman, PhD, Professor of Oncology in the Department of Cancer Genetics at Roswell Park Cancer Institute, has identified an 11-gene signature unique to advanced recurrent prostate cancer that they believe will help to identify these aggressive and potentially fatal prostate cancers sooner. The findings have been published online ahead of print in the journal Oncotarget.. For this analysis, Roswell Park researchers measured genes that were specifically induced in human prostate cancer cells by the Src oncogene, a known driver of metastatic progression and recurrence in this disease. They compared these genes to genes that are only active in prostate cancer cells and tumors that have recurred after androgen-deprivation ...
New Brunswick, N.J. - In what is believed to be the first study to describe the impact on men with a high risk of bone fracture who are receiving long-term androgen deprivation therapy (ADT) for prostate cancer, new research from The Cancer Institute of New Jersey shows this population to have a higher fracture incidence following treatment completion. The findings, published in the latest online version of BJU International (doi:10.1111/j.1464-410X.2012.11758.x), also show that men who experienced a fracture had a 1.38-fold higher mortality risk than those who did not. The Cancer Institute of New Jersey is a Center of Excellence of the University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School (RWJMS).. Men with localized prostate cancer who have underlying health conditions often receive this type of therapy with the hope to shrink or delay growth of their cancer, because they are considered inappropriate candidates for more aggressive therapies such as surgery or ...
The nonsteroidal antiandrogen casodex has been described as a peripherally selective drug for the treatment of prostatic cancer. In this study we determined its activity in various models of hormone-dependent malignancies including those of the prostate and the breast. Analysis of endocrine effects in rats after 15 days of treatment revealed a strong reduction of the weights of prostates and seminal vesicles and a significant rise of testosterone serum levels as a result of the interference with central feedback mechanisms. The growth of androgen-sensitive human LNCaP/FGC prostate cancer cells was strongly inhibited by casodex. Unlike hydroxyflutamide, casodex was also active in hormone-depleted medium. The inhibitory effect was overcome by addition of testosterone propionate, which indicates an androgen-receptor-mediated mode of action. In rats bearing Dunning R3327-G prostate carcinomas casodex exerted a strong antitumour effect at the beginning of therapy. However, after 4 weeks of treatment ...
A new study raises a red flag about a therapy commonly used in advanced prostate cancer. The work suggests that whats known as androgen deprivation therapy may increase a patients risk of developing acute kidney injury.
In their study, Rivera-Arkoncel and her colleagues compared 38 men with prostate cancer who received ADT and 36 men with less advanced prostate cancer who did not receive hormonal therapy. Men in the ADT group either underwent bilateral orchiectomy at least six months earlier or received six or more months of treatment with injections of GnRH agonists. Both groups received treatment at the Philippine General Hospital from 2004 to 2010. Although the average age of the two groups was not the same at the beginning of the study, the groups were similar in terms of other diabetes risk factors, Rivera-Arkoncel said ...
@vasregret inspired me to do a similar post for my Bilateral orchiectomy. As has been previously discussed- so far so good. No regrets. I decided to go bilateral in one operation, despite advice to do one at a time, unde…
@vasregret inspired me to do a similar post for my Bilateral orchiectomy. As has been previously discussed- so far so good. No regrets. I decided to go bilateral in one operation, despite advice to do one at a time, unde…
Development of resistance to androgen deprivation therapy (ADT) is a major obstacle for the management of advanced prostate cancer. Therapies with androgen receptor (AR) antagonists and androgen withdrawal initially result in tumor regression but development of compensatory mechanisms including AR bypass signaling leads to tumor re-growth, independent of circulating androgens. The result is the emergence of castration resistant prostate cancer (CRPC), a highly morbid disease exhibiting aberrant expression of many protein-coding and non-coding genes. Under the umbrella of non-coding RNAs is a class of small regulatory RNAs referred to as microRNAs (miRNAs). MicroRNAs are believed to function in the maintenance of cell homeostasis but are often differentially expressed in many different types of cancer including CRPC. In this study, the association of genome wide miRNA expression (1113 unique miRNAs) with development of resistance to ADT was determined. Androgen sensitive prostate cancer cells that
References. 1. Heidenreich A, Bastian PJ, Bellmunt J, Bolla M, Joniau S, van der Kwast T, et al. EAU Guidelines on Prostate Cancer. Part II: Treatment of Advanced, Relapsing, and Castration- Resistant Prostate Cancer. Eur Urol. 2014;65:467-79.. 2. Cookson MS, Roth BJ, Dahm P, Engstrom C, Freedland SJ, Hussain M, et al. Castration-resistant prostate cancer: AUA guideline. 2013.. 3. NCCN. NCCN Clinical Practice Guidelines in Oncology. Prostate Cancer. 2014.. 4. Fizazi K, Scher HI, Molina A, Logothetis CJ, Chi KN, Jones RJ, et al. Abiraterone acetate for treatment of metastatic castration-resistant prostate cancer: final overall survival analysis of the COU-AA-301 randomised, double-blind, placebo-controlled phase 3 study. Lancet Oncol. 2012;13:983-92.. 5. Ryan CJ, Smith MR, de Bono JS, Molina A, Logothetis CJ, de Souza P, et al. Abiraterone in metastatic prostate cancer without previous chemotherapy. N Engl J Med. 2013;368:138-48.. 6. Scher HI, Fizazi K, Saad F, Taplin ME, Sternberg CN, Miller K, ...
Androgen deprivation therapy (ADT) is the most preferred treatment for men with metastatic prostate cancer (PCa). However, the disease eventually progresses and develops resistance to ADT in majority of the patients, leading to the emergence of metastatic castration-resistant prostate cancer (mCRPC).
TY - JOUR. T1 - Drug Insight. T2 - Testosterone and selective androgen receptor modulators as anabolic therapies for chronic illness and aging. AU - Bhasin, Shalender. AU - Calof, Olga M.. AU - Storer, Thomas W.. AU - Lee, Martin L.. AU - Mazer, Norman A.. AU - Jasuja, Ravi. AU - Montori, Victor Manuel. AU - Gao, Wenqing. AU - Dalton, James T.. PY - 2006/3. Y1 - 2006/3. N2 - Several regulatory concerns have hindered development of androgens as anabolic therapies, despite unequivocal evidence that testosterone supplementation increases muscle mass and strength in men; it induces hypertrophy of type I and II muscle fibers, and increases myonuclear and satellite cell number. Androgens promote differentiation of mesenchymal multipotent cells into the myogenic lineage and inhibit their adipogenic differentiation, by facilitating association of androgen receptors with β-catenin and activating T-cell factor 4. Meta-analyses indicate that testosterone supplementation increases fat-free mass and muscle ...
Drugs and Targets FDA approves abiraterone acetate in combination with prednisone for high-risk metastatic castration-sensitive prostate cancer. FDA approved abiraterone acetate (Zytiga) tablets in combination with prednisone for metastatic high-risk castration-sensitive prostate cancer (CSPC). The drug is sponsored by Janssen Biotech Inc.. FDA initially approved abiraterone acetate with prednisone in 2011 for patients with metastatic castration-resistant prostate cancer (CRPC) who had received prior chemotherapy, and expanded the indication in 2012 for patients with metastatic CRPC. The latest approval was based on LATITUDE (NCT01715285), a placebo controlled international clinical trial that randomized 1,199 patients with metastatic high-risk CSPC. Patients received either abiraterone acetate, 1,000 mg orally once daily with prednisone 5 mg once daily (n=597), or placebos orally once daily (n=602). Patients in both arms received a gonadotropin releasing hormone or had a bilateral orchiectomy. ...
BERKELEY, CA (UroToday.com) - Prostate cancer is the most common male cancer in North America. While better screening and treatments have resulted in improved outcomes, a subset of patients eventually develops metastatic disease. Androgen deprivation is highly effective, but eventually resistance develops, leading to a lethal disease phenotype known as metastatic castration-resistant prostate cancer (mCRPC). Traditionally, mCRPC most commonly metastasizes to the bone, and less commonly to other sites. However, coupled with recent regulatory approval of 6 distinctive therapies with different mechanisms of action in the treatment of mCRPC, we have been observing an increasing number of patients now exhibiting disease metastasis at non-osseous sites (e.g., lymph nodes, liver, lung). We thus hypothesize this drug development renaissance has altered the natural history of mCRPC, leading to the emergence of new patterns of metastases.. In our study, we evaluated the pattern of metastatic disease in ...
BACKGROUNDThe neutrophil-to-lymphocyte ratio (NLR), a marker of inflammation, has been reported to be a poor prognostic indicator in prostate cancer. Here we explore the use of the NLR to establish a simple prognostic score for men with metastatic castration-resistant prostate cancer (mCRPC) treated with docetaxel. METHODS: In the training cohort, the NLR and other known prognostic variables were evaluated among a cohort of chemotherapy-naive patients treated with thrice-weekly docetaxel at the Princess Margaret Cancer Centre. Significant prognostic variables identified by univariable Cox regression were evaluated by the area under the receiver operating characteristic curves. Multivariable Cox regression was then used to derive a prognostic score where 1 risk point was assigned for each significant variable. The model was externally validated in a cohort of patients treated at the Royal Marsden. RESULTS: Three hudred fifty-seven patients were analyzed in the training cohort. Median age was 71 ...

Androgen Antagonists | GreenMedInfo | Pharmacological ActionAndrogen Antagonists | GreenMedInfo | Pharmacological Action

Pharmacological Actions : Androgen Antagonists, Antiproliferative , Wnt/β-catenin signaling pathway modulation. Additional ... 6 Abstracts with Androgen Antagonists Research. Filter by Study Type. Animal Study. ... A novel dietary flavonoid fisetin inhibits androgen receptor signaling and tumor growth in athymic mice. Oct 15, 2008. ... A compound within Pygeum bark antagonizes human androgen receptor in the prostate gland. Sep 23, 2009. ...
more infohttp://www.greenmedinfo.com/pharmacological-action/androgen-antagonists

Androgen Antagonists - Pipeline Insights, 2017Androgen Antagonists - Pipeline Insights, 2017

Androgen Antagonists Overview. Androgen Antagonists Disease Associated. Androgen Antagonists Pipeline Therapeutics. Androgen ... Androgen Antagonists Assessment by Molecule Type. Androgen Antagonists Assessment by Stage and Molecule Type. Androgen ... Androgen Antagonists Assessment by Combination Products. Androgen Antagonists Assessment by Route of Administration. Androgen ... Androgen Antagonists Assessment by Combination Products. Androgen Antagonists Assessment by Route of Administration. Androgen ...
more infohttps://www.researchandmarkets.com/reports/4037859/androgen-antagonists-pipeline-insights-2017

Androgen antagonist - definition of Androgen antagonist by The Free DictionaryAndrogen antagonist - definition of Androgen antagonist by The Free Dictionary

Androgen antagonist synonyms, Androgen antagonist pronunciation, Androgen antagonist translation, English dictionary definition ... of Androgen antagonist. n. A substance that inhibits the biological effects of androgenic hormones ... 18) Low androgen levels, such as in those who are androgen deficient or using androgen antagonists, can result in reduced ... Androgen antagonist - definition of Androgen antagonist by The Free Dictionary https://www.thefreedictionary.com/Androgen+ ...
more infohttp://www.thefreedictionary.com/Androgen+antagonist

Potent androgen antagonists based on carborane as a hydrophobic core structure. - Semantic ScholarPotent androgen antagonists based on carborane as a hydrophobic core structure. - Semantic Scholar

We report here the design and synthesis of novel androgen antagonists bearing carborane. The most potent compounds, the ... Further development of the potent carborane-containing androgen antagonists described here, having a new skeletal structure and ... as well as in cell growth inhibition assay using androgen-dependent SC-3 cells. ... unique characteristics, may yield novel therapeutic agents, especially selective androgen receptor modulators. ...
more infohttps://www.semanticscholar.org/paper/Potent-androgen-antagonists-based-on-carborane-as-a-Fujii-Goto/d55cceba742abc0f0c087821c5ec538b96c826b3

Androgen Antagonist Activity by the Antioxidant Moiety of Vitamin E, 2,2,5,7,8-Pentamethyl-6-chromanol in Human Prostate...Androgen Antagonist Activity by the Antioxidant Moiety of Vitamin E, 2,2,5,7,8-Pentamethyl-6-chromanol in Human Prostate...

Androgen Antagonist Activity by the Antioxidant Moiety of Vitamin E, 2,2,5,7,8-Pentamethyl-6-chromanol in Human Prostate ... Androgen Antagonist Activity by the Antioxidant Moiety of Vitamin E, 2,2,5,7,8-Pentamethyl-6-chromanol in Human Prostate ... Androgen Antagonist Activity by the Antioxidant Moiety of Vitamin E, 2,2,5,7,8-Pentamethyl-6-chromanol in Human Prostate ... Androgen Antagonist Activity by the Antioxidant Moiety of Vitamin E, 2,2,5,7,8-Pentamethyl-6-chromanol in Human Prostate ...
more infohttps://mct.aacrjournals.org/content/2/8/797

Nilandron
        -
        Androgen Antagonists,  Antineoplastic Agents,  ATC:L02BB02Nilandron - Androgen Antagonists, Antineoplastic Agents, ATC:L02BB02

Nilutamide is a pure, nonsteroidal anti-androgen with affinity for androgen receptors (but not for progestogen, estrogen, or ... Prostate cancer is mostly androgen-dependent and can be treated with surgical or chemical castration. To date, antiandrogen ... glucocorticoid receptors). Consequently, Nilutamide blocks the action of androgens of adrenal and testicular origin which ...
more infohttp://pharmacycode.com/Nilandron.html

Buy Dehydroepiandrosterone (DHEA) | Androgen Receptor antagonist | Price | IC50 | Research only
			
		
		
		
		
	Buy Dehydroepiandrosterone (DHEA) | Androgen Receptor antagonist | Price | IC50 | Research only

Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, ... Darolutamide (ODM-201) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM. ... Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. ... Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. ...
more infohttps://www.selleckchem.com/products/Dehydroepiandrosterone

Enzalutamide (MDV3100) | Androgen Receptor antagonist | Read Reviews & Product Use Citations
		
	Enzalutamide (MDV3100) | Androgen Receptor antagonist | Read Reviews & Product Use Citations

... is androgen-receptor inhibitor. Highly recommended inhibitor in AR research. Find all the information about MDV3100 ( ... Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, ... Darolutamide (ODM-201) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM. ... Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. ...
more infohttps://www.selleckchem.com/products/MDV3100.html

Synthesis and pharmacological evaluation of novel arylpiperazine derivatives as nonsteroidal androgen receptor antagonists. |...Synthesis and pharmacological evaluation of novel arylpiperazine derivatives as nonsteroidal androgen receptor antagonists. |...

Synthesis and pharmacological evaluation of novel arylpiperazine derivatives as nonsteroidal androgen receptor antagonists.. [ ...
more infohttps://www.sigmaaldrich.com/catalog/papers/15516756

Non-steroid androgen receptor antagonist compounds and methods - Patent # 5677336 - PatentGeniusNon-steroid androgen receptor antagonist compounds and methods - Patent # 5677336 - PatentGenius

... antagonists for the androgen receptor are disclosed. Also disclosed are methods for employing the disclosed compounds for ... modulating processes mediated by the androgen receptor and for treating patients requiring androgen receptor antagonist therapy ... androgen receptor antagonist therapy.. Claim:. We claim:. 1. A method of antagonizing androgen activity comprising the in vivo ... steroid androgen receptor antagonist compounds disclosed can be readily utilized in pharmacological applications where androgen ...
more infohttp://www.patentgenius.com/patent/5677336.html

Abstract 2460: Discovery of potent androgen receptor antagonists for treating CRPC and AR+ breast cancer. | Cancer ResearchAbstract 2460: Discovery of potent androgen receptor antagonists for treating CRPC and AR+ breast cancer. | Cancer Research

Abstract 2460: Discovery of potent androgen receptor antagonists for treating CRPC and AR+ breast cancer.. Youzhi Tong, Chunyun ... Androgen Receptor (AR) antagonists have been used in clinic to treat prostate cancer. One example is bicalutamide (Casodex®), ... Discovery of potent androgen receptor antagonists for treating CRPC and AR+ breast cancer. [abstract]. In: Proceedings of the ... Abstract 2460: Discovery of potent androgen receptor antagonists for treating CRPC and AR+ breast cancer. ...
more infohttp://cancerres.aacrjournals.org/content/73/8_Supplement/2460

Activity of Androgen Receptor Antagonist Bicalutamide in Prostate Cancer Cells Is Independent of NCoR and SMRT Corepressors |...Activity of Androgen Receptor Antagonist Bicalutamide in Prostate Cancer Cells Is Independent of NCoR and SMRT Corepressors |...

Selection for androgen receptor mutations in prostate cancers treated with androgen antagonist. Cancer Res 1999; 59: 2511-5. ... The mechanisms by which androgen receptor (AR) antagonists inhibit AR activity, and how their antagonist activity may be ... antagonist. Introduction. The androgen receptor (AR) plays a central role in prostate cancer development and progression, and ... Activity of Androgen Receptor Antagonist Bicalutamide in Prostate Cancer Cells Is Independent of NCoR and SMRT Corepressors. ...
more infohttp://cancerres.aacrjournals.org/content/67/17/8388

Assays to Measure Estrogen and Androgen Agonists and Antagonists | Springer for Research & DevelopmentAssays to Measure Estrogen and Androgen Agonists and Antagonists | Springer for Research & Development

1998) Assays to Measure Estrogen and Androgen Agonists and Antagonists. In: del Mazo J. (eds) Reproductive Toxicology. Advances ... Olea, N., Sakabe, K., Soto, A.M. and Sonnenschein, C., 1990, The proliferative effect of "anti-androgens" on the androgen- ... DDE is a potent androgen receptor antagonist, Nature. 375: 581.PubMedCrossRefGoogle Scholar ... Androgen-induced inhibition of proliferation in human breast cancer MCF7 cells transfected with androgen receptor, ...
more infohttps://rd.springer.com/chapter/10.1007/978-1-4899-0089-0_3

Suberoylanilide hydroxamic acid (vorinostat) represses androgen receptor expression and acts synergistically with an androgen...Suberoylanilide hydroxamic acid (vorinostat) represses androgen receptor expression and acts synergistically with an androgen...

... represses androgen receptor expression and acts synergistically with an androgen receptor antagonist to inhibit prostate cancer ... represses androgen receptor expression and acts synergistically with an androgen receptor antagonist to inhibit prostate cancer ... represses androgen receptor expression and acts synergistically with an androgen receptor antagonist to inhibit prostate cancer ... represses androgen receptor expression and acts synergistically with an androgen receptor antagonist to inhibit prostate cancer ...
more infohttp://mct.aacrjournals.org/content/6/1/51

JCI -
An androgen receptor N-terminal domain antagonist for treating prostate cancerJCI - An androgen receptor N-terminal domain antagonist for treating prostate cancer

An androgen receptor N-terminal domain antagonist for treating prostate cancer. Jae-Kyung Myung,1 Carmen A. Banuelos,1 Javier ... Bicalutamide functions as an androgen receptor antagonist by assembly of a transcriptionally inactive receptor. J Biol Chem. ... The androgen receptor co-activator CBP is up-regulated following androgen withdrawal and is highly expressed in advanced ... Androgen receptor regulates a distinct transcription program in androgen-independent prostate cancer. Cell. 2009;138(2):245-256 ...
more infohttps://www.jci.org/articles/view/66398

Kinase Inhibitors | Sloan Kettering InstituteKinase Inhibitors | Sloan Kettering Institute

Androgen Antagonists. Androgen antagonists prevent the growth of prostate cancer cells and induce a G1 cell cycle arrest. The ... We are studying the effect of these antagonists on p27, cyclin E, and cyclin D/cdk complexes. We are also interested in ...
more infohttps://www.mskcc.org/research/ski/labs/neal-rosen/kinase-inhibitors

Androgen receptor antagonist suppresses exercise-induced hypertrophy of skeletal muscle - Neurontin 600 mg para que sirveAndrogen receptor antagonist suppresses exercise-induced hypertrophy of skeletal muscle - Neurontin 600 mg para que sirve

androgen receptor antagonist or. to androgen suppresses.. The third section offers an update on the physiological effects of ... androgen receptor antagonist or. to androgen suppresses sexual.Guyton and Hall Textbook of Medical Physiology, 12th edition pdf ... Androgen receptor antagonist suppresses exercise-induced hypertrophy of skeletal muscle. Medico Cirujano y Partero por la ... Androgen Optimization Simple.A receptor antagonist is a. in skeletal muscle encoded by a. rats and which increases muscle mass ...
more infohttp://tylerweitzman.tk/rylas/androgen-receptor-antagonist-suppresses-exercise-induced-hypertrophy-of-skeletal-muscle-38.php

The natural compound atraric acid is an antagonist  of the human androgen receptor inhibiting cellular  invasiveness and...The natural compound atraric acid is an antagonist of the human androgen receptor inhibiting cellular invasiveness and...

The natural compound atraric acid is an antagonist of the human androgen receptor inhibiting cellular invasiveness and prostate ... The natural compound atraric acid is an antagonist of the human androgen receptor inhibiting cellular invasiveness and prostate ... Inhibition of human AR by androgen ablation therapy and by applying synthetic anti-androgens is therefore the primary goal in ... Importantly, AA is able to efficiently repress the growth of both the androgen-dependent LNCaP and also the androgen- ...
more infohttp://www.curehunter.com/public/pubmed18627423.do

11α-Hydroxyprogesterone - Wikipedia11α-Hydroxyprogesterone - Wikipedia

Tindall, D.J.; Chang, C.H.; Lobl, T.J.; Cunningham, G.R. (1984). "Androgen antagonists in androgen target tissues". ... Lerner, Leonard J. (1975). "Androgen antagonists". Pharmacology & Therapeutics. Part B: General and Systematic Pharmacology. 1 ... It was investigated as a topical antiandrogen for the treatment of androgen-dependent skin conditions in the early 1950s, and ...
more infohttps://en.wikipedia.org/wiki/11%CE%B1-Hydroxyprogesterone

Antiandrogen - WikipediaAntiandrogen - Wikipedia

Antiandrogens, also known as androgen antagonists or testosterone blockers, are a class of drugs that prevent androgens like ... N-Terminal domain antagonists[edit]. N-Terminal domain AR antagonists are a new type of AR antagonist that, unlike all ... Androgen antagonists; Androgen blockers; Testosterone blockers. Use. • Men and boys: Prostate cancer; Benign prostatic ... Tindall DJ, Chang CH, Lobl TJ, Cunningham GR (1984). "Androgen antagonists in androgen target tissues". Pharmacol. Ther. 24 (3 ...
more infohttps://en.wikipedia.org/wiki/Antiandrogen

Primary Treatment Choice Over Time and Relative Survival of Prostate Cancer Patients: Influence of Age, Grade, and Stage.  -...Primary Treatment Choice Over Time and Relative Survival of Prostate Cancer Patients: Influence of Age, Grade, and Stage. -...

Androgen Antagonists. LinkOut - more resources. Full Text Sources. *S. Karger AG, Basel, Switzerland ... In 2000/2001, older patients were more likely to choose active surveillance (AS)/watchful waiting (WW) or to receive androgen ...
more infohttps://www.ncbi.nlm.nih.gov/pubmed/28813713

Resistance exercise in men receiving androgen deprivation therapy for prostate cancer.  - PubMed - NCBIResistance exercise in men receiving androgen deprivation therapy for prostate cancer. - PubMed - NCBI

Androgen Antagonists. LinkOut - more resources. Full Text Sources. *Atypon - PDF. *Ovid Technologies, Inc. ... Resistance exercise in men receiving androgen deprivation therapy for prostate cancer.. Segal RJ1, Reid RD, Courneya KS, Malone ... Androgen deprivation therapy is a common treatment in men with prostate cancer that may cause fatigue, functional decline, ... In a two-site study, 155 men with prostate cancer who were scheduled to receive androgen deprivation therapy for at least 3 ...
more infohttps://www.ncbi.nlm.nih.gov/pubmed/12721238

Radiation Therapy With or Without Bicalutamide and Goserelin in Treating Patients With Prostate Cancer - Full Text View -...Radiation Therapy With or Without Bicalutamide and Goserelin in Treating Patients With Prostate Cancer - Full Text View -...

Androgen Antagonists. Hormone Antagonists. Hormones, Hormone Substitutes, and Hormone Antagonists. Physiological Effects of ... Short Androgen Suppression and Radiation Dose Escalation for Intermediate- and High-Risk Localized Prostate Cancer: Results of ...
more infohttps://clinicaltrials.gov/ct2/show?term=IMRT+Prostate%09ireland&rank=2

SWOG-9346, Hormone Therapy in Treating Men With Stage IV Prostate Cancer - Full Text View - ClinicalTrials.govSWOG-9346, Hormone Therapy in Treating Men With Stage IV Prostate Cancer - Full Text View - ClinicalTrials.gov

Androgen Antagonists. Hormone Antagonists. Hormones, Hormone Substitutes, and Hormone Antagonists. Physiological Effects of ... Intermittent versus continuous androgen deprivation in prostate cancer. N Engl J Med. 2013 Apr 4;368(14):1314-25. doi: 10.1056/ ... Moinpour C, Berry DL, Ely B, et al.: Preliminary quality-of-life outcomes for SWOG-9346: Intermittent androgen deprivation in ... The effectiveness of the current depot LHRH agonist would not extend beyond 8 months after initiation of combined androgen ...
more infohttps://www.clinicaltrials.gov/ct2/show/NCT00002651
  • All test systems showed that bicalutamide and hydroxyflutamide act as potent androgen antagonists (Ma et al. (thefreedictionary.com)
  • Elevated AR expression in tumor cells correlates with a change in the functional activity of bicalutamide from antagonist to agonist, suggesting that prostate tumors may adapt to survive on any residual agonism. (aacrjournals.org)
  • MDV3100, a more potent AR antagonist (∼5x vs bicalutamide) without residual agonism, has demonstrated excellent efficacy in CRPC patients and has been approved by FDA for treating CRPC in clinic. (aacrjournals.org)
  • Recent studies show that AR antagonists (including the clinically used drug bicalutamide) can enhance AR recruitment of corepressor proteins [nuclear receptor corepressor (NCoR) and silencing mediator of retinoid and thyroid receptors (SMRT)] and that loss of corepressors may enhance agonist activity and be a mechanism of antagonist failure. (aacrjournals.org)
  • We first show that the agonist activities of weak androgens and an AR antagonist (cyproterone acetate) are still dependent on the AR NH 2 /COOH-terminal interaction and are enhanced by steroid receptor coactivator (SRC)-1, whereas the bicalutamide-liganded AR did not undergo a detectable NH 2 /COOH-terminal interaction and was not coactivated by SRC-1. (aacrjournals.org)
  • Taken together, these results indicate that bicalutamide lacks agonist activity and functions as an AR antagonist due to ineffective recruitment of coactivator proteins and that enhanced coactivator recruitment, rather than loss of corepressors, may be a mechanism contributing to bicalutamide resistance. (aacrjournals.org)
  • One mechanism that may contribute to AR reactivation is increased accumulation or synthesis of androgens by prostate cancer cells, and a subset of patients who relapse after castration or luteinizing hormone-releasing hormone agonist treatment will respond to secondary hormonal therapies with AR antagonists such as bicalutamide or to treatments that suppress residual adrenal androgen production such as ketoconozole. (aacrjournals.org)
  • However, these responses are usually partial and transient, with AR activity becoming resistant to even high doses of the AR antagonist bicalutamide through unclear mechanisms ( 5 ). (aacrjournals.org)
  • Increased AR expression can enhance the growth of prostate cancer xenografts in castrated mice and has been reported to enhance the agonist activity of the AR antagonist bicalutamide ( 10 ). (aacrjournals.org)
  • Mutant ARs that are strongly stimulated by the AR antagonist flutamide have been found in approximately one third of patients who relapse after combination therapy with flutamide, and a distinct mutant AR that is strongly stimulated by bicalutamide has been found in long-term bicalutamide-treated patients, but such mutations are uncommon in patients treated with surgical or medical castration monotherapy ( 9 , 11 ). (aacrjournals.org)
  • Moreover, a combination of low, subeffective doses of SAHA and the AR antagonist bicalutamide resulted in a synergistic reduction in cell proliferation and increase in caspase-dependent cell death. (aacrjournals.org)
  • Induction therapy: Patients receive combined androgen-deprivation (CAD) therapy comprising goserelin subcutaneously once a month and oral bicalutamide once daily for 8 courses (7 months). (clinicaltrials.gov)
  • to androgen suppresses sexual.Guyton and Hall Textbook of Medical Physiology, 12th edition pdf and chm free download.Transcriptional profiling identifies gene expression changes induced in HCV-subgenomic. (tylerweitzman.tk)
  • The majority of patients have clinical and biochemical [decrease in serum prostate-specific antigen (PSA)] evidence of improvement but eventually relapse with a more aggressive form of prostate cancer that has been termed hormone-refractory, castration-resistant, or androgen-independent prostate cancer. (aacrjournals.org)
  • Although the majority of these patients respond initially to androgen ablation, virtually all tumors eventually progress with castration-resistant disease ( 2 ). (aacrjournals.org)
  • in androgen biosynthesis and the.Na+,K+-ATPase in Skeletal Muscle: Significance of Exercise and Thyroid Hormones for. (tylerweitzman.tk)
  • Addition of exogenous androgen prevented the induction of cell death, indicating that suppression of androgen signaling was required for synergy. (aacrjournals.org)
  • Compare the overall survival, disease specific survival, and time to progression in patients with locally advanced adenocarcinoma of the prostate treated with total androgen suppression with or without pelvic irradiation. (clinicaltrials.gov)
  • Consequently, Nilutamide blocks the action of androgens of adrenal and testicular origin which stimulate the growth of normal and malignant prostatic tissue. (pharmacycode.com)
  • 1993). The endocrine and reproductive effects of xenobiotics are believed to be due to their 1) mimicking the effects of endogenous hormones such as estrogens and androgens, 2) antagonizing the effects of normal, endogenous hormones, 3) altering the pattern of synthesis and metabolism of natural hormones, and 4) modifying the hormone receptor levels. (springer.com)
  • Relative to enzalutamide and apalutamide, shows greater efficacy as an AR antagonist, improved activity against mutated AR variants in prostate cancer, little or no inhibition or induction of cytochrome P450 enzymes, and little or no central nervous system distribution. (wikipedia.org)
  • Similar to enzalutamide and apalutamide, but with increased efficacy as an AR antagonist, little or no central nervous system distribution, and no induction of seizures in animals. (wikipedia.org)
  • Further mechanisms that can enhance AR activity and may contribute to AR activation and resistance to AR antagonists include increased expression of transcriptional coactivator proteins and activation of kinases and signal transduction pathways that can modulate AR function, including the protein kinase A, c-Src, cyclin-dependent kinase 1, Ras-Raf-mitogen-activated protein kinase (MAPK), and phosphatidylinositol 3-kinase pathways ( 12 - 17 ). (aacrjournals.org)
  • However, the AR and AR-regulated genes are still expressed at high levels in androgen-independent prostate cancer, indicating that AR transcriptional activity is reactivated in these tumors and that AR remains as a potential therapeutic target ( 1 - 4 ). (aacrjournals.org)