Androgen antagonists. Medical search

Compounds which inhibit or antagonize the biosynthesis or actions of 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.

An antiandrogen with about the same potency as cyproterone in rodent and canine species.

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.

An agent with anti-androgen and progestational properties. It shows competitive binding with dihydrotestosterone at androgen receptor sites.

A potent androgenic metabolite of TESTOSTERONE. It is produced by the action of the enzyme 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE.

Tumors or cancer of the PROSTATE.

Compounds that bind to and inhibit the activation of ANDROGEN RECEPTORS.

A potent androgenic steroid and major product secreted by the LEYDIG CELLS of the TESTIS. Its production is stimulated by LUTEINIZING HORMONE from the PITUITARY GLAND. In turn, testosterone exerts feedback control of the pituitary LH and FSH secretion. Depending on the tissues, testosterone can be further converted to DIHYDROTESTOSTERONE or ESTRADIOL.

Steroidal compounds related to TESTOSTERONE, the major mammalian male sex hormone. Testosterone congeners include important testosterone precursors in the biosynthetic pathways, metabolites, derivatives, and synthetic steroids with androgenic activities.

A synthetic non-aromatizable androgen and anabolic steroid. It binds strongly to the androgen receptor and has therefore also been used as an affinity label for this receptor in the prostate and in prostatic tumors.

Chemical substances which inhibit the function of the endocrine glands, the biosynthesis of their secreted hormones, or the action of hormones upon their specific sites.

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.

Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME.

Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.

Compounds that inhibit or block the activity of NEUROKININ-1 RECEPTORS.

Agents inhibiting the effect of narcotics on the central nervous system.

Drugs that selectively bind to but do not activate histamine H2 receptors, thereby blocking the actions of histamine. Their clinically most important action is the inhibition of acid secretion in the treatment of gastrointestinal ulcers. Smooth muscle may also be affected. Some drugs in this class have strong effects in the central nervous system, but these actions are not well understood.

The relationship between the dose of an administered drug and the response of the organism to the drug.

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.

A ligand that binds to but fails to activate the INTERLEUKIN 1 RECEPTOR. It plays an inhibitory role in the regulation of INFLAMMATION and FEVER. Several isoforms of the protein exist due to multiple ALTERNATIVE SPLICING of its mRNA.

A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.

Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.

Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.

Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.

A family of hexahydropyridines.

Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.

A delta-4 C19 steroid that is produced not only in the TESTIS, but also in the OVARY and the ADRENAL CORTEX. Depending on the tissue type, androstenedione can serve as a precursor to TESTOSTERONE as well as ESTRONE and ESTRADIOL.

Drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists. Classical antihistaminics block the histamine H1 receptors only.

Drugs that bind to nicotinic cholinergic receptors (RECEPTORS, NICOTINIC) and block the actions of acetylcholine or cholinergic agonists. Nicotinic antagonists block synaptic transmission at autonomic ganglia, the skeletal neuromuscular junction, and at central nervous system nicotinic synapses.

Certain tumors that 1, arise in organs that are normally dependent on specific hormones and 2, are stimulated or caused to regress by manipulation of the endocrine environment.

Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.

Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.

Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.

C18 steroid with androgenic and anabolic properties. It is generally prepared from alkyl ethers of ESTRADIOL to resemble TESTOSTERONE but less one carbon at the 19 position.

The unspecified form of the steroid, normally a major metabolite of TESTOSTERONE with androgenic activity. It has been implicated as a regulator of gonadotropin secretion.

A major C19 steroid produced by the ADRENAL CORTEX. It is also produced in small quantities in the TESTIS and the OVARY. Dehydroepiandrosterone (DHEA) can be converted to TESTOSTERONE; ANDROSTENEDIONE; ESTRADIOL; and ESTRONE. Most of DHEA is sulfated (DEHYDROEPIANDROSTERONE SULFATE) before secretion.

Drugs that bind to but do not activate SEROTONIN 5-HT3 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT3 RECEPTOR AGONISTS.

Drugs that bind to but do not activate SEROTONIN 5-HT2 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT2 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more specific 5-HT2 receptor subtypes.

An enzyme that catalyzes the reduction of TESTOSTERONE to 5-ALPHA DIHYDROTESTOSTERONE.

A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.

A cell line derived from cultured tumor cells.

Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.

A class of drugs designed to prevent leukotriene synthesis or activity by blocking binding at the receptor level.

Agents that antagonize ANGIOTENSIN RECEPTORS. Many drugs in this class specifically target the ANGIOTENSIN TYPE 1 RECEPTOR.

The 17-beta-isomer of estradiol, an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Estradiol-17-beta is the most potent form of mammalian estrogenic steroids.

The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.

RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.

The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.

Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.

A decapeptide that stimulates the synthesis and secretion of both pituitary gonadotropins, LUTEINIZING HORMONE and FOLLICLE STIMULATING HORMONE. GnRH is produced by neurons in the septum PREOPTIC AREA of the HYPOTHALAMUS and released into the pituitary portal blood, leading to stimulation of GONADOTROPHS in the ANTERIOR PITUITARY GLAND.

Drugs that bind to but do not activate ADRENERGIC RECEPTORS. Adrenergic antagonists block the actions of the endogenous adrenergic transmitters EPINEPHRINE and NOREPINEPHRINE.

Drugs that bind to but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.

Organic compounds containing the -CN radical. The concept is distinguished from CYANIDES, which denotes inorganic salts of HYDROGEN CYANIDE.

The male gonad containing two functional parts: the SEMINIFEROUS TUBULES for the production and transport of male germ cells (SPERMATOGENESIS) and the interstitial compartment containing LEYDIG CELLS that produce ANDROGENS.

Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists. Adrenergic alpha-antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma.

Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.

Compounds which inhibit or antagonize the action or biosynthesis of estrogenic compounds.

Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).

Drugs that selectively bind to but do not activate HISTAMINE H3 RECEPTORS. They have been used to correct SLEEP WAKE DISORDERS and MEMORY DISORDERS.

A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)

A microsomal cytochrome P450 enzyme that catalyzes the 17-alpha-hydroxylation of progesterone or pregnenolone and subsequent cleavage of the residual two carbons at C17 in the presence of molecular oxygen and NADPH-FERRIHEMOPROTEIN REDUCTASE. This enzyme, encoded by CYP17 gene, generates precursors for glucocorticoid, androgen, and estrogen synthesis. Defects in CYP17 gene cause congenital adrenal hyperplasia (ADRENAL HYPERPLASIA, CONGENITAL) and abnormal sexual differentiation.

The circulating form of a major C19 steroid produced primarily by the ADRENAL CORTEX. DHEA sulfate serves as a precursor for TESTOSTERONE; ANDROSTENEDIONE; ESTRADIOL; and ESTRONE.

An enzyme that catalyzes the desaturation (aromatization) of the ring A of C19 androgens and converts them to C18 estrogens. In this process, the 19-methyl is removed. This enzyme is membrane-bound, located in the endoplasmic reticulum of estrogen-producing cells of ovaries, placenta, testes, adipose, and brain tissues. Aromatase is encoded by the CYP19 gene, and functions in complex with NADPH-FERRIHEMOPROTEIN REDUCTASE in the cytochrome P-450 system.

Elements of limited time intervals, contributing to particular results or situations.

Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action.

Compounds that interact with ESTROGEN RECEPTORS in target tissues to bring about the effects similar to those of ESTRADIOL. Estrogens stimulate the female reproductive organs, and the development of secondary female SEX CHARACTERISTICS. Estrogenic chemicals include natural, synthetic, steroidal, or non-steroidal compounds.

Cell surface proteins that bind ENDOTHELINS with high affinity and trigger intracellular changes which influence the behavior of cells.

An oxidoreductase that catalyzes the conversion of 3-oxo-delta4 steroids into their corresponding 5alpha form. It plays an important role in the conversion of TESTOSTERONE into DIHYDROTESTOSTERONE and PROGESTERONE into DIHYDROPROGESTERONE.

Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS.

A class of ionotropic glutamate receptors characterized by affinity for N-methyl-D-aspartate. NMDA receptors have an allosteric binding site for glycine which must be occupied for the channel to open efficiently and a site within the channel itself to which magnesium ions bind in a voltage-dependent manner. The positive voltage dependence of channel conductance and the high permeability of the conducting channel to calcium ions (as well as to monovalent cations) are important in excitotoxicity and neuronal plasticity.

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)

Malignant prostatic neoplasms are cancerous tumors that can be aggressive and spread to other parts of the body (metastasize). The most common type of malignant prostatic neoplasm is adenocarcinoma of the prostate, which accounts for approximately 95% of all prostate cancers. Other types of malignant prostatic neoplasms include sarcomas and small cell carcinomas.

Prostatic neoplasms can be diagnosed through a variety of tests such as digital rectal examination (DRE), prostate-specific antigen (PSA) test, imaging studies (ultrasound, CT scan or MRI), and biopsy. Treatment options for prostatic neoplasms depend on the type, stage, and grade of the tumor, as well as the patient's age and overall health. Treatment options can include active surveillance, surgery (robotic-assisted laparoscopic prostatectomy or open prostatectomy), radiation therapy (external beam radiation therapy or brachytherapy), and hormone therapy.

In summary, Prostatic Neoplasms are tumors that occur in the prostate gland, which can be benign or malignant. The most common types of malignant prostatic neoplasms are adenocarcinoma of the prostate, and other types include sarcomas and small cell carcinomas. Diagnosis is done through a variety of tests, and treatment options depend on the type, stage, and grade of the tumor, as well as the patient's age and overall health.

People with AIS typically have female physical characteristics, such as a lack of facial and body hair, a narrow pelvis, and underdeveloped genitalia. They may also experience infertility and heightened risk of certain medical conditions, such as gonadal dysgenesis and cardiovascular disease.

AIS is diagnosed through a combination of clinical evaluation, hormone level testing, and genetic analysis. Treatment options for the condition include hormone replacement therapy to promote masculinization and address any associated medical issues, as well as psychological support and counseling to address any gender identity or expression concerns.

It is important to note that AIS is a rare condition, and its prevalence is estimated to be around 1 in 10,000 to 1 in 20,000 male births. However, the condition is often misdiagnosed or undiagnosed, and some individuals may not receive an accurate diagnosis until later in life.

Overall, Androgen Insensitivity Syndrome is a complex and rare genetic disorder that can have significant implications for the physical and psychological well-being of affected individuals. It is important to provide appropriate medical care and support to those with AIS to help them live healthy and fulfilling lives.

Examples of hormone-dependent neoplasms include:

1. Breast cancer: Many breast cancers are estrogen receptor-positive (ER+), meaning that they grow in response to estrogen. These cancers can be treated with selective estrogen receptor modulators (SERMs) or aromatase inhibitors, which block the effects of estrogen on cancer growth.
2. Prostate cancer: Some prostate cancers are androgen-dependent, meaning that they grow in response to androgens such as testosterone. These cancers can be treated with androgen deprivation therapy (ADT), which reduces the levels of androgens in the body to slow or stop cancer growth.
3. Uterine cancer: Some uterine cancers are estrogen-dependent, meaning that they grow in response to estrogen. These cancers can be treated with hormone therapy to reduce estrogen levels.

Hormone-dependent neoplasms are often characterized by the presence of hormone receptors on the surface of the cancer cells. These receptors can bind to specific hormones and trigger signals that promote cancer growth and progression. Targeting these hormone receptors with hormone therapy can be an effective way to slow or stop the growth of these cancers.

... is an antiandrogen, or antagonist of the androgen receptor (AR), the biological target of androgens such as ... Clascoterone is a steroidal antiandrogen, or antagonist of the androgen receptor (AR), the biological target of androgens such ... Lerner LJ (1975). "Androgen antagonists". Pharmacol Ther B. 1 (2): 217-31. doi:10.1016/0306-039x(75)90006-9. PMID 772705. "Drug ... is an Androgen Receptor Antagonist in Dermal Papilla Cells In Vitro". J Drugs Dermatol. 18 (2): 197-201. PMID 30811143. Rosette ...

https://en.wikipedia.org/wiki/Clascoterone

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 B. 1 (2): 217-231. doi:10.1016/0306-039X(75) ... 11α-OHP was investigated as a topical antiandrogen for the treatment of androgen-dependent skin conditions in the early 1950s, ...

https://en.wikipedia.org/wiki/11α-Hydroxyprogesterone

Tindall DJ, Chang CH, Lobl TJ, Cunningham GR (1984). "Androgen antagonists in androgen target tissues". Pharmacol Ther. 24 (3 ... Singh, Shankar; Gauthier, Sylvain; Labrie, Fernand (2000). "Androgen Receptor Antagonists (Antiandrogens) Structure-Activity ... In addition, although CPA reduces androgen production in the gonads, it can increase the production of adrenal androgens, in ... The use of CPA in men has been associated with cellulite, which has been attributed to androgen deficiency as well. CPA has ...

https://en.wikipedia.org/wiki/Side_effects_of_cyproterone_acetate

... is an antiandrogen, or an antagonist of the androgen receptor (AR), the biological target of the androgen sex ... ISBN 978-3-642-80859-3. Tindall DJ, Chang CH, Lobl TJ, Cunningham GR (1984). "Androgen antagonists in androgen target tissues ... Thus we are left with CPA as the only anti-androgen that is already on the market in several countries. J. Elks (14 November ... ISBN 978-0-87489-225-3. Limited clinical experience also exists with benorterone, the first anti-androgen tried in man, and ...

https://en.wikipedia.org/wiki/Benorterone

"Androgen antagonists in androgen target tissues". Pharmacol. Ther. 24 (3): 367-400. doi:10.1016/0163-7258(84)90010-x. PMID ... It is a selective antagonist of the androgen receptor and consequently has progonadotropic effects by increasing gonadotropin ... Singh SM, Gauthier S, Labrie F (2000). "Androgen receptor antagonists (antiandrogens): structure-activity relationships". Curr ... RU-58642 RU-58841 "Compositions and methods for inhibiting the action of androgens". Tindall DJ, Chang CH, Lobl TJ, Cunningham ...

https://en.wikipedia.org/wiki/RU-22930

Ran F, Xing H, Liu Y, Zhang D, Li P, Zhao G (2015). "Recent Developments in Androgen Receptor Antagonists". Archiv der ... 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". ...

https://en.wikipedia.org/wiki/RU-59063

They are typically selective and full or silent antagonists of the androgen receptor (AR) and act by directly blocking the ... ISBN 978-1-60761-471-5. Singh SM, Gauthier S, Labrie F (2000). "Androgen receptor antagonists (antiandrogens): structure- ... Singh SM, Gauthier S, Labrie F (2000). "Androgen receptor antagonists (antiandrogens): structure-activity relationships". Curr ... An over-the-counter histamine H2 receptor antagonist that also shows very weak activity as an AR antagonist. Also inhibits ...

https://en.wikipedia.org/wiki/Nonsteroidal_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 ... There are many different androgen blockers used for transition care. Spironolactone, an aldosterone receptor antagonist, is ... ISBN 978-1-60761-471-5. Singh SM, Gauthier S, Labrie F (2000). "Androgen receptor antagonists (antiandrogens): structure- ...

https://en.wikipedia.org/wiki/Steroidal_antiandrogen

"Androgen receptor antagonists (antiandrogens): structure-activity relationships". Curr. Med. Chem. 7 (2): 211-47. doi:10.2174/ ... It shows 163% of the affinity of testosterone for the androgen receptor and negligible affinity for other steroid hormone ... synthesis and biological profile of high-affinity ligands for the androgen receptor". J. Steroid Biochem. Mol. Biol. 48 (1): ...

https://en.wikipedia.org/wiki/RU-57073

... 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 ...

https://en.wikipedia.org/wiki/Flutamide

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

https://en.wikipedia.org/wiki/Azasteroid

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 ...

https://en.wikipedia.org/wiki/AA560

CPA is a potent competitive antagonist of the androgen receptor (AR), the biological target of androgens such as testosterone ... It has been said that in combined androgen blockade regimens with castration and CPA as the AR antagonist for prostate cancer, ... Androgens: Pharmacodynamics and antagonists. Biochemical and biological studies with 4-aza-steroidal 5 alpha-reductase ... ISBN 978-1-4496-8695-6. Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): ...

https://en.wikipedia.org/wiki/Pharmacology_of_cyproterone_acetate

Antiandrogens that directly block the androgen receptor are known as androgen receptor antagonists or blockers, while ... nonsteroidal antiandrogens are highly selective for the androgen receptor and act as pure androgen receptor antagonists. ... It works as an antiandrogen mainly by acting as an androgen receptor antagonist. The medication is also a weak steroidogenesis ... In addition to its actions as an antigonadotropin, cyproterone acetate is an androgen receptor antagonist. However, this action ...

https://en.wikipedia.org/wiki/Feminizing_hormone_therapy

Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): structure-activity ... Ojasoo T, Delettré J, Mornon JP, Turpin-VanDycke C, Raynaud JP (1987). "Towards the mapping of the progesterone and androgen ... ISBN 978-1-4831-4566-2. R-2956 [41-43], a dimethyl derivative of an extremely potent androgen, R 1881 [44], is a powerful ... Takeda AN, Pinon GM, Bens M, Fagart J, Rafestin-Oblin ME, Vandewalle A (2007). "The synthetic androgen methyltrienolone (r1881 ...

https://en.wikipedia.org/wiki/Metribolone

In fact, it is actually an antagonist of the androgen receptor (AR), and hence has antiandrogenic activity. The antiandrogenic ... 63-. ISBN 978-3-319-20185-6. Singh SM, Gauthier S, Labrie F (2000). "Androgen receptor antagonists (antiandrogens): structure- ... It may be able to improve androgen-dependent symptoms such as acne and hirsutism. Metabolites of dienogest, such as 9α,10β- ... Ojasoo T, Delettré J, Mornon JP, Turpin-VanDycke C, Raynaud JP (1987). "Towards the mapping of the progesterone and androgen ...

https://en.wikipedia.org/wiki/Dienogest

... 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 ... Kemppainen JA, Wilson EM (July 1996). "Agonist and antagonist activities of hydroxyflutamide and Casodex relate to androgen ... 11-. ISBN 978-981-256-920-2. Singh, Shankar; Gauthier, Sylvain; Labrie, Fernand (2000). "Androgen Receptor Antagonists ( ...

https://en.wikipedia.org/wiki/Nilutamide

The medication is a silent antagonist of the androgen receptor. RU-56187 is 3- to 10-fold more potent as an antiandrogen than ... RU-57073 RU-58642 RU-59063 Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): ... "Distinguishing androgen receptor agonists and antagonists: distinct mechanisms of activation by medroxyprogesterone acetate and ... It shows 92% of the affinity of testosterone for the androgen receptor and negligible affinity for other steroid hormone ...

https://en.wikipedia.org/wiki/RU-56187

Kemppainen JA, Wilson EM (July 1996). "Agonist and antagonist activities of hydroxyflutamide and Casodex relate to androgen ... 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 ...

https://en.wikipedia.org/wiki/Comparison_of_bicalutamide_with_other_antiandrogens

Kemppainen JA, Wilson EM (July 1996). "Agonist and antagonist activities of hydroxyflutamide and Casodex relate to androgen ... Singh, Shankar; Gauthier, Sylvain; Labrie, Fernand (2000). "Androgen Receptor Antagonists (Antiandrogens) Structure-Activity ... a steroidal androgen receptor antagonist". J. Steroid Biochem. 33 (6): 1133-8. doi:10.1016/0022-4731(89)90420-2. PMID 2615358. ... Differential effects on high-androgen responder and low-androgen responder muscle groups". Endocrinology. 154 (12): 4594-606. ...

https://en.wikipedia.org/wiki/Hydroxyflutamide

Masiello D, Cheng S, Bubley GJ, Lu ML, Balk SP (July 2002). "Bicalutamide functions as an androgen receptor antagonist by ... Kawahara T, Minamoto H (2014). "Androgen Receptor Antagonists in the Treatment of Prostate Cancer". Clinical Immunology, ... Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): structure-activity ... It works by selectively blocking the androgen receptor (AR), the biological target of the androgen sex hormones testosterone ...

https://en.wikipedia.org/wiki/Bicalutamide

53-. ISBN 978-3-642-88429-0. Jost A (1971). "Use of androgen antagonists and antiandrogens in studies on sex differentiation". ... Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): structure-activity ... These conditions are worsened by the presence of androgens, and by suppressing androgen levels and blocking their actions, CPA ... Chemical Control of Androgen Action. Annual Reports in Medicinal Chemistry. Vol. 21. pp. 179-188. doi:10.1016/S0065-7743(08) ...

https://en.wikipedia.org/wiki/Cyproterone_acetate

ISBN 978-3-527-30247-5. Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): ...

https://en.wikipedia.org/wiki/Delanterone

Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): structure-activity ... 27 November 2013). Androgens II and Antiandrogens / Androgene II und Antiandrogene. Springer Science & Business Media. pp. 351 ... Handelsman DJ (October 2020). "Androgen Physiology, Pharmacology, Use and Misuse". In Feingold KR, Anawalt B, Boyce A, Chrousos ... Zouboulis CC, Degitz K (2004). "Androgen action on human skin -- from basic research to clinical significance". Experimental ...

https://en.wikipedia.org/wiki/Seborrhoeic_dermatitis

Singh SM, Gauthier S, Labrie F (2000). "Androgen receptor antagonists (antiandrogens): structure-activity relationships". Curr ... List of androgens/anabolic steroids R.A. Hill; H.L.J. Makin; D.N. Kirk; G.M. Murphy (23 May 1991). Dictionary of Steroids. CRC ... Androgens and anabolic steroids, Androstanes, Enones, All stub articles, Steroid stubs, Genito-urinary system drug stubs, ...

https://en.wikipedia.org/wiki/Ethyltestosterone

Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): structure-activity ... Rosterolone is a derivative of mesterolone, which, in contrast, is an androgen and anabolic steroid. Steroidal antiandrogen - ...

https://en.wikipedia.org/wiki/Rosterolone

Non-steroidal selective androgen receptor antagonists, developed as a treatment for androgen-sensitive prostate cancer, are ... Enzalutamide is an antiandrogen, and acts as an antagonist of the androgen receptor, the biological target of androgens like ... Enzalutamide acts as a selective silent antagonist of the androgen receptor (AR), the biological target of androgens like ... Rathkopf D, Scher HI (2013). "Androgen receptor antagonists in castration-resistant prostate cancer". Cancer Journal. 19 (1): ...

https://en.wikipedia.org/wiki/Enzalutamide

... is a selective competitive antagonist of the androgen receptor (AR), although it is described as an "only relatively weak ... ISBN 978-1-4831-6510-3. Singh, Shankar; Gauthier, Sylvain; Labrie, Fernand (2000). "Androgen Receptor Antagonists ( ... is not an androgen antagonist within the central nervous system". Steroids. 34 (2): 139-149. doi:10.1016/0039-128X(79)90043-6. ... On the basis of animal research, BOMT does not appear to act as an AR antagonist in central nervous system tissues, and in ...

https://en.wikipedia.org/wiki/BOMT

... is an antiandrogen, and acts as an antagonist of the androgen receptor, the biological target of androgens like ... Apalutamide acts as a selective competitive silent antagonist of the androgen receptor (AR), via the ligand-binding domain, and ... "Espacenet - Original document". Rathkopf D, Scher HI (2013). "Androgen receptor antagonists in castration-resistant prostate ... Kawahara, Takashi; Miyamoto, Hiroshi (2014). "Androgen Receptor Antagonists in the Treatment of Prostate Cancer". Clinical ...

https://en.wikipedia.org/wiki/Apalutamide

... - AdisInsight Research programme: androgen receptor antagonists (EM-4350, EM-5855, EM-6537) - AdisInsight v t e v t e ( ... Gauthier S, Martel C, Labrie F (October 2012). "Steroid derivatives as pure antagonists of the androgen receptor". J. Steroid ... The drug acts as a potent and selective competitive antagonist of the androgen receptor (AR). Unlike other steroidal ... Fujii S, Kagechika H (June 2019). "Androgen receptor modulators: a review of recent patents and reports (2012-2018)". Expert ...

https://en.wikipedia.org/wiki/EM-5854

Cutler GB, Pita JC, Rifka SM, Menard RH, Sauer MA, Loriaux DL (1978). "SC 25152: A potent mineralocorticoid antagonist with ... for the rat ventral prostate androgen receptor (AR), which is similar to that of spironolactone and its active metabolite 7α- ...

https://en.wikipedia.org/wiki/7α-Thioprogesterone

... is a strong dopamine receptor antagonist (D2 (Ki 0.027 nM) and D4 (Ki 0.066 nM)) with weaker serotonin receptor ... as an alternative to anti-androgen drugs such as cyproterone acetate. Benperidol was discovered by Janssen Pharmaceutica in ... "Endocrine changes in male sexual deviants after treatment with anti-androgens, oestrogens or tranquillizers". The Journal of ...

https://en.wikipedia.org/wiki/Benperidol

... oligomenorrhea and infertility in women due to elevations in androgens. Studies have also shown that the resultant amenorrhea ... Mifepristone is a powerful glucocorticoid type II receptor antagonist and, since it does not interfere with normal cortisol ... abnormalities in women with Cushing's disease are correlated with hypercortisolemia rather than raised circulating androgen ...

https://en.wikipedia.org/wiki/Cushing's_syndrome

Dexamethasone and other corticosteroids are agonists, while mifepristone and ketoconazole are antagonists of the GR. ... and androgen receptors". Pharmacological Reviews. 58 (4): 782-797. doi:10.1124/pr.58.4.9. PMID 17132855. S2CID 28626145. [Free ... a nuclear protein that interacts with and regulates transcriptional activity of androgen receptor and glucocorticoid receptor ...

https://en.wikipedia.org/wiki/Glucocorticoid_receptor

Some androgen-independent LNCaP sublines have been developed from the ATCC androgen-dependent LNCaP cells after androgen ... "5-lipoxygenase antagonist therapy: a new approach towards targeted cancer chemotherapy". Acta Biochimica et Biophysica Sinica. ... These androgen-independent LNCaP cells have elevated AR expression and express prostate specific antigen upon androgen ... The proliferation of LNCaP cells is androgen-dependent but the proliferation of PC-3 and DU-145 cells is androgen-insensitive. ...

https://en.wikipedia.org/wiki/Prostate_cancer

... including of androgens, estrogens, glucocorticoids, mineralocorticoids, and neurosteroids. Steroidogenesis inhibitor Androgen ... synthesis inhibitor Estrogen synthesis inhibitor Ray S, Sharma I (1987). "Development of progesterone antagonists as fertility ...

https://en.wikipedia.org/wiki/Progesterone_synthesis_inhibitor

... androgen receptor - angiotensin - angiotensin II - angiotensin receptor - ankyrin - annexin II - antibiotic - antibody - ... receptor antagonist - receptor protein-tyrosine kinase - recombinant fusion protein - recombinant interferon-gamma - ...

https://en.wikipedia.org/wiki/Index_of_biochemistry_articles

Binding of antagonist ligands to nuclear receptors in contrast induces a conformation of the receptor that preferentially binds ... such as the androgen receptor, estrogen receptors, glucocorticoid receptor, and progesterone receptor. It has been noted that ... Antagonist ligands work by inducing a conformation of the receptor which prevents coactivator and promotes corepressor binding ... These ligands are referred to as antagonists. An example of antagonistic nuclear receptor drug is mifepristone which binds to ...

https://en.wikipedia.org/wiki/Nuclear_receptor

Androgen receptor antagonists such as flutamide and bicalutamide cause little to no decrease in sexual desire in women. Low ... High-dosage monotherapy with an androgen receptor antagonist such as bicalutamide or enzalutamide, which preserves testosterone ... Research suggests androgens, such as testosterone, are not sufficient by themselves to prompt sexual motivation in females. In ... Menopause is associated with a rapid decline of estrogen, as well as a steady rate of decline of androgens. The decline of ...

https://en.wikipedia.org/wiki/Effects_of_hormones_on_sexual_motivation

Steroidal anti-androgens are a class of steroid drugs that inhibit the actions of androgens. Cyproterone acetate, a 17- ... It compiles a serotonin 1A receptor agonist and a serotonin 2A receptor antagonist. and is an antidepressant that was ... Cyproterone acetate suppresses libido by directly reducing the level of active androgen, testosterone, in males. The ... In addition to this mechanism, it also competes for the androgen receptors against testosterone and dihydrotestosterone, ...

https://en.wikipedia.org/wiki/Drugs_and_sexual_desire

The drug is a high-affinity antagonist of the androgen receptor (AR) with a Ki value of 26 nM and has been found to inhibit ... Gao W, Kim J, Dalton JT (2006). "Pharmacokinetics and pharmacodynamics of nonsteroidal androgen receptor ligands". Pharm. Res. ... Nyrönen TH, Söderholm AA (2010). "Structural basis for computational screening of non-steroidal androgen receptor ligands". ... "Selective androgen receptor modulators". Expert Opinion on Therapeutic Patents. 13 (1): 59-66. doi:10.1517/13543776.13.1.59. ...

https://en.wikipedia.org/wiki/LG-120907

October 2000). "Steroid-induced androgen receptor-oestradiol receptor beta-Src complex triggers prostate cancer cell ... Antagonists of ERβ selective over ERα include: PHTPP (R,R)-Tetrahydrochrysene ((R,R)-THC) - actually not selective over ERα, ... but rather an agonist instead of antagonist of ERα Estrogen receptor beta has been shown to interact with: CCND1, ESR1 MAD2L1, ... "Differential response of estrogen receptor alpha and estrogen receptor beta to partial estrogen agonists/antagonists". ...

https://en.wikipedia.org/wiki/Estrogen_receptor_beta

... a fourth generation GnRH antagonist, induces apoptosis in hormone refractory androgen receptor negative prostate cancer cells ... Ozarelix (developmental code names D-63153, SPI-153) is a peptide gonadotropin-releasing hormone antagonist (GnRH antagonist) ... Gonadotropin-releasing hormone receptor § Antagonists "Ozarelix - AdisInsight". Festuccia C, Dondi D, Piccolella M, Locatelli A ... GnRH antagonists, Hormonal antineoplastic drugs, Peptides, All stub articles, Genito-urinary system drug stubs, Systemic ...

https://en.wikipedia.org/wiki/Ozarelix

... the tendency to attack intruder males decreases as the dose of antagonist increases. This antagonist has been known to decrease ... Androgens in particular have well documented effects on enhancing aggression in male rodents, and testosterone injections into ... It is hypothesized[by whom?] that serotonin acts as an antagonist to vasopressin by eliciting its effects on vasopressin- ... 1990) suggests that when a vasopressin receptor antagonist is injected into the anterior hypothalamus of the resident male, ...

https://en.wikipedia.org/wiki/Agonistic_behaviour

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

https://en.wikipedia.org/wiki/Cruciferous_vegetables

Mixed agonist/antagonist and partial agonist opioids may reduce the analgesic effect of benzhydrocodone/APAP or cause ... Chronic hydrocodone use can lead to androgen deficiency, which may result in low libido, impotence, erectile dysfunction, ...

https://en.wikipedia.org/wiki/Benzhydrocodone

In addition to the mineralocorticoid receptor, mexrenone also binds to the glucocorticoid, androgen, and progesterone receptors ... Cutler GB, Sauer MA, Loriaux DL (1979). "SC 25152: a potent mineralocorticoid antagonist with decreased antiandrogenic activity ... Hofmann LM, Weier RM, Suleymanov OD, Pedrera HA (1977). "Mexrenoate potassium: a steroidal aldosterone antagonist and ... A Potent Mineralocorticoid Antagonist with Reduced Affinity for the 5α-Dihydrotestosterone Receptor of Human and Rat Prostate ...

https://en.wikipedia.org/wiki/Mexrenone

v t e Hormone levels with GnRH agonists and antagonists Testosterone levels during the first month of androgen deprivation ... Usage of GnRH agonist for this purpose necessitates using a GnRH antagonist instead of a GnRH agonist for suppression of ... Common side effects of the GnRH agonists and antagonists include symptoms of hypogonadism such as hot flashes, gynecomastia, ... Testosterone levels in the long-term androgen deprivation therapy of men with prostate cancer by different GnRH agonists ...

https://en.wikipedia.org/wiki/Gonadotropin-releasing_hormone_agonist

In short GnRH-antagonist protocols metformin may reduce live birth rates with uncertainty on its effect on clinical pregnancy ... androgen excess, and oligomenorrhea in adolescence". The Journal of Clinical Endocrinology and Metabolism. 96 (8): E1262-7. doi ... The H2-receptor antagonist cimetidine causes an increase in the plasma concentration of metformin by reducing clearance of ... found that metformin was only slightly effective for decreasing androgen levels in women with PCOS. Metformin also has ...

https://en.wikipedia.org/wiki/Metformin

... bicalutamide acts as a selective antagonist of the androgen receptor (AR), the biological target of androgens like testosterone ... For comparison, the androgen antagonists flutamide and bicalutamide reduced both prostate and levator ani weights by 51 to 67% ... 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 ...

https://en.wikipedia.org/wiki/Pharmacology_of_bicalutamide

... , sold under the brand name Inspra, is an aldosterone antagonist type of potassium-sparing diuretic that is used to ... However, in contrast to spironolactone, eplerenone has little affinity for the androgen, progesterone, and glucocorticoid ... ISBN 978-0-9757919-2-9. Craft J (April 2004). "Eplerenone (Inspra), a new aldosterone antagonist for the treatment of systemic ... It is a steroidal antimineralocorticoid of the spirolactone group and a selective aldosterone receptor antagonist (SARA). ...

https://en.wikipedia.org/wiki/Eplerenone

The fossa was depicted as an antagonist in the 2005 DreamWorks animated film Madagascar, being referred to as the "foosa", and ... "Exposure to naturally circulating androgens during foetal life incurs direct reproductive costs in female spotted hyenas, but ...

https://en.wikipedia.org/wiki/Fossa_(animal)

Lundström E, Conner P, Naessén S, Löfgren L, Carlström K, Söderqvist G (2015). "Estrone - a partial estradiol antagonist in the ... though they can also be formed from adrenal androgens in adipose tissue. Relative to estradiol, both estrone and estriol have ...

https://en.wikipedia.org/wiki/Estrone

Some steroid antagonists: Androgen: cyproterone acetate Progestins: mifepristone, gestrinone Steroid hormones are transported ... and androgens, estrogens, and progestogens (sex steroids). Vitamin D derivatives are a sixth closely related hormone system ... dihydrotachysterol Androgens: oxandrolone, oxabolone, nandrolone (also known as anabolic-androgenic steroids or simply anabolic ...

https://en.wikipedia.org/wiki/Steroid_hormone

Valproic acid has been found to be an antagonist of the androgen and progesterone receptors, and hence as a nonsteroidal ... Valproic acid has been found to directly stimulate androgen biosynthesis in the gonads via inhibition of histone deacetylases ... Death AK, McGrath KC, Handelsman DJ (December 2005). "Valproate is an anti-androgen and anti-progestin". Steroids. 70 (14): 946 ...

https://en.wikipedia.org/wiki/Valproate

What is more clear is that DDE is a weak androgen receptor antagonist and can produce male genital tract abnormalities. ...

https://en.wikipedia.org/wiki/Dichlorodiphenyldichloroethylene

Androgen-dependent condition Estrogen insensitivity syndrome "Estrogen: Hormone, Function, Levels & Imbalances". Cleveland ... estrogen receptor antagonists such as fulvestrant, aromatase inhibitors such as anastrozole and exemestane, gonadotropin- ...

https://en.wikipedia.org/wiki/Estrogen-dependent_condition

In addition, it has also been found to act as a competitive antagonist of the androgen receptor (AR), with potency reportedly ... "Redirecting abiraterone metabolism to fine-tune prostate cancer anti-androgen therapy" (PDF). Nature. 533 (7604): 547-51. ...

https://en.wikipedia.org/wiki/Δ4-Abiraterone

... On-line free medical diagnosis assistant. Ranked list of possible diseases from either several ... Androgen Receptor Antagonists. Compounds that bind to and inhibit the activation of ANDROGEN RECEPTORS. ...

https://lookfordiagnosis.com/mesh_info.php?term=Androgen+Receptor+Antagonists&lang=1

The Androgen Receptor (AR) is the main driver of prostate cancer and functions in conjunction with chromatin modifications. ... The Androgen Receptor (AR) is the key-driving transcription factor in prostate cancer, tightly controlled by epigenetic ... Agonist and antagonist switch DNA motifs recognized by human androgen receptor in prostate cancer. EMBO J. 34, 502-516 (2015). ... The androgen receptor induces a distinct transcriptional program in castration-resistant prostate cancer in man. Cancer Cell 23 ...

https://www.nature.com/articles/s41467-018-07270-2?error=cookies_not_supported&code=5efd5f64-7726-4ba6-993a-fd54629a10ef

Spironolactone is an aldosterone antagonist that inhibits ovarian and adrenal production of androgens. It competes with ... Cyproterone (not available in the United States) inhibits androgen binding to target cells. ...

https://emedicine.medscape.com/article/1073117-medication

novel androgen receptor inhibitor for patients with for mCRPC, ARAMIS trial, metastatic prostate cancer, ARCHES trial ... Darolutamide is a structurally unique androgen-receptor antagonist that is under development for the treatment of prostate ... The results show that enzalutamide plus androgen deprivation therapy (ADT) met the primary endpoint by significantly reducing ...

https://www.urotoday.com/video-lectures/nmcrpc/video/mediaitem/1157-darolutamide-demonstrates-efficacy-and-safety-in-men-with-nmcrpc-neeraj-agarwal.html

Kintor OKd to Start US Trial of Androgen Receptor Antagonist for COVID-19 $5.00 Available ...

http://www.chinabiotoday.com/store/?p=71

The FDA recently announced approval of the novel nonsteroidal androgen receptor (AR) antagonist for the treatment of this ... Novel nonsteroidal AR antagonist shows benefit in treating nmCRPC. Aug 6, 2019. Cheryl Guttman Krader, BS, Pharm ... "Recently, two AR antagonists, namely apalutamide [Erleada] and enzalutamide [XTANDI], demonstrated improvements in metastasis- ... After adjustment for duration of treatment exposure, the incidence of all adverse events associated with AR antagonists was ...

https://www.urologytimes.com/view/novel-nonsteroidal-ar-antagonist-shows-benefit-treating-nmcrpc

LH-RH antagonists are another class of treatments, including degarelix (Firmagon) and relugolix (Orgovyx). They reduce androgen ... Androgen deprivation therapy; ADT; Androgen suppression therapy; Combined androgen blockade; Orchiectomy - prostate cancer; ... Androgens are male sex hormones. Testosterone is one main type of androgen. Most testosterone is made by the testicles. The ... Androgens cause prostate cancer cells to grow. Hormone therapy for prostate cancer lowers the effect level of androgens in the ...

https://medlineplus.gov/ency/patientinstructions/000908.htm

Balk, 2002, Androgen receptor as a target in androgen-independent prostate cancer., Urology ... Pastor-Soler et al., 2002, Expression of aquaporin 9 in the adult rat epididymal epithelium is modulated by androgens., Biol. ... Pastor-Soler et al., 2002, Expression of aquaporin 9 in the adult rat epididymal epithelium is modulated by androgens., Biol. ... Pazos et al., 2000, Mechanisms of reduced body growth in the pubertal feminized male rat: unbalanced estrogen and androgen ...

https://www.dgidb.org/drugs/FLUTAMIDE

An anti-androgen, (or androgen antagonist) is any of a group of hormone antagonist compounds that are capable of preventing or ... Weaker Anti-androgens. There are a class of anti-androgens, less commonly used in HRT, due to their weaker anti-androgen effect ... Strong Anti-androgens. These two anti-androgens are most popular as primary treatment for HRT, Spironolactone and Cyproterone ... When the tissues do not respond normally to androgens, this is known as Androgen Insensitivity Syndrome. ...

https://susans.org/wiki/Antiandrogen

Vinclozolin (Vin CAS 50471-44-8), a dicarboximide fungicide, has been reported be an antagonist of androgen receptor binding in ...

http://www2a.cdc.gov/nioshtic-2/BuildQyr.asp?s1=skin&t3=1&f1=%2A&s5=percutaneous&Startyear=&t1=1&s2=dermal&t4=1&terms=7&Adv=1&ct=&B1=Search&f2=%2A&t2=1&Limit=500&Sort=DP+DESC&s3=dermatitis&f3=%2A&s4=cutaneous&EndYear=&f4=%2A&f5=%2A&whichdate=DP&D1=10&PageNo=250&RecNo=2496&View=f&

keywords = "androgen antagonists, castration, prostatic neoplasms, testosterone",. author = "Juan Morote and Anna Orsola and ... However, maximal androgen blockade provided a significantly longer survival free of androgen independent progression in those ... However, maximal androgen blockade provided a significantly longer survival free of androgen independent progression in those ... However, maximal androgen blockade provided a significantly longer survival free of androgen independent progression in those ...

https://portalrecerca.uab.cat/en/publications/redefining-clinically-significant-castration-levels-in-patients-w

Androgen Antagonists Entry term(s):. Androgen Antagonist. Antagonist, Androgen. Antagonists, Androgen. Anti Androgen Effect. ... Antagonist, Androgen Receptor. Antagonists, Androgen Receptor. Receptor Antagonist, Androgen. Receptor Antagonists, Androgen. ... Agonist, Androgen Receptor. Agonists, Androgen Receptor. Androgen. Androgen Effect. Androgen Effects. Androgen Receptor Agonist ... Analogues, Androgen. Androgen Analogs. Androgen Analogues. Androgens, Synthetic. Synthetic Androgen. Synthetic Androgens. ...

https://decs.bvsalud.org/en/ths/?filter=ths_termall&q=andr%C3%B3genos&sort=name

Androgen receptor signaling in androgen-refractory prostate cancer. Grossmann, M. E., Huang, H. & Tindall, D. J., Nov 21 2001, ... Posttranslational regulation of androgen dependent and independent androgen receptor activities in prostate cancer. Wen, S., ... The androgen receptor: A potential target for therapy of prostate cancer. Santos, A. F., Huang, H. & Tindall, D. J., Feb 1 2004 ... The role of the androgen receptor in prostate cancer. Huang, H. & Tindall, D. J., 2002, In: Critical Reviews in Eukaryotic Gene ...

https://mayoclinic.pure.elsevier.com/en/persons/haojie-huang/publications/?type=%2Fdk%2Fatira%2Fpure%2Fresearchoutput%2Fresearchoutputtypes%2Fcontributiontojournal%2Fsystematicreview&ordering=title&descending=false

LHRH antagonist. No 2003. 2005. Jan. 1, 2005 No Longer Used. J0128. Abarelix Plenaxis. 10 mg. Hormonal Therapy Androgen ... LHRH antagonist. No 2003. 2005. Jan. 1, 2005 No Longer Used. S0165. Abarelix Plenaxis. 100 mg. Hormonal Therapy Androgen ... LHRH antagonist. No 2003. 2005. Jan. 1, 2005 No Longer Used. J9060. Cisplatin Platinol, Platinol-AQ. 10 mg. Chemotherapy ...

https://seer.cancer.gov/oncologytoolbox/canmed/hcpcs/?s=-brandname&p=9

Androgen receptor antagonists produced by Streptomyces overcome resistance to enzalutamide. Imoto, M., Fujimaki, T., Saito, S. ... Androgen and reproductive physiology. Sueoka, K., 2006 4月, In: Nippon rinsho. Japanese journal of clinical medicine. 64 Suppl 4 ...

https://keio.pure.elsevier.com/ja/organisations/keio-university-2/publications/?type=%2Fdk%2Fatira%2Fpure%2Fresearchoutput%2Fresearchoutputtypes%2Fcontributiontojournal%2Fsystematicreview&ordering=type&descending=false&page=3

Darolutamide is a nonsteroidal androgen receptor antagonist for the treatment of nonmetastatic castrate-resistant prostate ... occurs in the majority of patients with advanced prostate cancer who have been treated with androgen receptor antagonists. ...

https://affygility.com/oel/darolutamide.html

Novel androgen receptor pathway antagonists are expanding treatment options. Cost and access to contemporary treatments and ...

https://pesquisa.bvsalud.org/portal/?lang=pt&q=au:T%C3%BCrkeri,+Levent

ICD-10 code T38.7X2S for Poisoning by androgens and anabolic congeners, intentional self-harm, sequela is a medical ... Excludes1: mineralocorticoids and their antagonists (T50.0-). oxytocic hormones (T48.0-). parathyroid hormones and derivatives ... Poisoning by androgens and anabolic congeners, intentional self-harm, sequela T38. ... ICD-10-CM Code for Poisoning by androgens and anabolic congeners, intentional self-harm, sequela T38.7X2S ICD-10 code T38.7X2S ...

https://www.aapc.com/codes/icd-10-codes/T38.7X2S

Androgen receptor antagonist. US approval. Prostate cancer. Q4. 2,472. 78%. MDV3100. Astellas Pharma. Androgen receptor ... Opioid antagonist. EU approval. Alcohol dependence. Q3. 72. 2%. Crofelemer. Salix Pharmaceuticals. CFTR channel & calcium- ... Mu opioid antagonist. US approval. Opoid induced constipation. 27 Jul. 733. 250%. ... antagonist. US approval. Prostate cancer. Q4. 2,016. 11%. Kyprolis. Onyx Pharmaceuticals. Proteasome inhibitor. US approval. ...

https://www.evaluate.com/vantage/articles/analysis/key-regulatory-events-next-six-months-q3-and-q4-2012

1 Androgen Antagonists. *1 Androgen Deprivation Therapy. *. next > Date issued. *4 2023 ...

https://imsear.searo.who.int/handle/123456789/149612/simple-search?filterquery=Hypertension&filtername=subject&filtertype=equals

Androgen Receptor Antagonists 22% * The Development and Preclinical Evaluation of a Theronostic Nanovehicle Drug for Treating ...

https://hub.tmu.edu.tw/en/organisations/taipei-medical-university-2/projects/?status=FINISHED&ordering=statusStartDate&descending=true&page=82

Ski-interacting protein (SKIP) interacts with androgen receptor in the nucleus and modulates androgen-dependent transcription. ... Our in vitro and in vivo experimental studies revealed N6L anti-tumoral activity in numerous androgen-dependent or -independent ... C. Effect of the combination of N6L and androgen deprived (AD) condition. LNCaP cells were treated for 24 hours with N6L or ... Since DU145 cells are androgen-independent and sensitive to docetaxel and N6L, we thought to use this model to evaluate the ...

https://www.oncotarget.com/article/8043/text/

H2 receptor antagonists, fibrates, propoxyphene, pentoxifylline, somatostatin analogs, anabolic steroids and androgens, ...

https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=7f80bf43-18ae-1b1f-e053-2991aa0ace24&type=display

Androgen antagonists: Potential role in prostate cancer prevention. Urology. Apr 2001;57(4 Suppl 1):64-7. ...

https://francais.dev01.medscape.com/voirarticle/3600071_8

And androgen receptor (AR) antagonist with IC50. *Pure Pharmaceuticals Steroids. *Alpha Pharma Oxydrolone ... Androgen receptors then tell cells to fire up their cardiovascular protection can general structure, with. ...

https://edward-kim.com/fast-muscle-co-stanozolol.html

An updated review of environmental estrogen and androgen mimics and antagonists. Sonnenschein C, Soto AM. J Steroid Biochem Mol ... Estrogen-androgen levels in aging men and women: therapeutic considerations. Greenblatt RB, Oettinger M, Bohler CS J Am Geriatr ... Androgen and estrogen production in elderly men with gynecomastia and testicular atrophy after mumps orchitis. Aiman J, Brenner ... Age variation of the 24-hour mean plasma concentrations of androgens, estrogens, and gonadotropins in normal adult men. Zumoff ...

https://antiaging-nutrition.com/articles/estrogen-the-unrecognized-male-hormone/

Cyproterone acetate. A progestin, anti-androgen, and androgen receptor antagonist; usually combined with birth control pills. ... Home Hair Loss Treatment Options Drug Treatment Options Ovarian Anti-Androgens for Hair Loss ... In women, oral contraception pills for preventing pregnancy can be used to counteract androgen hormone activity to treat female ... Non-birth control drugs that suppress ovarian androgen hormones include:(15, 30) ...

https://www.thinninghair.com/hair-loss-treatment-options/drug-treatment-options/295-ovarian-anti-androgens-for-hair-loss

The Androgen Receptor (AR) is the key-driving transcription factor in prostate cancer, tightly controlled by epigenetic regulation. (nature.com)
Darolutamide is a structurally unique androgen-receptor antagonist that is under development for the treatment of prostate cancer. (urotoday.com)
The FDA recently announced approval of the novel nonsteroidal androgen receptor (AR) antagonist for the treatment of this patient population. (urologytimes.com)
The UCLA team of chemists and biologists then used preclinical models to identify novel androgen receptor antagonists that blocked the growth of tumors, and it was these studies led to the clinical development of enzalutamide. (uclahealth.org)
Vinclozolin (Vin CAS 50471-44-8), a dicarboximide fungicide, has been reported be an antagonist of androgen receptor binding in rats, effects that could result in decreased fertility, defects in reproductive organs or cancer. (cdc.gov)
Darolutamide is a nonsteroidal androgen receptor antagonist for the treatment of nonmetastatic castrate-resistant prostate cancer (nmCRPC). (affygility.com)
This condition occurs in the majority of patients with advanced prostate cancer who have been treated with androgen receptor antagonists. (affygility.com)
Furthermore, NPM1 binds to androgen receptor (AR) and modulate its activity. (oncotarget.com)
We showed that phosphorylated forms of NPM1 interact with androgen receptor (AR) in nucleoplasm. (oncotarget.com)
Propecia is not approved for use as an androgen-receptor antagonist or as a 5-a reductase inhibitor. (bountybooks.net)
Today we'll be discussing mineralocorticoid receptor antagonists (MRAs) for diabetic kidney disease. (medscape.com)

Compounds that bind to and inhibit the activation of ANDROGEN RECEPTORS. (lookfordiagnosis.com)
Anti-androgens preferentially block the appropriate receptors, competing for binding sites on the cell's surface, effectively inhibiting the androgens' pathway. (susans.org)

All patients continued on androgen deprivation therapy. (urologytimes.com)
Androgen deprivation therapy can increase the risks for diabetes and heart disease. (medlineplus.gov)
abstract = "Purpose: We determined the testosterone castration level with clinical relevance in patients with prostate cancer on continuous androgen deprivation therapy. (uab.cat)

When the tissues do not respond normally to androgens, this is known as Androgen Insensitivity Syndrome . (susans.org)

Recently, two AR antagonists, namely apalutamide [Erleada] and enzalutamide [XTANDI], demonstrated improvements in metastasis-free survival (MFS) in men with nmCRPC. (urologytimes.com)
Jung and Drs. Charles Sawyers and Howard Scher of the Memorial Sloan Kettering Cancer Center are being recognized for their groundbreaking work in the discovery and development of the anti-androgen drug enzalutamide (Xtandi). (uclahealth.org)

Androgens cause prostate cancer cells to grow. (medlineplus.gov)
Hormone therapy for prostate cancer lowers the effect level of androgens in the body. (medlineplus.gov)
Some drugs that work by blocking the effect of androgen on prostate cancer cells. (medlineplus.gov)
Some prostate cancer cells can also make androgens. (medlineplus.gov)
Anti-androgens are often indicated to treat severe male sexual disorders, such as hypersexuality, (excessive sexual desire) "sexual deviation", and in hormonal therapy in prostate cancer, where there is a direct link between testosterone and the spread of cancer. (susans.org)
Materials and Methods: Serum testosterone was determined 3 times (in 6 months) in 73 patients with nonmetastatic prostate cancer treated with medical castration, 28 (38.4%) of whom also received bicalutamide (maximal androgen blockade). (uab.cat)
Maximal androgen blockade might benefit medically castrated cases of prostate cancer with breakthrough increases of more than 50 ng/dl. (uab.cat)
A clinical trial is being conducted to see the benefit of a known lipid-lowering drug such as pitavastatin in patients with advanced prostate cancer who are being treated with the new anti-androgens. (who.int)

They are called luteinizing hormone-releasing hormone (LH-RH) analogs (injections) and anti-androgens (oral tablets). (medlineplus.gov)

In the initial studies, Sawyers determined that androgen overexpression was responsible for fueling the growth and survival of castration-resistant prostate cancers. (uclahealth.org)
Surgery to remove the testicles (castration) stops the production of most androgens in the body. (medlineplus.gov)
During a mean followup of 51 months (range 12 to 240) 41 (67.1%) events of androgen independent progression were identified, and correlated with breakthrough testosterone increases of 50 ng/dl (classic level) and 20 ng/dl (surgical castration level). (uab.cat)

Compounds which inhibit or antagonize the biosynthesis or actions of androgens. (bvsalud.org)
An anti-androgen , (or androgen antagonist ) is any of a group of hormone antagonist compounds that are capable of preventing or inhibiting the biological effects of androgens , ( male sex hormones ) on normally responsive tissues in the body, which maintain male secondary sex characteristics . (susans.org)

Testosterone is one main type of androgen. (medlineplus.gov)
Secondary objectives were to analyze the role of associated bicalutamide in breakthrough increases of serum testosterone in these patients and the possible benefit of maximal androgen blockade. (uab.cat)
The lowest testosterone level with a significant impact on survival free of androgen independent progression was 32 ng/dl. (uab.cat)
Patients on maximal androgen blockade had an incidence of testosterone increase similar to those receiving monotherapy. (uab.cat)
sous la marque Anavar,, https://individuelprox.com/achater-du-sustanon-en-europe-booster-de-testosterone-musculation-avis/ . (mediatimenews.com)
As you likely already know, testosterone is the primary sex hormone in males, but healthy females also produce only small amounts of this androgen. (atplab.com)
Believe it or not, in male and females, the main starting materials for estrogen production are androgens (testosterone and adrostenedione). (atplab.com)

The [current] results show that darolutamide significantly improves MFS, has a very favorable safety profile with apparently no side effects associated with other AR antagonists, and delays worsening of pain and disease-related symptoms compared with placebo. (urologytimes.com)

Androgens are male sex hormones. (medlineplus.gov)

The most common treatment is to take drugs that lower the amount of androgens made by the testicles. (medlineplus.gov)
These drugs lower androgen levels just as well as surgery does. (medlineplus.gov)
Three drugs help to stop the body from making androgens from tissue other than the testicles. (medlineplus.gov)

However, maximal androgen blockade provided a significantly longer survival free of androgen independent progression in those with breakthrough increases greater than 50 ng/dl. (uab.cat)
Breakthrough increases greater than this threshold predicted a lower survival free of androgen independent progression. (uab.cat)

In women, oral contraception pills for preventing pregnancy can be used to counteract androgen hormone activity to treat female pattern hair loss. (thinninghair.com)

In the instance that puberty has either just started or is in progress, a strong anti-androgen will either reduce, or in some cases, stop the further development of secondary sex characteristics. (susans.org)

They reduce androgen levels more quickly and have fewer side effects. (medlineplus.gov)
Androgens have effects all over the body. (medlineplus.gov)

They are often used when medicines to lower androgen levels are no longer working as well. (medlineplus.gov)

This means that cancer only needs low levels of androgen to grow. (medlineplus.gov)

An anti-androgen will also result in reduced activity or function of the accessory male sex organs , and hyposexuality (diminished sexual desire or libido). (susans.org)

Through modification via aromatase enzymes (more on this later), androgens are converted to estrogen, which is an essential healthy step for glucose control, cardiovascular health, immunity, bone health, fertility, sexual health, and neural function in males and females. (atplab.com)

LH-RH antagonists are used in men with advanced cancer. (medlineplus.gov)

Androgens can be produced in other areas of the body, such as the adrenal glands. (medlineplus.gov)

18. Enzalutamide: targeting the androgen signalling pathway in metastatic castration-resistant prostate cancer. (nih.gov)

October 24, 2008 - In a phase 1/2 study of a novel androgen-receptor antagonist in advanced prostate cancer patients who have failed standard hormonal therapies and have very poor prognoses, 42% of patients have remained on treatment 24 weeks or more. (medscape.com)
11. Investigational therapies targeting the androgen signaling axis and the androgen receptor and in prostate cancer - recent developments and future directions. (nih.gov)
16. Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies. (nih.gov)

Among the other agents is CB7630 from Cougar Biotechnology, which shuts off the adrenal gland and stimulates the production of androgen, and thus cancer-cell proliferation, in prostate cancer. (medscape.com)
For patients with advanced/metastatic prostate cancer, hormones are used to block the production of androgen. (medscape.com)
Liver Disease in Men Undergoing Androgen Deprivation Therapy for Prostate Cancer. (nih.gov)
1. New approaches to targeting the androgen receptor pathway in prostate cancer. (nih.gov)
2. Moving Towards Precision Urologic Oncology: Targeting Enzalutamide-resistant Prostate Cancer and Mutated Forms of the Androgen Receptor Using the Novel Inhibitor Darolutamide (ODM-201). (nih.gov)
3. A New Old Target: Androgen Receptor Signaling and Advanced Prostate Cancer. (nih.gov)
4. Targeting the androgen receptor signaling pathway in advanced prostate cancer. (nih.gov)
5. Androgen receptor antagonists for prostate cancer therapy. (nih.gov)
6. Novel drugs targeting the androgen receptor pathway in prostate cancer. (nih.gov)
7. Second-Generation Androgen Receptor Antagonists as Hormonal Therapeutics for Three Forms of Prostate Cancer. (nih.gov)
8. Androgen receptor variant-driven prostate cancer: clinical implications and therapeutic targeting. (nih.gov)
9. Orally Bioavailable Androgen Receptor Degrader, Potential Next-Generation Therapeutic for Enzalutamide-Resistant Prostate Cancer. (nih.gov)
10. Androgen receptor-dependent and -independent mechanisms driving prostate cancer progression: Opportunities for therapeutic targeting from multiple angles. (nih.gov)
13. Interference with the androgen receptor protein stability in therapy-resistant prostate cancer. (nih.gov)
14. An Overview of Next-Generation Androgen Receptor-Targeted Therapeutics in Development for the Treatment of Prostate Cancer. (nih.gov)
17. Targeting the androgen receptor and overcoming resistance in prostate cancer. (nih.gov)
20. Recent progress in the development of protein-protein interaction inhibitors targeting androgen receptor-coactivator binding in prostate cancer. (nih.gov)
Androgens cause prostate cancer cells to grow. (medlineplus.gov)
Hormone therapy for prostate cancer lowers the effect level of androgens in the body. (medlineplus.gov)
Some drugs that work by blocking the effect of androgen on prostate cancer cells. (medlineplus.gov)
Some prostate cancer cells can also make androgens. (medlineplus.gov)

These experimental findings suggest that atrazine-induced gonadal malformations result from the depletion of androgens and production of estrogens, perhaps subsequent to the induction of aromatase by atrazine, a mechanism established in fish, amphibians, reptiles, and mammals (rodents and humans). (nih.gov)

Clascoterone cream targets androgen receptors in the skin to reduce cutaneous 5-alpha dihydrotestosterone. (medscape.com)
Antiandrogens bind to androgen receptors and competitively inhibit their interaction with testosterone and dihydrotestosterone. (medscape.com)

Patients may not have had therapy modulating testosterone levels (such as luteinizing-hormone, releasing-hormone agonists/antagonists and antiandrogens) within 6 months prior to randomization. (nih.gov)
They are called luteinizing hormone-releasing hormone (LH-RH) analogs (injections) and anti-androgens (oral tablets). (medlineplus.gov)

MDV3100 is a once-a-day oral therapy and is a novel small-molecule androgen-receptor antagonist that inhibits androgen-receptor function. (medscape.com)

A first-in-class topical selective androgen receptor inhibitor, clascoterone 1% topical cream, was approved by the FDA in August 2020. (medscape.com)

Androgens can be produced in other areas of the body, such as the adrenal glands. (medlineplus.gov)

Androgens are male sex hormones. (medlineplus.gov)

They reduce androgen levels more quickly and have fewer side effects. (medlineplus.gov)
Androgens have effects all over the body. (medlineplus.gov)
Vinclozolin (Vin CAS 50471-44-8), a dicarboximide fungicide, has been reported be an antagonist of androgen receptor binding in rats, effects that could result in decreased fertility, defects in reproductive organs or cancer. (cdc.gov)

It depletes androgens in adult frogs and reduces androgen-dependent growth of the larynx in developing male larvae. (nih.gov)

The most common treatment is to take drugs that lower the amount of androgens made by the testicles. (medlineplus.gov)
Three drugs help to stop the body from making androgens from tissue other than the testicles. (medlineplus.gov)

LH-RH antagonists are another class of treatments, including degarelix (Firmagon) and relugolix (Orgovyx). (medlineplus.gov)

Performance data from applying the ToxCast/Tox 21 androgen receptor model, based on 11 high throughput assays, to 39 reference chemicals. (nih.gov)

Anatomy4

Organisms2

Diseases3

Chemicals and Drugs59

Analytical, Diagnostic and Therapeutic Techniques and Equipment2

Phenomena and Processes4

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

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

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)

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

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)

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

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

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

Androgen Antagonists

Androgens

Flutamide

Receptors, Androgen

Tosyl Compounds

Cyproterone Acetate

Dihydrotestosterone

Anilides

Prostatic Neoplasms

Androgen Receptor Antagonists

Testosterone

Testosterone Congeners

Metribolone

Hormone Antagonists

Androgen-Insensitivity Syndrome

Dopamine Antagonists

Excitatory Amino Acid Antagonists

Neurokinin-1 Receptor Antagonists

Narcotic Antagonists

Histamine H2 Antagonists

Dose-Response Relationship, Drug

Prostate

Interleukin 1 Receptor Antagonist Protein

Rats, Sprague-Dawley

Muscarinic Antagonists

GABA Antagonists

Histamine H1 Antagonists

Piperidines

Purinergic P1 Receptor Antagonists

Androstenedione

Histamine Antagonists

Nicotinic Antagonists

Neoplasms, Hormone-Dependent

Adenosine A2 Receptor Antagonists

Adrenergic alpha-1 Receptor Antagonists

Purinergic P2 Receptor Antagonists

Nandrolone

Androstane-3,17-diol

Dehydroepiandrosterone

Serotonin 5-HT3 Receptor Antagonists

Serotonin 5-HT2 Receptor Antagonists

3-Oxo-5-alpha-Steroid 4-Dehydrogenase

Rats, Wistar

Cell Line, Tumor

Adenosine A1 Receptor Antagonists

Leukotriene Antagonists

Angiotensin Receptor Antagonists

Estradiol

Signal Transduction

RNA, Messenger

Binding, Competitive

Adrenergic alpha-2 Receptor Antagonists

Gonadotropin-Releasing Hormone

Adrenergic Antagonists

GABA-A Receptor Antagonists

Nitriles

Testis

Adrenergic alpha-Antagonists

Cells, Cultured

Estrogen Antagonists

Radioligand Assay

Histamine H3 Antagonists

Ligands

Steroid 17-alpha-Hydroxylase

Dehydroepiandrosterone Sulfate

Aromatase

Time Factors

Receptors, Serotonin

Estrogens

Receptors, Endothelin

Cholestenone 5 alpha-Reductase

Adrenergic beta-2 Receptor Antagonists

Receptors, N-Methyl-D-Aspartate

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

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

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)

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

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)

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

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