Aromatase Inhibitors: Compounds that inhibit AROMATASE in order to reduce production of estrogenic steroid hormones.TriazolesNitriles: Organic compounds containing the -CN radical. The concept is distinguished from CYANIDES, which denotes inorganic salts of HYDROGEN CYANIDE.Fadrozole: A selective aromatase inhibitor effective in the treatment of estrogen-dependent disease including breast cancer.Aromatase: 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.Androstatrienes: Derivatives of the steroid androstane having three double bonds at any site in any of the rings.Antineoplastic Agents, Hormonal: Antineoplastic agents that are used to treat hormone-sensitive tumors. Hormone-sensitive tumors may be hormone-dependent, hormone-responsive, or both. A hormone-dependent tumor regresses on removal of the hormonal stimulus, by surgery or pharmacological block. Hormone-responsive tumors may regress when pharmacologic amounts of hormones are administered regardless of whether previous signs of hormone sensitivity were observed. The major hormone-responsive cancers include carcinomas of the breast, prostate, and endometrium; lymphomas; and certain leukemias. (From AMA Drug Evaluations Annual 1994, p2079)Tamoxifen: One of the SELECTIVE ESTROGEN RECEPTOR MODULATORS with tissue-specific activities. Tamoxifen acts as an anti-estrogen (inhibiting agent) in the mammary tissue, but as an estrogen (stimulating agent) in cholesterol metabolism, bone density, and cell proliferation in the ENDOMETRIUM.Breast Neoplasms: Tumors or cancer of the human BREAST.Androstenedione: 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.Aminoglutethimide: An aromatase inhibitor that is used in the treatment of advanced BREAST CANCER.Postmenopause: The physiological period following the MENOPAUSE, the permanent cessation of the menstrual life.Neoplasms, Hormone-Dependent: 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.Estrogens: 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.Estrogen Antagonists: Compounds which inhibit or antagonize the action or biosynthesis of estrogenic compounds.Androstadienes: Derivatives of the steroid androstane having two double bonds at any site in any of the rings.Estradiol: 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.Receptors, Estrogen: Cytoplasmic proteins that bind estrogens and migrate to the nucleus where they regulate DNA transcription. Evaluation of the state of estrogen receptors in breast cancer patients has become clinically important.Estrogen Receptor Modulators: Substances that possess antiestrogenic actions but can also produce estrogenic effects as well. They act as complete or partial agonist or as antagonist. They can be either steroidal or nonsteroidal in structure.Testolactone: An antineoplastic agent that is a derivative of progesterone and used to treat advanced breast cancer.Chemotherapy, Adjuvant: Drug therapy given to augment or stimulate some other form of treatment such as surgery or radiation therapy. Adjuvant chemotherapy is commonly used in the therapy of cancer and can be administered before or after the primary treatment.Selective Estrogen Receptor Modulators: A structurally diverse group of compounds distinguished from ESTROGENS by their ability to bind and activate ESTROGEN RECEPTORS but act as either an agonist or antagonist depending on the tissue type and hormonal milieu. They are classified as either first generation because they demonstrate estrogen agonist properties in the ENDOMETRIUM or second generation based on their patterns of tissue specificity. (Horm Res 1997;48:155-63)Testosterone: 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.Estrone: An aromatized C18 steroid with a 3-hydroxyl group and a 17-ketone, a major mammalian estrogen. It is converted from ANDROSTENEDIONE directly, or from TESTOSTERONE via ESTRADIOL. In humans, it is produced primarily by the cyclic ovaries, PLACENTA, and the ADIPOSE TISSUE of men and postmenopausal women.Gynecomastia: Enlargement of the BREAST in the males, caused by an excess of ESTROGENS. Physiological gynecomastia is normally observed in NEWBORNS; ADOLESCENT; and AGING males.Enzyme Inhibitors: Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.Antineoplastic Agents: Substances that inhibit or prevent the proliferation of NEOPLASMS.Receptors, Progesterone: Specific proteins found in or on cells of progesterone target tissues that specifically combine with progesterone. The cytosol progesterone-receptor complex then associates with the nucleic acids to initiate protein synthesis. There are two kinds of progesterone receptors, A and B. Both are induced by estrogen and have short half-lives.Megestrol Acetate: Megestrol acetate is a progestogen with actions and uses similar to those of the progestogens in general. It also has anti-androgenic properties. It is given by mouth in the palliative treatment or as an adjunct to other therapy in endometrial carcinoma and in breast cancer. Megestrol acetate has been approved to treat anorexia and cachexia. (From Reynolds JEF(Ed): Martindale: The Extra Pharmacopoeia (electronic version). Micromedex, Inc, Englewood, CO, 1995)Estrogen Receptor alpha: One of the ESTROGEN RECEPTORS that has marked affinity for ESTRADIOL. Its expression and function differs from, and in some ways opposes, ESTROGEN RECEPTOR BETA.Ovary: The reproductive organ (GONADS) in female animals. In vertebrates, the ovary contains two functional parts: the OVARIAN FOLLICLE for the production of female germ cells (OOGENESIS); and the endocrine cells (GRANULOSA CELLS; THECA CELLS; and LUTEAL CELLS) for the production of ESTROGENS and PROGESTERONE.Clinical Trials as Topic: Works about pre-planned studies of the safety, efficacy, or optimum dosage schedule (if appropriate) of one or more diagnostic, therapeutic, or prophylactic drugs, devices, or techniques selected according to predetermined criteria of eligibility and observed for predefined evidence of favorable and unfavorable effects. This concept includes clinical trials conducted both in the U.S. and in other countries.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.Pargyline: A monoamine oxidase inhibitor with antihypertensive properties.Drug Resistance, Neoplasm: Resistance or diminished response of a neoplasm to an antineoplastic agent in humans, animals, or cell or tissue cultures.Puberty, Precocious: Development of SEXUAL MATURATION in boys and girls at a chronological age that is 2.5 standard deviations below the mean age at onset of PUBERTY in the population. This early maturation of the hypothalamic-pituitary-gonadal axis results in sexual precocity, elevated serum levels of GONADOTROPINS and GONADAL STEROID HORMONES such as ESTRADIOL and TESTOSTERONE.Papio anubis: A species of baboon in the family CERCOPITHECIDAE with a somewhat different social structure than PAPIO HAMADRYAS. They inhabit several areas in Africa south of the Sahara.Hot Flashes: A sudden, temporary sensation of heat predominantly experienced by some women during MENOPAUSE. (Random House Unabridged Dictionary, 2d ed)Arthralgia: Pain in the joint.Dihydrotestosterone: A potent androgenic metabolite of TESTOSTERONE. It is produced by the action of the enzyme 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE.Endometriosis: A condition in which functional endometrial tissue is present outside the UTERUS. It is often confined to the PELVIS involving the OVARY, the ligaments, cul-de-sac, and the uterovesical peritoneum.Musculoskeletal Pain: Discomfort stemming from muscles, LIGAMENTS, tendons, and bones.Sex Differentiation: The process in developing sex- or gender-specific tissue, organ, or function after SEX DETERMINATION PROCESSES have set the sex of the GONADS. Major areas of sex differentiation occur in the reproductive tract (GENITALIA) and the brain.Follicle Stimulating Hormone: A major gonadotropin secreted by the adenohypophysis (PITUITARY GLAND, ANTERIOR). Follicle-stimulating hormone stimulates GAMETOGENESIS and the supporting cells such as the ovarian GRANULOSA CELLS, the testicular SERTOLI CELLS, and LEYDIG CELLS. FSH consists of two noncovalently linked subunits, alpha and beta. Within a species, the alpha subunit is common in the three pituitary glycoprotein hormones (TSH, LH, and FSH), but the beta subunit is unique and confers its biological specificity.Ovariectomy: The surgical removal of one or both ovaries.Clomiphene: A triphenyl ethylene stilbene derivative which is an estrogen agonist or antagonist depending on the target tissue. Note that ENCLOMIPHENE and ZUCLOMIPHENE are the (E) and (Z) isomers of Clomiphene respectively.Bone Density Conservation Agents: Agents that inhibit BONE RESORPTION and/or favor BONE MINERALIZATION and BONE REGENERATION. They are used to heal BONE FRACTURES and to treat METABOLIC BONE DISEASES such as OSTEOPOROSIS.Treatment Outcome: Evaluation undertaken to assess the results or consequences of management and procedures used in combating disease in order to determine the efficacy, effectiveness, safety, and practicability of these interventions in individual cases or series.Neoadjuvant Therapy: Preliminary cancer therapy (chemotherapy, radiation therapy, hormone/endocrine therapy, immunotherapy, hyperthermia, etc.) that precedes a necessary second modality of treatment.Gonads: The gamete-producing glands, OVARY or TESTIS.Estrogen Receptor beta: One of the ESTROGEN RECEPTORS that has greater affinity for ISOFLAVONES than ESTROGEN RECEPTOR ALPHA does. There is great sequence homology with ER alpha in the DNA-binding domain but not in the ligand binding and hinge domains.Gonadotropins: Hormones that stimulate gonadal functions such as GAMETOGENESIS and sex steroid hormone production in the OVARY and the TESTIS. Major gonadotropins are glycoproteins produced primarily by the adenohypophysis (GONADOTROPINS, PITUITARY) and the placenta (CHORIONIC GONADOTROPIN). In some species, pituitary PROLACTIN and PLACENTAL LACTOGEN exert some luteotropic activities.Luteinizing Hormone: A major gonadotropin secreted by the adenohypophysis (PITUITARY GLAND, ANTERIOR). Luteinizing hormone regulates steroid production by the interstitial cells of the TESTIS and the OVARY. The preovulatory LUTEINIZING HORMONE surge in females induces OVULATION, and subsequent LUTEINIZATION of the follicle. LUTEINIZING HORMONE consists of two noncovalently linked subunits, alpha and beta. Within a species, the alpha subunit is common in the three pituitary glycoprotein hormones (TSH, LH and FSH), but the beta subunit is unique and confers its biological specificity.Receptor, erbB-2: A cell surface protein-tyrosine kinase receptor that is overexpressed in a variety of ADENOCARCINOMAS. It has extensive homology to and heterodimerizes with the EGF RECEPTOR, the ERBB-3 RECEPTOR, and the ERBB-4 RECEPTOR. Activation of the erbB-2 receptor occurs through heterodimer formation with a ligand-bound erbB receptor family member.Randomized Controlled Trials as Topic: Works about clinical trials that involve at least one test treatment and one control treatment, concurrent enrollment and follow-up of the test- and control-treated groups, and in which the treatments to be administered are selected by a random process, such as the use of a random-numbers table.Mammary Neoplasms, Experimental: Experimentally induced mammary neoplasms in animals to provide a model for studying human BREAST NEOPLASMS.Ovulation Induction: Techniques for the artifical induction of ovulation, the rupture of the follicle and release of the ovum.Placenta: A highly vascularized mammalian fetal-maternal organ and major site of transport of oxygen, nutrients, and fetal waste products. It includes a fetal portion (CHORIONIC VILLI) derived from TROPHOBLASTS and a maternal portion (DECIDUA) derived from the uterine ENDOMETRIUM. The placenta produces an array of steroid, protein and peptide hormones (PLACENTAL HORMONES).Puberty, Delayed: The lack of development of SEXUAL MATURATION in boys and girls at a chronological age that is 2.5 standard deviations above the mean age at onset of PUBERTY in a population. Delayed puberty can be classified by defects in the hypothalamic LHRH pulse generator, the PITUITARY GLAND, or the GONADS. These patients will undergo spontaneous but delayed puberty whereas patients with SEXUAL INFANTILISM will not.Fibrous Dysplasia, Polyostotic: FIBROUS DYSPLASIA OF BONE affecting several bones. When melanotic pigmentation (CAFE-AU-LAIT SPOTS) and multiple endocrine hyperfunction are additionally associated it is referred to as Albright syndrome.Uterine Diseases: Pathological processes involving any part of the UTERUS.Steroids: A group of polycyclic compounds closely related biochemically to TERPENES. They include cholesterol, numerous hormones, precursors of certain vitamins, bile acids, alcohols (STEROLS), and certain natural drugs and poisons. Steroids have a common nucleus, a fused, reduced 17-carbon atom ring system, cyclopentanoperhydrophenanthrene. Most steroids also have two methyl groups and an aliphatic side-chain attached to the nucleus. (From Hawley's Condensed Chemical Dictionary, 11th ed)Diphosphonates: Organic compounds which contain P-C-P bonds, where P stands for phosphonates or phosphonic acids. These compounds affect calcium metabolism. They inhibit ectopic calcification and slow down bone resorption and bone turnover. Technetium complexes of diphosphonates have been used successfully as bone scanning agents.Double-Blind Method: A method of studying a drug or procedure in which both the subjects and investigators are kept unaware of who is actually getting which specific treatment.Drug Administration Schedule: Time schedule for administration of a drug in order to achieve optimum effectiveness and convenience.Bone Density: The amount of mineral per square centimeter of BONE. This is the definition used in clinical practice. Actual bone density would be expressed in grams per milliliter. It is most frequently measured by X-RAY ABSORPTIOMETRY or TOMOGRAPHY, X RAY COMPUTED. Bone density is an important predictor for OSTEOPOROSIS.Cyprinidae: A family of freshwater fish comprising the minnows or CARPS.

The aromatase inactivator 4-hydroxyandrostenedione (4-OH-A) inhibits tamoxifen metabolism by rat hepatic cytochrome P-450 3A: potential for drug-drug interaction of tamoxifen and 4-OH-A in combined anti-breast cancer therapy. (1/981)

Tamoxifen (tam), an anti-breast cancer agent, is metabolized into tam-N-oxide by the hepatic flavin-containing monooxygenase and into N-desmethyl- and 4-hydroxy-tam by cytochrome P-450s (CYPs). Additionally, tam is metabolically activated by hepatic CYP3A, forming a reactive intermediate that binds covalently to proteins. Tam and 4-hydroxyandrostenedione (4-OH-A) are currently used to treat breast cancer, and it has been contemplated that 4-OH-A be given concurrently with tam to contravene potential tumor resistance to tam. Because alterations in tam metabolism may influence its therapeutic efficacy, the effect of 4-OH-A on tam metabolism was examined. Incubation of tam with liver microsomes from phenobarbital-treated rats, in the presence of 4-OH-A (10-100 microM), resulted in marked inhibition of tam-N-demethylation and tam covalent binding and in decreased tam-N-oxide accumulation; however, there was no inhibition of the formation of 4-hydroxy-tam and of 3,4-dihydroxytamoxifen. These findings indicate that 4-OH-A inhibits CYP3A, but not P-450(s) that catalyze tam 4-hydroxylation. The diminished tam-N-oxide accumulation could be due to decreased N-oxide formation and/or due to increased N-oxide reduction. Incubation of tam-N-oxide with liver microsomes containing heat-inactivated flavin-containing monooxygenase demonstrated that 4-OH-A increases the accumulation of tam, possibly by diminishing its P-450-mediated metabolism. Kinetic studies indicate that 4-OH-A is a competitive inhibitor of CYP3A, but not a time-dependent inactivator. Consequently, the concurrent treatment of tam and 4-OH-A may result in increased tam half-life and thus could potentiate the therapeutic efficacy of tam and diminish the potential side effects of tam by inhibiting its covalent binding to proteins and possibly to DNA.  (+info)

Inhibitory effects of nitric oxide on the expression and activity of aromatase in human granulosa cells. (2/981)

The aim of the present study was to explore the mechanisms by which nitric oxide (NO) may inhibit aromatase activity of human granulosa cells. Ovarian granulosa-luteal cells, obtained from patients undergoing in-vitro fertilization (IVF) were cultured in the presence of NO-related substances. After 24 h of culture, aromatase activity of the cells was significantly inhibited by treatment with the NO donors, SNAP or NOC12 at > or =10(-4) M in a dose-dependent manner. Treatment with NO catabolites or a peroxynitrite-releasing compound, SIN1, had no significant influence. Treatment with SNAP at 10(-3) M decreased relative aromatase mRNA values by 72% (P<0.05) and intracellular cyclic AMP concentrations by 53% (P<0.01). However, treatment with H89, an inhibitor of protein kinase A, did not inhibit aromatase activity. Since there were no significant effects of NO catabolites or peroxinitrite, the inhibitory action of NO donors on aromatase must be related to NO release. The action of NO is, in part, attributable to the down-regulation of aromatase gene transcription. Although NO decreased intracellular cAMP values, down-regulation of aromatase gene transcription may not be mediated by protein kinase A-dependent mechanisms.  (+info)

Evidence of sex reversal in the gonads of chicken embryos after oestrogen treatment as detected by expression of lutropin receptor. (3/981)

In chicken embryos, there is a difference between the sexes in the onset of lutropin receptor mRNA expression in the gonads. The effects of oestrogen on lutropin receptor expression were studied to investigate the mechanism controlling this difference. Lutropin receptor mRNA expression was detected in the ovaries of sesame oil-treated control female embryos on day 12 of incubation, while no expression was found in the testes of the male controls. Oestradiol administration to genetically male embryos before sexual differentiation resulted in gonadal sex reversal which was characterized histologically by the proliferation of cortical cords and the presence of lacunae. Lutropin receptor expression was detected in the feminizing testis on day 12 of incubation. Administration of aromatase inhibitor (CGS 16949 A) to genetically female embryos before sexual differentiation inhibited the formation of cortical cords, although a relatively weak expression of lutropin receptor was detected. These results indicate that early expression of the lutropin receptor is regulated by oestrogen.  (+info)

Presence of an aromatase inhibitor, possibly heat shock protein 90, in dominant follicles of cattle. (4/981)

In cattle, it has been suggested that follicular fluid has direct modulatory effects on follicular growth and maturation. In the first part of this study, an in vitro test using aromatase activity of follicular wall fragments as an end point was validated for cattle follicles and was used to test whether follicular fluid (from dominant or non-dominant follicles) modulates aromatase activity. Fluid from dominant follicles at a concentration of 24 or 12% (obtained during the luteal and follicular phases, respectively) significantly inhibited aromatase activity. Inhibitory activity was low or absent in fluid from non-dominant follicles. FSH-stimulated aromatase activity was also reduced by fluid from dominant follicles, but not to a greater extent than in basal conditions. Finally, charcoal-treated fluid from dominant follicles retained its inhibitory activity. In contrast, ovarian venous serum draining a dominant follicle had no activity at the three concentrations tested (6, 12 and 24%). In the second part of the study, identification of the compounds involved in this modulatory activity was attempted using SDS-PAGE. Comparison of the fluorographs from de novo synthesized proteins stored in follicular fluid (inhibitory medium) with those secreted in incubation medium (inactive medium) demonstrated that one protein (90 kDa, pI 5.8) was significantly (P < 0.05) more abundant in fluid from dominant follicles (2.0 +/- 0.09%) than in the culture medium (1.3 +/- 0.1% of the total proteins). This protein had characteristics similar to those of heat shock protein 90 (hsp 90). Therefore, in the final part of the study, the presence of hsp 90 in ovarian cells and follicular fluid was investigated using immunohistochemistry and western blot analysis. After immunohistochemistry, a positive signal was detected mainly in the granulosa cells of larger follicles and to a smaller extent in thecal cells and oocytes. Western blot analysis also demonstrated the presence of hsp 90 in follicular wall fragments and fluid. When blotting was achieved on a sample of follicular fluid resolved by two-dimensional PAGE, the spot detected had a similar location to that at 90 kDa and pI 5.8. Addition of purified hsp 90 to bovine follicles in vitro depressed aromatase activity by altering the K(m) value (and possibly the Vmax value) of the enzyme. It is proposed that hsp 90 is a functional regulator of follicular maturation through its action on aromatase.  (+info)

The third-generation non-steroidal aromatase inhibitors: a review of their clinical benefits in the second-line hormonal treatment of advanced breast cancer. (5/981)

Three new aromatase inhibitors have recently completed phase III evaluation as treatment of metastatic breast cancer in post-menopausal women whose disease has progressed despite tamoxifen therapy: anastrozole (ARIMIDEX, Zeneca), letrozole (FEMARA, Novartis) and vorozole (RIVIZOR, Janssen). All belong to the third generation of non-steroidal aromatase inhibitors, and each is superior to previous generations in terms of potency and selectivity. The trials that have been performed compare each agent to megestrol acetate, and letrozole and vorozole to aminoglutethimide. Although the studies are not directly comparable due to differing study designs and patient populations, it has been demonstrated each of these drugs provides single agent, once-daily, oral palliation of hormone-responsive, post-menopausal metastatic breast cancer. Letrozole is clearly more effective than megestrol acetate, and anastrozole and vorozole are possibly so. All three are better tolerated than the progestin, particularly in terms of weight gain. Both letrozole and vorozole are significantly more effective, and better tolerated than aminoglutethimide. Overall, this most recent generation of aromatase inhibitors is a clear improvement on our current standard second-line therapies. In 1999, tamoxifen remains the first choice in the hormonal therapy of breast cancer. Following tamoxifen failure, the optimal second-line hormonal therapy remains undefined, but aminoglutethimide and megestrol acetate are no longer optimal therapy in this setting. The third-generation non-steroidal aromatase inhibitors must now be compared to each other, to the steroidal aromatase inhibitors, to the pure anti-oestrogens, and to tamoxifen.  (+info)

Estrogen-inducible, sex-specific expression of brain-derived neurotrophic factor mRNA in a forebrain song control nucleus of the juvenile zebra finch. (6/981)

The expression of brain-derived neurotrophic factor (BDNF) mRNA is increased significantly within the high vocal center (HVc) of male but not female zebra finches from posthatching day 30-35 on. The population of HVc cells expressing BDNF mRNA included 35% of the neurons projecting to the nucleus robustus of the archistriatum (RA). In the RA and in RA-projecting neurons of the lateral portion of the magnocellular nucleus of the anterior neostriatum, BDNF mRNA was expressed at very low levels in both sexes. The BDNF-receptor trkB mRNA was expressed in the RA, in RA-projecting neurons of lateral portion of the magnocellular nucleus of the anterior neostriatum, and in the HVc, except in most of its RA-projecting neurons. Premature stimulation and an inhibitory effect on the normal increase of the BDNF mRNA expression in juvenile males occurred after treatments with 17beta-estradiol and the aromatase inhibitor fadrozole, respectively. The up-regulation of the BDNF expression in the HVc could be a mechanism by which estrogen triggers the differentiation of cells within and connected to the HVc of male zebra finches.  (+info)

Mitogenic and antioxidant mechanisms of estradiol action in preovulatory ovine follicles: relevance to luteal function. (7/981)

The objectives of this investigation were to determine the intrafollicular mechanisms and physiological consequences of estradiol actions in preovulatory ovine follicles. Acute suppression of estradiol production in proestrous ewes by an aromatase inhibitor (Arimidex) was associated with follicular lipid peroxidation, testosterone accumulation, and a granulosa cell deficiency (decreased proliferation/increased apoptosis). Estradiol-17beta stimulated granulosa proliferating cell nuclear antigen (PCNA) and protected cells from oxidative (H(2)O(2)) stress-induced apoptosis in vitro; the PCNA, but not the antiapoptotic response, was negated by the transcriptional inhibitor actinomycin D. Thus, it appears that genomic/mitotic and cytoprotective (oxygen-scavenging) modes of estradiol action operate in preovulatory follicles. Luteal (large steroidogenic cell) function was diminished following ovulation induction of estradiol-deficient follicles. It is suggested that inadequate exposure of the preovulatory follicle to estradiol caused the granulosa lutein insufficiency.  (+info)

Gonadal stage-dependent effects of gonadal steroids on gonadotropin II secretion in the Atlantic croaker (Micropogonias undulatus). (8/981)

Involvement of gonadal steroids in the control of gonadotropin II (GTH II) (homologous to LH) secretion was investigated in the Atlantic croaker (Micropogonias undulatus) using gonadectomy (Gx) and steroid replacement paradigms. Gonadectomy in males and females during the late gonadal recrudescence phase elicited significant increases in the gonadotropin response to stimulation by an LHRH analog (LHRHa), without altering basal GTH II secretion. Slow-release silicone elastomer implants of testosterone or estradiol significantly inhibited LHRHa-induced GTH II secretion in gonad-intact and Gx males, and in Gx females, whereas 5alpha-dihydrotestosterone, a nonaromatizable androgen, was ineffective. Pretreatment of fish with an aromatase inhibitor, 1,4, 6-androstatrien-3,17-dione, 2 days before the administration of testosterone implants, completely blocked the negative effect of testosterone on LHRHa-induced GTH II secretion in males, but only partially restored it in females. This suggests that the negative feedback of testosterone in males is primarily mediated by its conversion to estradiol at the level of the hypothalamus and/or pituitary gland, while in females the androgen may also exert a direct inhibitory effect on GTH II secretion, probably mediated via an androgen receptor. In addition, estradiol and testosterone exerted positive effects on basal and LHRHa-induced GTH II secretion during the early-recrudescence phase of the gonadal cycle. The steroids switched to a negative effect on LHRHa-induced GTH II secretion once the fish had fully developed gonads, possibly as a mechanism that prevents a precocious surge in GTH II secretion and final gamete maturation until gametogenesis is complete and the environmental conditions are appropriate for spawning.  (+info)

RATIONALE: Estrogen can cause the growth of breast cancer cells. Hormone therapy using letrozole may fight breast cancer by lowering the amount of estrogen the body makes. It is not yet known whether letrozole is more effective than a placebo in treating in women with breast cancer who have already received 5 years of aromatase inhibitor therapy.. PURPOSE: This randomized phase III trial is studying letrozole to see how well it works compared with a placebo in treating women with primary breast cancer who have received 5 years of aromatase inhibitor therapy. ...
Objective: To analyze the implementation of a switching policy of adjuvant aromatase inhibitor (AI) therapy sequentially after tamoxifen in consecutively treated stage I (T1N0M0) hormone receptor (HR)-positive breast cancer (BC) patients. Methods: The records of 279 consecutive HR-positive BC patients diagnosed between 2002 and 2006 and followed at the Soroka Medical Center were reviewed. Results: Two-hundred-seventeen patients who initially received tamoxifen were suitable for switching and 28 received an AI as initial adjuvant treatment. The switch was accomplished in 82.5% of the 217 patients. Those who switched to an AI had a higher proportion of T1c stage than patients eligible who were not switched, but did not differ in age, histologic grade, or having received chemotherapy. Of the 179 patients who switched, 155 (86.6%) completed at least 4.5-5 years of adjuvant tamoxifen/AI therapy. Eighteen patients discontinued AI therapy prematurely because of toxicity. Conclusions: In this stage I BC ...
Impact of Chemotherapy Followed by Aromatase Inhibitors on Bone Health of Women With ER-positive Early Breast Cancer (POCHARBI ...
Methods Female patients referred for BMD estimation in a scanner in the North West of England between 2004 and 2014 on aromatase inhibitors were identified from a dual X-ray absorptiometry database. Demographics and other risk factors, as well as fragility fractures, were recorded. Initially, those who had sustained a fracture were compared to those who had not sustained a fracture using chi-squared tests for categorical variables and T-tests for continuous variables. Following that, univariate and multivariate logistic regression models were fitted looking at the predictors of fracture. Variables included age at scan, height, weight, alcohol, smoking, family history, rheumatoid arthritis, secondary osteoporosis as defined by FRAX™, body mass index and steroid exposure, in addition to BMD in the lumbar spine and femoral neck. ...
Ligand- and Structure-Based Drug Design of Non-Steroidal Aromatase Inhibitors (NSAIs) in Breast Cancer: 10.4018/978-1-5225-0549-5.ch004: Aromatase is a multienzyme complex overexpressed in breast cancer and responsible for estrogen production. It is the potential target for designing
rant, so stay tuned.. February 2019 update: You might want to read and download, Endocrine Therapy - Managing & Making Decisions About Your Aromatase Inhibitor Medication.. Many breast cancer tumors are estrogen positive (ER-positive), progesterone positive (PR-positive), or both (ER-positive and PR-positive). Mine was both.. By the way, this information about your tumor(s) is provided in your pathology report, and you simply must have a copy of this report in your possession so you can familiarize yourself with your own unique cancers biology, even though this might sound like the last thing you want to do after your diagnosis.. Be sure to ask for a copy if you dont receive one.. If a woman is ER and/or PR positive, her oncologist might very likely prescribe an aromatase inhibitor after surgery, chemotherapy or radiation as part of her adjuvant therapy treatment plan. The intent is, of course, to prevent recurrence.. There are three kinds of aromatase inhibitors (referred to as AIs from ...
en] Treatment of castrated quail with testosterone (T) reliably activates male copulatory behavior and, at the same time, increases the aromatase activity (AA), the number of aromatase-immunoreactive (ARO-ir) cells and the concentration of aromatase mRNA as measured by RT-PCR in the brain. All these effects can be mimicked by estrogens. The behavioral effects of T can be blocked by a variety of aromatase inhibitors and, in parallel, the AA is strongly inhibited in the preoptic area (POA). We showed recently that the steroidal inhibitor, 4-OH-androstenedione (OHA) markedly decreases the immunostaining density of brain ARO-ir cells while the non-steroidal inhibitor, R76713 (racemic Vorozole; VOR) unexpectedly increased the density of this staining, despite the fact that the enzyme activity was completely inhibited. To generalize these findings and try to identify the underlying mechanism, we compared here the effects of two steroidal (OHA and androstatrienedione [ATD]) and two non-steroidal (VOR ...
One of the major drawback of aromatase inhibitors, a class of drugs, commonly used in the management of estrogen receptor-positive (ER+) breast cancer is the debilitating joint pain.
Introduction. Aromatase inhibitors (AI) have become the accepted adjuvant therapy for postmenopausal patients with breast cancer with hormonal receptor expression1. AI brought about a marked reduction in estrogen levels through inhibition of the aromatase enzyme2 whose activity is relegated to peripheral tissues during menopause3. The American Society for Clinical Oncology (ASCO) recommends using the AI for 5 years, or for 2 or 3 years, after previous therapy with tamoxifen (TMX)4, where the latter option is prescribed for pre/peri-menopausal women5.. However, reduced estrogen levels increase bone resorption and raise the risk of fracture that occurs after menopause1,6-9. Clinical guidelines for the management of bone loss associated with AI (AIBL: Aromatase Inhibitor associated Bone Loss) recommends a strict monitoring of bone mineral density (BMD) and other risk factors to assess the need for treatment with anti-resortive therapies10.. Despite existing data, most of which based on randomized ...
TY - JOUR. T1 - Adjuvant endocrine therapy in postmenopausal breast cancer. AU - Ingle, James N.. PY - 2003/1/1. Y1 - 2003/1/1. N2 - Adjuvant endocrine therapy with tamoxifen has a clearly established benefit in postmenopausal women with resected early breast cancer that expresses the estrogen receptor and/or progesterone receptor. Whereas there is a vast and long experience with tamoxifen, the major focus of clinical trials over the past 6 years has involved the study of the third-generation aromatase inhibitors. Recently published data from the Arimidex, Tamoxifen, Alone or in Combination (ATAC) trial, which involved only postmenopausal women and is the largest adjuvant trial ever conducted, has demonstrated superior efficacy for anastrozole over tamoxifen alone or in combination with anastrozole. These data have engendered a great deal of discussion as to whether they provide a sufficient basis for changing the standard of practice in terms of choice of agent. Currently, a case can be made ...
Postmenopausal women with hormone receptor-positive breast cancer who took the aromatase inhibitor anastrozole for 2 years after an initial 5 years of adjuvant endocrine therapy received an equal benefit to those who took the drug for 5 additional years. The trial results suggest that a shorter duration of treatment may provide sufficient benefits while protecting women from harmful side effects, according to data from the Austrian Breast and Colorectal Cancer Study Group (ABCSG)-16 phase III trial presented by Gnant et al at the 2017 San Antonio Breast Cancer Symposium (Abstract GS3-01).. "In early-stage hormone receptor-positive breast cancer, the risk of relapse persists despite many advances in treatment," said Michael Gnant, MD, FACS, Director and Chairman of the Department of Surgery, Comprehensive Cancer Center, at the Medical University of Vienna. "Adjuvant treatment with aromatase inhibitors has been demonstrated to improve disease-free survival of postmenopausal women with this subtype ...
Aromatase Inhibitors in Davie, FL. Synthetic/natural aromatase inhibitors are-for many-the best choice in fighting breast cancer.
Aromatase Inhibitor Drugs market research study in brief The business intelligence study for the Aromatase Inhibitor Drugs market provides an extensive synopsis of essential aspects ...
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BACKGROUND: The authors examined the published evidence on the use of aromatase inhibitors (AIs) in the adjuvant setting in postmenopausal, hormone receptor-positive patients, and they provide recommendations for clinical management in 3 different situations: newly diagnosed women, women who have already received tamoxifen for 2-3 years, and women who have completed 5-years of tamoxifen and are disease free.. METHODS: All double-blind, randomized, prospective studies were reviewed. Data sources included the MEDLINE data base, reviews, editorials, and experts.. RESULTS: The Arimidex, Tamoxifen Alone or in Combination (ATAC) trial, the Intergroup Exemestane Study (IES), and the MA-17 trial confirmed the superiority of AIs over tamoxifen in women with early-stage breast carcinoma, improving disease-free survival (DFS) considerably. In the ATAC trial, the 4-year DFS rate was 86.9% on anastrozole and 84.5% on tamoxifen (P = 0.03); in the IES, the 3-year DFS rate was 91.5% on exemestane and 86.8% on ...
Hormonal therapy reduces the risk of recurrence for women with early-stage breast cancer that is ER-and/or PR-positive. Standard therapy lasts 5 years. A new study looks at whether extending one type of hormonal therapy, known as aromatase inhibitor therapy, to 10 years lowers recurrence rates even more for these women. (7/26/16)
ESMO 2016. Recommended first-line treatments for postmenopausal women with hormone receptor-positive advanced/metastatic breast cancer include third-generation aromatase inhibitors (ie, anastrozole) or tamoxifen. Fulvestrant, is a complete estrogen receptor (ER) antagonist approved for the treatment of ER+ advanced breast cancer after aromatase inhibitors have failed. Although a previous phase 2 study was unable to show a difference in clinical benefit rate (CBR) between first-line fulvestrant and anastrozole in these patients, "the median time to progression was significantly increased in patients receiving fulvestrant, which unusually translated into increased overall survival [OS]," said Dr Matthew Ellis of Houston, TX, an author of the subsequent FALCON study.. The FALCON study was a phase 3, randomized, double-blind, multicenter trial designed to confirm the superiority of fulvestrant over anastrozole in postmenopausal women with ER+ and/or progesterone receptor-positive (PR+) advanced ...
In order to understand the nature of resistance to AIs, this review has drawn upon endocrine, molecular and pathological measurements made in clinical material taken before and after therapy with AIs and upon observations from clinical trials in which AIs have been given as treatment either alone or in combination with other targeted agents. The major message from these studies is that no single reason can account for resistance in all cases and that there are multiple and diverse mechanisms by which breast cancers may avoid the restraints of AI therapy. The consequences of this are that a battery of tests and predictive markers may be needed in order to elucidate the nature of resistance in individual tumours and that if rational treatments to avoid or reverse resistance are based on an underlying mechanism, they also will be both varied and individually targeted.. In terms of general identification of resistance, assessment of ER is essential. However, in ER-positive tumours, additional ...
Despite the fact that estrogen is essential for both quality and quantity of life, aromatase inhibitors (AIs) are regularly prescribed to most post-menopausal women with estrogen-sensitive breast cancer - even if they have low estrogen levels.
A significant amount of data has accumulated suggesting an important role for translational dysregulation in many cancer lineages, including breast cancer. It remained unclear, however, which of these alterations are the most significant determinants of cancer progression and poor patient outcomes. We sought to determine the association of translational regulators with clinical-pathologic factors and survival outcomes in hormone receptor-positive breast cancer. We found that high eEF2, S6, pS6 S240/244, p4E-BP1 T70, and low pdcd4 were significantly associated with node positivity. High p4E-BP1 T36/47, p4E-BP1 S65, p4E-BP1 T70 as well as total 4E-BP1 were associated with worse RFS. High p4E-BP1 T70 and pS6 S235/236, and low pdcd4, were associated with worse OS. In the multivariable analysis, in addition to positive nodes, high p4E-BP1 S65 remained a significant predictor of lower RFS. High pS6 S235/236, eEF2K and low pdcd4 were associated with lower OS. These results confirm that translational ...
What is hormone receptor-positive breast cancer? Our award-winning Dignity Health Central Coast doctors can answer all your questions about this type of breast cancer.
We present a single-cell application to determine PIK3CA mutations in CTCs, which uncovered the degree of intra-patient heterogeneity in patients with metastatic hormone receptor-positive breast cancer (HR+ MBC) and high CTC count (>10 CTCs/7.5mL). Using CellSearch and DEPArray we isolated circulating tumor cells (CTCs) and white blood cells (WBCs) from peripheral blood and sequenced PIK3CA exons 9 and 20 by targeted amplicon sequencing. Comparative analysis between the primary tumor (PT, n=27 patients), circulating cell-free DNA (cfDNA, n=31 patients), single (n=146 CTCs) and pools (n=70 CTC suspensions, ranging 5-120 cells/suspension) of CTCs from 26 patients and metastases/DTCs (n=11 patients) was performed. Mutations were frequent in PT (15/27 (55.5%)) and showed slight and substantial agreement with cfDNA (n=21; kappa=0.14) and CTCs (n=22; kappa=0.6733), respectively. A wild-type genotype in WBCs indicates a high specificity. Inter-compartmental concordance was observed in 13/18 (72.2%) ...
Adjuvant treatment with aromatase inhibitors improves outcomes in postmenopausal women with hormone-sensitive early breast cancer; however, they should not be used in premenopausal women. Menopausal status is the most important factor in the choice of the hormonal treatment. There is no direct correlation between amenorrhea and ovarian function, as even the patients with amenorrhea may present...
Exemestane, sold under the brand name Aromasin among others, is a medication used to treat breast cancer. It is a member of the class of antiestrogens known as aromatase inhibitors. Some breast cancers require estrogen to grow. Those cancers have estrogen receptors (ERs), and are called ER-positive. They may also be called estrogen-responsive, hormonally-responsive, or hormone-receptor-positive. Aromatase is an enzyme that synthesizes estrogen. Aromatase inhibitors block the synthesis of estrogen. This lowers the estrogen level, and slows the growth of cancers. Exemestane is indicated for the adjuvant treatment of postmenopausal women with estrogen-receptor positive early breast cancer who have received two to three years of tamoxifen and are switched to it for completion of a total of five consecutive years of adjuvant hormonal therapy. US FDA approval was in October 2005. Exemestane is also indicated for the treatment of advanced breast cancer in postmenopausal women whose disease has ...
Letrozole (Femara), an aromatase inhibitor currently used to prevent breast cancer recurrence in postmenopausal women, shows promise in the treatment
A randomized study in a similar patient population has demonstrated a small disease free-survival benefit when these patients receive an aromotase inhibitor, such as femara, after completing 5 years of tamoxifen," said Gary Freedman, M.D., a radiation oncologist at Fox Chase Cancer Center and lead author of the study. "For this study, we looked at women who were free of cancer after completing all therapy, including five years of tamoxifen, to better define which women would benefit from taking an aromatase inhibitor rather than recommending it for all women ...
Vaginal atrophy symptoms such as dryness, irritation, and itching, are common after menopause. Vaginal estrogen therapy is the most effective treatment but not appropriate for all women. Women with estrogen-responsive breast cancer treated with aromatase inhibitor (AI) treatment, suppressing estrogen levels, often suffer from more pronounced vaginal atrophy symptoms. However, vaginal estrogen treatment is not recommended, leaving them without effective treatment options. The aim of this thesis was to study the effect of long-term anti-estrogen therapy on circulating estrogen levels and biochemical factors in vaginal mucosa in relation to morphological changes and clinical signs of vaginal atrophy.. Circulating estrogen levels were analyzed by use of mass spectrometry and radioimmunoassay. Immunohistochemistry was used to study vaginal proliferation and steroid hormone receptors in vaginal mucosa. Vaginal gene expression was studied by use of microarray technology and bioinformatic tools, and ...
Recent advances in breast cancer treatment include the advent of aromatase inhibitors (AIs) in the adjuvant setting with better efficacy and toxicity profiles than tamoxifen. However, AIs generally do
San Antonio Breast Cancer Symposium, California (ots/PRNewswire) - - New Results From Two Phase II Trials Demonstrate Efficacy andTolerability for Faslodex Following...
For postmenopausal women with breast cancer, extension of treatment with an aromatase inhibitor to 10 years is associated with improved outcomes, according to a study published online in the New England Journal of Medicine.
Study says the toxicities associated with aromatase inhibitors (AIs) may explain the lack of overall survival improvement compared with tamoxifen
TY - JOUR. T1 - Vitamin D prevents bone loss tied to aromatase inhibitors. T2 - Commentary. AU - Loprinzi, Charles L.. PY - 2011/7/1. Y1 - 2011/7/1. UR - http://www.scopus.com/inward/record.url?scp=80052293596&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=80052293596&partnerID=8YFLogxK. M3 - Comment/debate. AN - SCOPUS:80052293596. JO - Oncology Report. JF - Oncology Report. SN - 1548-5323. IS - JULY-AUGUST. ER - ...
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Aromatase inhibitors, when used for up to three years in combination with growth hormone, may effectively and safely help very short adolescent boys grow taller, new research suggests. The study results will be presented Sunday, April 3, at ENDO 2016, the annual meeting of the Endocrine Society in Boston.
ditionally, the increase in average TFSF in the letrozole group The findings of the present study suggest that some men after treatment compared with the pretreatment value was with severe oligospermia (,5 Â 106/mL), low T levels (,300 31.6%, and the increase in average TFSF in the anastrazole ng/dL), a T (ng/dL) to E2 (pg/mL) ratio ,10, and normal go- group after treatment compared with the pretreatment value nadotropins concentration may have a treatable endocrinop- was 21.1%. To detect whether there is a statistically signifi- athy. Accordingly, the endocrine evaluation should perhaps cant difference between the 31.6% increase of average TFSF include an estimation of E2 and calculation of the T (ng/dL) seen in the letrozole group in comparison with the 21.1% in- to E2 (pg/mL) ratio. A ratio ,10 identifies those who might crease of average TFSF seen in the anastrazole group, having benefit from treatment with an aromatase inhibitor to im- a type I error of 0.05 and a type II error of ...
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After surgery, women diagnosed with breast cancer face the risk of the breast cancer coming back (recurrence). Recurrence can happen at any time. But the risk of recurrence is highest during the first 3 years after treatment. To lower the risk of recurrence in postmenopausal women diagnosed with hormone-receptor-positive early breast cancer, hormonal therapy usually is prescribed for 5 years after the initial treatment. Treatment that comes after surgery or another initial treatment is called adjuvant therapy.. For years, tamoxifen was the hormonal therapy of choice for women diagnosed with hormone-receptor-positive early breast cancer. But in 2005, large clinical studies showed that aromatase inhibitors worked better than tamoxifen to reduce the risk of the cancer coming back in postmenopausal women diagnosed with hormone-receptor-positive breast cancer. So aromatase inhibitors - Arimidex (chemical name: anastrozole), Aromasin (chemical name: exemestane), and Femara (chemical name: letrozole) - ...
SAN ANTONIO — Extended adjuvant endocrine therapy with letrozole improved DFS compared with placebo among postmenopausal women with hormone receptor-positive breast cancer who completed previous adjuvant therapy with an aromatase inhibitor, according to 10-year results from the randomized NRG Oncology/NSABP B-42 trial presented at San Antonio Breast Cancer Symposium.Extended letrozole also
article{35f5221a-bc65-4366-a61d-af8012cbecfa, abstract = {It was previously shown that letrozole (Femara(R)) was significantly more potent than anastrozole (Arimidex(R)) in inhibiting aromatase activity in vitro and in inhibiting total body aromatisation in patients with breast cancer. The objective of this study was to compare letrozole (2.5 mg per day) and anastrozole (1 mg per day) as endocrine therapy in postmenopausal women with advanced breast cancer previously treated with an anti-oestrogen. This randomised, multicentre and multinational open-label phase IIIb/IV study enrolled 713 patients. Treatment was for advanced breast cancer that had progressed either during anti-oestrogen therapy or within 12 months of completing that therapy. Patients had tumours that were either positive for oestrogen and/or progesterone receptors (48%) or of unknown receptor status (52%). The primary efficacy endpoint was time to progression (TTP). Secondary endpoints included objective response, duration of ...
Aromasin (Exemestane) Aromasin is a steroidal aromatase inactivator used to lower circulating estrogen. It was developed to help fight breast cancer as estrogen plays a role in the growth of cancer cells. Aromasin binds irreversibly to the aromatase enzyme. This suppresses the conversion of androgens into estrogen. Circulating estrogen can be reduced by nearly 85% in women using Aromasin. A common misconception is that aromatase inhibition is similar in men than women. However in trials
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This research has been highlighted as a practice changing update by DynaMed Plus. It concludes that Fulvestrant has superior efficacy and is a preferred treatment option for patients with hormone receptor-positive locally advanced or metastatic breast cancer who have not received previous endocrine therapy compared with a third-generation aromatase inhibitor, a standard of care for first-line trea...
ABSTRACT: Aromatase inhibitors have been used for the treatment of breast cancer, ovulation induction, endometriosis, and other estrogen-modulated conditions. For women with breast cancer, bone mineral density screening is recommended with long-term aromatase inhibitor use because of risk of osteoporosis due to estrogen deficiency. Based on long-term adverse effects and complication safety data, when compared with tamoxifen, aromatase inhibitors are associated with a reduced incidence of thrombosis, endometrial cancer, and vaginal bleeding. For women with polycystic ovary syndrome and a body ... ...
A higher prescription co-payment, especially among older women, is associated with the early discontinuation and incomplete use of adjuvant aromatase inhibitor therapy, a life-saving therapy for women with hormone-sensitive, early-stage breast cancer, research shows.
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Breast cancer patients significantly benefit by taking hormone therapy drugs called aromatase inhibitors for an additional five years, according to a major study presented at the Plenary Session of the American Society of Clinical Oncology annual meeting in Chicago and published in the New England Journal of Medicine.. Loyola University Medical Center is among the centers funded by the National Cancer Institute that enrolled patients in the trial. "This will have enormous implications for thousands of women with breast cancer," said Kathy S. Albain, MD, FACP, FASCO, principal investigator for the Loyola site. "It will change practice standards worldwide." The trial included postmenopausal women with early-stage breast cancer. Some of the women had taken anti-estrogen therapy with aromatase inhibitors for five years. Other women in the study had taken the anti-estrogen drug tamoxifen for five years, followed by five years of aromatase inhibitors. The study found that in both groups, extending the ...
By September 2005 issue of Arthritis & Rheumatism, One of the most effective new treatments for breast cancer is a hormone therapy. Aromatase inhibitors work by powerfully blocking the conversion of androgen precursors into estrogens, which lowers estradiol levels in the bloodstream and estrogen levels in peripheral tissues. Because aromatase inhibitors reduce the rates of recurrence in women with early-stage postmenopausal breast cancer, these agents are not only becoming widely used in breast cancer treatment, but also being explored for their potential to prevent the disease in women at high risk. While focusing on this therapys promise, advocates have tended to downplay one of its drawbacks. Women treated with aromatase inhibitors often experience joint pain and musculoskeletal aching--severe enough, in some cases, to make them stop the treatment ...
The model showed that women with this genotype had an outcome with tamoxifen that was similar or superior to the outcome seen with aromatase inhibitors. This finding differs from the results in unselected populations, in which aromatase inhibitors have demonstrated statistically significant improvements in disease-free survival over tamoxifen. It is possible that women who are concerned about the relative toxicity or cost of an aromatase inhibitor could consider undergoing genetic testing; if they are found to be wild type for CYP2D6, they could then pursue treatment with tamoxifen instead ...
Do not take AROMASIN® (exemestane tablets) if you are allergic to AROMASIN or to anything in it. The active ingredient is exemestane.. Let your doctor know if you are taking or applying any medication that has estrogen in it including hormone replacement therapy or birth control pills or patches, or if you are taking any other medicines including over-the counter medicines, herbal supplements, and vitamins as they can affect how well AROMASIN works.. If you become pregnant while taking AROMASIN, talk to your doctor immediately to learn about the potential risks to the baby. Taking AROMASIN during pregnancy or within 1 month of becoming pregnant can harm your unborn baby. Use effective birth control (contraceptive) during treatment with AROMASIN and for 1 month after your last dose of AROMASIN.. A serious side effect of AROMASIN is bone loss over time that may increase your risk of bone fractures and weak and brittle bones (osteoporosis). The health of your bones should be carefully monitored by ...
Resistance to endocrine therapy in breast carcinogenesis due to the redox regulation of the signal transduction system by reactive oxygen species (ROS) is the subject of this review article. Both antiestrogens and aromatase inhibitors are thought to prevent cancer through modulating the estrogen receptor function, but other mechanisms cannot be ruled out as these compounds also block metabolism and redox cycling of estrogen and are free radical scavengers. Endocrine therapeutic agents, such as, tamoxifen and other antiestrogens, and the aromatase inhibitor, exemestane, are capable of producing ROS. Aggressive breast cancer cells have high oxidative stress and chronic treatment with exemestane, fulvestrant or tamoxifen may add additional ROS stress. Breast cancer cells receiving long-term antiestrogen treatment appear to adapt to this increased persistent level of ROS. This, in turn, may lead to the disruption of reversible redox signaling that involves redox-sensitive phosphatases, protein ...
Most premenopausal women with hormone receptor-positive breast cancer assigned to adjuvant treatment with the aromatase inhibitor exemestane plus triptorelin had large reductions in estrogen levels (estradiol [E2]) during the first year of treatment, …. ...
PI3K-mTOR pathway genes are commonly mutated in estrogen receptor (ER)-positive breast cancer, and preclinical and clinical data have indicated that PI3K-mTOR pathway inhibition may enhance endocrine therapy, prompting Schmid and colleagues to perform a phase II preoperative window-of-opportunity study investigating the effects of the PI3K inhibitor pictilisib in combination with the aromatase inhibitor anastrozole on tumor cell proliferation. This study randomly assigned 75 postmenopausal women with newly diagnosed operable ER+, HER2− breast cancer to receive anastrozole alone (26 patients) or anastrozole plus pictilisib (49 patients). Treatment was given for 14 days prior to surgical resection and adjuvant therapy. At least two tumor biopsies were taken at baseline and at the end of treatment, and used for immunohistochemistry. The primary end point was inhibition of tumor cell proliferation measured by change in Ki67 staining before and after treatment. Ki67 staining decreased in all but 3 ...
Life has been full of weirdness lately. Part of the weirdness is my trying to decide if I wanted to apply for a spot in a trial cancer treatment. I admit, that when my oncologist told me that my tumor markers had doubled at the beginning of the month, I was put into a tailspin. He has put me on Tamoxifen because sometimes, when youve been on aromatase inhibitors (like aromasin and arimidex) which have failed, you can fool the cancer into accepting Tamoxifen again and then it dies off. The process, however, takes two months to see if it works or not and it may cause cancer flare ups initially ...
2004 habilitáció Kutatási témák: 1. Aromatázgátló kezelés hatása a csontállományra onkológiai betegségekben. Effect of aromatase inhibitor on bone content in oncologic diseases. 2. Autoimmunbetegségek és a csontvesztés kapcsolata. Relationship between autoimmune diseases and bone loss. 3. Dyslipidaemia és endokrin folyamatok hatása a csontállományra. Effects of dyslipidemic and endocrine processes on the bone content ...
Modeling suggests that among patients who are wild type for CYP2D6, 5-year disease-free survival outcomes are similar to or perhaps even superior with tamoxifen than with aromatase inhibitors. Endocrine therapy tailored to CYP2D6 genotype could be considered for women who are newly diagnosed with br …
Purpose:Aromatase inhibitors (AI) can exert unfavorable effects on lipid profiles; however, previous studies have reported inconsistent results. We describe the association of single-nucleotide polymorphisms (SNP) in candidate genes with lipid profiles in women treated with adjuvant AIs. Experimental Design:We conducted a prospective observational study to test the associations between SNPs in candidate genes in estrogen signaling and AI metabolism pathways with fasting lipid profiles during the first three months of AI therapy in postmenopausal women with early breast cancer randomized to adjuvant letrozole or exemestane. We performed genetic association analysis and multivariable linear regressions using dominant, recessive, and additive models. Results:A total of 303 women had complete genetic and lipid data and were evaluable for analysis. In letrozole-treated patients, SNPs in CYP19A1, including rs4646, rs10046, rs700518, rs749292, rs2289106, rs3759811, and rs4775936 were significantly ...
Ran-Anastrozole: Anastrozole belongs to the group of cancer-fighting medications known as antineoplastics, and specifically to the group of antineoplastics known as nonsteroidal aromatase inhibitors. It fights breast cancer by inactivating an enzyme known as aromatase. This prevents the enzyme from supplying the estrogen that allows certain types of breast cancers to grow.
Anastrozole belongs to the group of cancer-fighting medications known as antineoplastics, and specifically to the group of antineoplastics known as nonsteroidal aromatase inhibitors. It fights breast cancer by inactivating an enzyme known as aromatase. This prevents the enzyme from supplying the estrogen that allows certain types of breast cancers to grow.
Aromasin (Exemestane) is officially classified as a steroidal Suicide Aromatase Inhibitor and carries the ability to inhibit the aromatase enzyme
TORONTO-Postmenopausal women with early-stage breast cancer who took the aromatase inhibitor letrozole (Femara) after completing 5 years of tamoxifen therapy had a 43% lower risk of recurrence than those receiving placebo, an international phase III clinical trial has found. 1
Hormone therapy is an effective approach for the treatment of breast cancer. Although the antiestrogen tamoxifen has had a major impact on the treatment of the disease, aromatase inhibitors (AIs), which reduce estrogen synthesis, have recently proved to be more effective. These agents are now used as first-line therapy for postmenopausal breast cancer. Nevertheless, despite the efficacy of these agents, resistance to treatment eventually may occur in some patients. In an effort to overcome this resistance and extend the benefits of AIs, investigators have studied the mechanisms involved in resistance to AIs. Adaptive changes that result in activation of alternate signaling pathways in AI-resistant tumors have been identified in xenograft and cell line models. Expression of estrogen receptor α and aromatase was shown to be decreased in tumors after long-term treatment with AIs. In contrast, increased expression was observed in tyrosine kinase receptors such as Her-2 and insulin-like growth ...
On July 20, 2012, the U.S. Food and Drug Administration (FDA) gave us another option for treating postmenopausal patients with metastatic, ER-positive, HER2-negative breast cancer whose disease has progressed on Arimidex or Femara by approving Afinitor (everolimus) in combination with Aromasin (exemestane). This new approval was based on the BOLERO-2 trial which was a randomized, double-blind, multicenter trial conducted in 724 postmenopausal women. Patients were randomized to receive either Afinitor 10 mg/day plus Aromasin 25 mg/day or to placebo plus Aromasin 25 mg/day. Both Aromasin and Afinitor are oral drugs.. Aromasin is an aromatase inhibitor which works by lowering estrogen levels in postmenopausal women. This trial was based on the observation that resistance (either not responding or stopping responding) to hormonal therapy is associated with a tumor being able to use pathways other than the estrogen pathway to survive and grow. One example of this is activation of the mammalian target ...
MA.17R - A Double Blind Randomization to Letrozole or Placebo for Women Previously Diagnosed with Primary Breast Cancer Completing Five Years of Adjuvant Aromatase Inhibitor Either as Initial Therapy or After Tamoxifen (Including Those in the MA.17 Study ...
rs4646 is a SNP in the CYP19A1 gene on chromosome 15. The CYP19A1 gene is probably the primary one studied to date as possibly associated with the efficacy or toxicity of aromatase inhibitors such as letrozole, anastrozole and exemestane. The effect of CYP19A1 variant in response to such inhibitors has produced conflicting results in studies (see citations below), and although rs4646 may be perhaps the best studied CYP19A1 variant, there is to date no robust or replicated conclusion about it with respect to aromatase inhibitor response.[PMID 26203310 ...
The presence of circulating ESR1 somatic mutations at disease progression in patients with HR-positive metastatic breast cancer treated with first-line AIs represent a strong and independent poor prognostic value for overall survival but no predictive value, a study presented at the 2016 ASCO Annual Meeting has found.
Purpose: PI3K/AKT/mTOR network adaptation through the upregulation of receptor tyrosine kinases signaling and subsequent re-activation of AKT is a common resistance mechanism to chemotherapies and small molecule inhibitors of mammalian target of rapamycin (mTOR). In order to block this feedback loop, MM-141, a tetravalent bispecific antibody directed at IGF-1R and ErbB3, was co-administered in combination with everolimus in various preclinical models of cancer. As everolimus is an approved therapy for women with advanced hormone receptor-positive breast cancer after failure of treatment with aromatase inhibitor, we have specifically focused on the analysis of a MM-141/everolimus combination in a hormone refractory breast cancer mouse model.. Experimental Procedures: Estrogen-supplemented mice bearing BT-474-M3 ER+/PR+ breast cancer xenografts were implanted with tamoxifen-releasing pellets. Following the development of resistance to tamoxifen, these mice were randomized into pharmacodynamics and ...
Body mass index (BMI) affects the level of estradiol and estrone sulfate suppression achieved when treating postmenopausal women with estrogen receptor (ER)-positive breast cancer with either of two aromatase inhibitors, anastrozole or letrozole.
Besides, I have learned about a new study on the use of Tamoxifen and Aromatase Inhibitors so now I have some good talking points for my Oncologist when I see him later this week and discuss the prescribed Femara (Letrozole), which is an Aromatase Inhibitor. Thanks to my pharmacist niece, Sharleen, for alerting me to this new information. It sure is nice to have nurses and pharmacists in the family ...
Tamoxifen is a pro-drug. It functions as an Estrogen Receptor Inhibitor requiring activation and conversion of the drug to the functional metabolites, 4- OH-Tamoxifen and endoxifen for clinical effect. Endoxifen is the most potent Tamoxifen (x100) metabolite. Cytochrome P450-2D6 is required for endoxifen synthesis. Common DNA polymorphisms in Cytochrome P450-2D6 can reduce enzyme activity and as a result decrease endoxifen therapeutic concentrations. These changes result in an increase in the frequency of disease recurrence and a decrease in five year survival rate.. The Tamoxifen DNA Typing System analyzes 20 gene variants found within the highly polymorphic CYP 2D6 gene which result in decreased CYP2D6 functional activity. Patients testing positive should be considered for alternative estrogen receptor (SERM) or aromatase inhibitor therapy. Presentation: ...
I had the results of my latest MRI scan yesterday. I have been on hormone therapy - aromatase inhibitor Letrozole - since the end of June. The news is encouraging. The tumour on the right hand side of my pelvis has shrunk so that it is not visible. The tumour on the left has also shrunk, but is still visible. The tumours had beeen pressing on one of my ureters and constricting it, but that has now resolved and the kidney is draining freely. So I dont now need to have a stent inserted to keep it open ...
The expression values of Her2, PR, and ER and subtype designation are correlated with the metagenes of BCAM and therefore are indirectly taken into account. They obviously provide vital information and improved understanding of breast cancer biology, which has led to effective treatments. However, our results suggest that an optimum breast cancer biomarker product does not need to include them.. Many early versions of microarray platforms, notably the popular Affymetrix U133A, do not contain probes for FGD3 and SUSD3, which may provide some explanation as to why these genes were not found earlier as highly prognostic in breast cancer. The two genes are genomically adjacent to each other and are correlated with ESR1 and PGR. The simultaneous silencing of FGD3 and SUSD3 is strongly associated (6) with poor prognosis. Furthermore, a recent study (21) identified SUSD3 as the single most predictive gene (more than ESR1) of response to aromatase inhibitor therapy. On the basis of the above facts, we ...
Can anyone explain how each of these work, the difference, and benifits or cons of each pertained to coming off a cycle trying to control estrogen production? I am getting ready to start 6-0xo when finishing my 1-test/4ad cycle. I am just wondering where this falls.....
BACKGROUND. The double blind, placebo-controlled BOLERO-2 trial demonstrated a significant doubling of progression free survival (PFS) with EVE and EXE compared to EXE alone for postmenopausal women with hormone-receptor positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) BC after recurrence/progression on non-steroidal aromatase inhibitors (NSAI) (Baselga J, et al. NEJM. 2012). The 4EVER study further evaluates the combination of EVE+EXE in a broader population to obtain greater insights and presents an extensive exploratory translational research program.. SPECIFIC AIMS/TRIAL DESIGN. 4EVER is a German multi-center, open-label, single-arm trial. 300 patients will receive EVE (10 mg/d)+EXE (25 mg/d) within clinical practice. The primary objective is to assess the overall response rate (ORR), the secondary objectives include PFS, overall survival, safety, quality of life (QoL), health utilities and health care resources. The exploratory biomarker objectives include ...
You should consider the glycemic load of any carbs and avoid higher glycemic. Stay away from gluten-free pasta, too high. Best rice is Indian basmati. Vegetable sources of starch like yams, rutabaga, winter squash are best. Here are copies of some of my posts: Please consider finding a clinic that does insulin-potentiated low-dose chemotherapy as well as a circulating tumor cells blood test with chemo sensitivity testing. Unfortunately you will need to go to a specialty clinic that will not be covered by insurance, but if you can afford it this will greatly increase your odds of beating metastatic cancer. At the very least, consider getting a biopsy done and sending the fresh tumor sample to Dr. Larry Weisenthal in California who does chemosensitivity testing and works with traditional oncologists. Its really important to get the chemotherapy that matches your tumor genetics rather than the standard chemotherapy that is first line for your disease and is the " Standard of care" for your ...
Case Reports in Hematology is a peer-reviewed, Open Access journal that publishes case reports in all areas of hematology, including general hematology, pathology, and oncology, with a specific focus on lymphomas and leukemias.
I had the pleasure of discussing AI using on cycle with Dylan Gemelli. We talked about his next video about AI on cycle. Here are my thoughts on our conversation: AI is a requirement on Cycle Testosterone, Dianabol cycle have to be ran with AIs no questions asked Anavar and Winstrol cycles dont need an AI SARMS dont require AIs
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AET, composed of hormone-blocking drugs such as tamoxifen or aromatase inhibitors, is associated with a 29% reduction in the risk of death for hormone-receptor-positive breast cancer patients. The authors of a study, published recently in JAMA Oncology, approximate that 14,630 women who did not receive hormone treatment died unnecessarily between 2004 and 2013 due to recurrence of their malignancies.. Although adherence to guidelines for AET following surgery had slowly improved over the 10-year study period, by the end of the study, 18% of women that could have benefited from the potentially life-saving therapy were not receiving treatment. Researchers also discovered that approximately 3% of women inappropriately received AET despite lacking the required hormone receptors.. "The use of adjuvant endocrine therapy slowly gained popularity over this time," commented senior author Dezheng Huo (University of Chicago, IL, US). "It improved after 2004, rising from 70% in 2004 to almost 84 % in 2011. ...
Factory quality control, hot sell strong steroid powder:Exemestane with CAS NO:107868-30-4 Exemestane is a drug used to treat breast cancer. It is a member of the class of drugs known as aromatase inhibitors. Some breast cancers...
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Among patients with advanced, hormone receptor-positive breast cancer who had not been treated previously for advanced disease, those who took fulvestrant
Adding the targeted therapy ribociclib to hormone therapy significantly improved overall survival (OS) in premenopausal patients with advanced hormone receptor-positive (HR+) breast cancer, according to results of the MONALEESA-7 Phase III clinical trial led by researchers at The University of Texas MD Anderson Cancer Center.
Health,The U.S. Food and Drug Administration (FDA) have approved the drug Fem...Various studies have been done before the approval of the drug. The ...It said that the Novartis drug Femara was very efficient in controll...This drug has to be given in the initial therapy after surgery inste...The drug is an aromatase inhibitor and prevents/inhibits the product...,Femara:,The,Wonder,Drug,to,Prevent,Relapse,of,Breast,Cancer.,medicine,medical news today,latest medical news,medical newsletters,current medical news,latest medicine news
Learn why Femara (letrozole), a type of aromatase inhibitor, is sometimes recommended for breast cancer treatment, plus get info on its side effects.
Postmenopausal women with estrogen receptor-positive breast cancer will be able to have breast-conserving surgery if they are given preoperative treatment with aromatase inhibitors
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Background: Preclinical data suggest that patients with ER+ Breast Cancer become less sensitive to hormonal therapy by upregulation of the mTOR pathway. BOLERO-2 demonstrated that the combination of an allosteric mTOR inhibitor and an aromatase inhibitor improves progression-free survival in postmenopausal women with hormone resistant advanced breast cancer (NEJM 2012; 366:520-529). AZD2014 is a selective dual mTORC1 and mTORC2 inhibitor whilst fulvestrant is an estrogen receptor antagonist that is approved for the treatment of postmenopausal women with disease progression following antiestrogen therapy. This phase I trial assessed the safety, tolerability, pharmacokinetics, and preliminary efficacy of AZD2014 administered in combination with fulvestrant.. Methods: Continuous BID or QD dosing of AZD2014 was administered in combination with fulvestrant 500 mg intramuscularly on day 1 of each 28 day cycle. An additional 500 mg dose of fulvestrant was administered on day 15 of cycle 1 as per the ...
This is a two stage study, with an initial dose escalation phase I study and subsequent double blind randomised phase II controlled trial. Eligible patients are post-menopausal women with metastatic ER+ breast cancer not suitable for surgical resection. Patients should be suitable for endocrine treatment, but have received no more than 3 previous lines of endocrine treatment and up to 1 line of chemotherapy for metastatic disease. They will also have had progressive disease during treatment with an aromatase inhibitor. Following the dose-escalation in stage 1, patients will be randomised to receive fulvestrant plus either placebo or 480mg (or maximum tolerated dose) of AZD5363 oral capsules or tablets taken once daily. Patients will receive fulvestrant in combination with either placebo or AZD5363 until disease progression. Patients may continue to receive fulvestrant and AZD5363/placebo treatment even after the last trial visit. ...
Aromatase inhibitors like letrozole blocks the aromatase enzyme. This procedure reduces the conversion of testosterone into estrogen. Letrozole is an ...
This drug works through avoiding the activity of the aromatase enzyme. The enzyme is part of the production of female sex hormone, the oestrogen who went passed through menopause. It converts sex hormones testosterone and androstenedione into oestrogen. The drug also avoids the conversion through blocking of the activity of aromatose enzyme. This result in the reduction of oestrogen levels. Through reduction of the levels of oestrogen, exemestane blocks the breast cancer cells from growing. However, exemestane will only be useful in the treatment of breast cancers which are sensitive to oestrogen or the oestrogen receptor positive cancers. Exemestane is also effective in breast cancer treatment for women in postmenopausal stage, naturally or as the result of any medical treatment. It may also be used for the treatment of early invasive cancers, following the completion of 2 to 3 years of tamoxifen treatment. Advanced cancers may also be treated where cancer continued to grow even after the use ...
rs7158782 is one of 4 SNPs found on chromosome 14 near a gene known as T-cell leukemia/lymphoma 1A (TCL1A). This gene appears to be estrogen dependent. In a study of ~300 patients with early-stage estrogen receptor-positive (ER+) breast cancer who were treated with the aromatase inhibitor (AI) anastrozole or exemestane and who developed musculoskeletal toxicity severe enough to prompt discontinuation, rs7158782(G) allele carriers were at ~2x higher risk for toxicity (CI: 1.5 - 2.9, p , 10e-6). The population attributable risk (i.e., the fraction of such adverse events that could be due to this allele) was estimated to be 11%. 10.1200/JCO.2010.28.5064 An editorial accompanying this article downplays the clinical utility of this finding, since testing for this allele, given its frequency and (mere) doubling of risk, has about equal odds of yielding a true positive and a false positive. 10.1200/JCO.2010.31.2926 ...
Letrozole is an aromatase inhibitor that is approved in the first-line treatment of postmenopausal women with hormone receptor-positive or hormone recep
Lee S. Schwartzberg, MD, of the West Cancer Center, discusses phase II study findings evaluating exemestane with or without enzalutamide in patients with hormone receptor-positive breast cancer (Abstract GS4-07).. ...
L. Jose, MD, PhD, Milton Keynes College: "Order online Aromasin no RX - Discount Aromasin online OTC.".. The main symptoms and signs of hy ponatremia are as a result of generic 25 mg aromasin with mastercard the osmotic shift of water into mind cells. It has a variety of results including the stimulation of the adrenal gland to release the hor mone aldosterone. Internal mammary (ipsilateral): lymph nodes within the intercostal spaces alongside the sting of the sternum within the endothoracic fascia four. Association of neoplasia and congenital malformations the idea that teratogenesis and oncogenesis have shared mechanisms is well documented by numerous examples. In the 4 electrode measurement, the ana the analyzer measures the current and makes use of Ohms lyzer injects an alternating present by way of the outer legislation to calculate the resistance of the solution (resis electrodes and measures the voltage across the inner tance = voltage/present). Sonography avoids underestimation of ...
Healthy postmenopausal women who took 25 mg of a type of aromatase inhibitor called exemestane daily for two years experienced bone loss in their forearm and ankle, the study published in the journal Lancet found.
This study is investigating the efficacy and tolerability of adding pertuzumab to first-line therapy with trastuzumab + an aromatase inhibitor (anastrozole or
Aromatase inhibitors like exemestane (which forms a permanent and deactivating bond with the aromatase enzyme) and anastrozole ... Avendaño, C.; Menéndez, J. C. (2008). "Aromatase Inhibitors". Medicinal Chemistry of Anticancer Drugs. Elsevier. pp. 65-73. doi ... Aromatase is an enzyme which converts some enones with a six membered ring to aromatic rings - specifically testosterone to ... Aromatase Aromatic hydrocarbon Reppe, W.; Schlichting, O.; Klager, K.; Toepel, T. (1948). "Cyclisierende Polymerisation von ...
... aromatase, on breast cancer. Brodie managed to get an aromatase inhibitor into a limited clinical trial in breast cancer ... aromatase. They developed several steroidal aromatase inhibitors, she focused on 4-OHA. In 1979, she moved to Maryland, ... She presented a paper on her aromatase inhibitors at a Rome conference in 1980, which led to collaboration with Charles Coombes ... 4-OHA, named Formestane, was the first aromatase inhibitor used on breast cancer patients and proved to be a significant ...
Aromatase inhibitors. *Non-selective: Aminoglutethimide. *Testolactone. *Selective: Anastrozole. *Exemestane. *Fadrozole. * ...
Aromatase inhibitors. *Non-selective: Aminoglutethimide. *Testolactone. *Selective: Anastrozole. *Exemestane. *Fadrozole. * ... Kuhl, H.; Schneider, H. P. G. (2013). "Progesterone - promoter or inhibitor of breast cancer". Climacteric. 16 Suppl 1: 54-68. ...
... and its major active metabolite 5α-DHNET have been found to act as irreversible aromatase inhibitors (Ki = 1.7 ... Mainly CYP3A4 (liver);[1] also 5α-/5β-reductase, 3α-/3β-HSD, and aromatase. ... Norethisterone is a substrate for and is known to be an inhibitor of 5α-reductase, with 4.4% and 20.1% inhibition at 0.1 and 1 ... Norethisterone is a very weak inhibitor of CYP2C9 and CYP3A4 (IC50 = 46 μM and 51 μM, respectively), but these actions require ...
Although aromatase inhibitors and antigonadotropins can be considered antiestrogens by some definitions, they are often treated ... Riggins RB, Bouton AH, Liu MC, Clarke R (2005). "Antiestrogens, aromatase inhibitors, and apoptosis in breast cancer". Vitam. ... aromatase inhibitors (AIs) like anastrozole, and antigonadotropins including androgens/anabolic steroids, progestogens, and ... Aromatase inhibitors and antigonadotropins reduce the production of estrogen, while the term "antiestrogen" is often reserved ...
Aromatase inhibitors. *Non-selective: Aminoglutethimide. *Testolactone. *Selective: Anastrozole. *Exemestane. *Fadrozole. * ... PEP is a strong inhibitor of several enzymes, including acid phosphatase, alkaline phosphatase, and hyaluronidase.[37][38][39] ... Cytochrome P450 inhibitors, especially of CYP3A4, can reduce the metabolism of estradiol and thereby increase estradiol levels ... John's wort; in addition, while ritonavir and nelfinavir are known as strong inhibitors, they have an inducing effect in ...
Aromatase inhibitors. *Non-selective: Aminoglutethimide. *Testolactone. *Selective: Anastrozole. *Exemestane. *Fadrozole. * ... Aromatase deficiency is ultimately suspected which is involved in the synthesis of estrogen in humans and has therapeutic ... Rochira V, Carani C (October 2009). "Aromatase deficiency in men: a clinical perspective". Nature Reviews. Endocrinology. 5 (10 ... When estrogen levels were raised through the increased activity of the enzyme aromatase in male lab mice, OCD rituals were ...
Aromatase inhibitors. *Non-selective: Aminoglutethimide. *Testolactone. *Selective: Anastrozole. *Exemestane. *Fadrozole. * ...
Aromatase inhibitors. *First-generation: Aminoglutethimide. *Testolactone. *Second-generation: Fadrozole. *Formestane. *Third- ...
Progesterone.[citation needed] Aromatase inhibitors. Adjusted for age and stage the prognosis for breast cancer in males is ...
Medications such as aromatase inhibitors have been found to be effective in rare cases of gynecomastia from disorders such as ... Aromatase inhibitors (AIs) such as anastrozole have been used off-label for cases of gynecomastia occurring during puberty but ... Wit JM, Hero M, Nunez SB (October 2011). "Aromatase inhibitors in pediatrics". Nature Reviews. Endocrinology. 8 (3): 135-47. ... "Use of aromatase inhibitors in children and adolescents with disorders of growth and adolescent development". Pediatrics. 121 ( ...
Aromatase inhibitors show promising results. A Cochrane review came to the results that the aromatase inhibitor letrozole ...
In addition to its activity as an aromatase inhibitor, plomestane has weak androgenic properties. Minamestane F. Macdonald ( ... January 1998). "Aromatase inhibitors as potential cancer chemopreventives". Cancer Epidemiology, Biomarkers & Prevention. 7 (1 ... irreversible aromatase inhibitor which was under development by Marion Merrell Dow/Hoechst Marion Russell (now Hoechst AG) as ...
... is an aromatase (CYP19A1) inhibitor. Huuskonen, P; Myllynen, P; Storvik, M; Pasanen, M (2013). "The effects of ...
Chalcones are also natural aromatase inhibitors. Chalcones are aromatic ketones with two phenyl rings that are also ... "Chalcones are potent inhibitors of aromatase and 17β-hydroxysteroid dehydrogenase activities". Life Sciences. 68 (7): 751-61. ...
Raman JD, Schlegel PN (February 2002). "Aromatase inhibitors for male infertility". The Journal of Urology. 167 (2 Pt 1): 624-9 ... Estradiol is produced by action of aromatase mainly in the Leydig cells of the mammalian testis, but also by some germ cells ... Ryan KJ (August 1982). "Biochemistry of aromatase: significance to female reproductive physiology". Cancer Research. 42 (8 ... A portion of the androstenedione is converted to testosterone, which in turn undergoes conversion to estradiol by aromatase. In ...
Examples of aromatase inhibitors include anastrozole and letrozole. Evidence for aromatase inhibitors is limited due to the ... Aromatase inhibitors are medications that block the formation of estrogen and have become of interest for researchers who are ... Nawathe A, Patwardhan S, Yates D, Harrison GR, Khan KS (June 2008). "Systematic review of the effects of aromatase inhibitors ... Attar E, Bulun SE (May 2006). "Aromatase inhibitors: the next generation of therapeutics for endometriosis?". Fertility and ...
... and aromatase inhibitors. As of 2016 the only marketed SERD was fulvestrant. As of November 2016 other SERDs under development ... Aromatase inhibitor Estrogen deprivation therapy Lee, CI; Goodwin, A; Wilcken, N (3 January 2017). "Fulvestrant for hormone- ...
June 1994). "Novel aromatase and 5 alpha-reductase inhibitors". The Journal of Steroid Biochemistry and Molecular Biology. 49 ( ... Unlike other steroidal aromatase inhibitors such as formestane and exemestane, minamestane does not have androgenic properties ... Minamestane (INN (former developmental code name FCE-24,928) is a steroidal aromatase inhibitor which was under development by ... Combs, Donald W (1995). "Review Oncologic, Endocrine & Metabolic: Recent developments in aromatase inhibitors". Expert Opinion ...
Aromatase is an enzyme that synthesizes estrogen. Aromatase inhibitors block the synthesis of estrogen. This lowers the ... Type II aromatase inhibitors such as anastrozole and letrozole, by contrast, are not steroids and work by interfering with the ... Along with other aromatase inhibitors, exemestane is on the World Anti-Doping Agency's list of prohibited substances. Oral ... Like the aromatase inhibitors formestane and atamestane, exemestane is a steroid that is structurally similar to 4- ...
Vanden Bossche HV, Moereels H, Koymans LM (1994). "Aromatase inhibitors--mechanisms for non-steroidal inhibitors". Breast ... but instead having pharmacological activity as a selective aromatase inhibitor similar to the related drug aminoglutethimide, ...
Reversible inhibitors[edit]. Types of reversible inhibitors[edit]. Reversible inhibitors attach to enzymes with non-covalent ... fraction of the enzyme population bound by inhibitor [. I. ]. [. I. ]. +. K. i. {\displaystyle {\cfrac {{\ce {[I]}}}{[{{\ce {I ... Uses of inhibitors[edit]. Enzyme inhibitors are found in nature and are also designed and produced as part of pharmacology and ... Examples of irreversible inhibitors[edit]. Trypanothione reductase with the lower molecule of an inhibitor bound irreversibly ...
"Metastatic Uterine Leiomyosarcoma Regression Using an Aromatase Inhibitor". Obstetrics & Gynecology. 110 (2 Pt 2): 518-520. doi ...
"Bicalutamide and third-generation aromatase inhibitors in testotoxicosis". Pediatrics. 126 (3): e728-33. doi:10.1542/peds.2010- ...
Robert A. Copeland (2013). Evaluation of Enzyme Inhibitors in Drug Discovery: A Guide for Medicinal Chemists and ... Suhara, K., Ohashi, K., Takahashi, K. and Katagiri, M. (1988). "Aromatase and nonaromatizing 10-demethylase activity of adrenal ... Kupfer, D., Miranda, G.K., Navarro, J., Piccolo, D.E. and Theoharides, A.D. (1979). "Effect of inducers and inhibitors of ... http://books.google.com/books/about/Evaluation_of_Enzyme_Inhibitors_in_Drug.html?id=l2rMy8QNUk0C. ...
Medications such as aromatase inhibitors have been found to be effective in rare cases of gynecomastia from disorders such as ... Aromatase inhibitors (AIs) such as anastrozole have been used off-label for cases of gynecomastia occurring during puberty but ... Wit JM, Hero M, Nunez SB (October 2011). "Aromatase inhibitors in pediatrics". Nature Reviews. Endocrinology. 8 (3): 135-47. ... "Use of aromatase inhibitors in children and adolescents with disorders of growth and adolescent development". Pediatrics. 121 ( ...
Aromatase inhibitors are a class of hormonal agents that form part of the therapy for some types of breast cancer. These agents ... Advantages of using aromatase inhibitors. The advantages of using aromatase inhibitors over other hormonal agents such as ... What are Aromatase Inhibitors?. News-Medical. 23 July 2019. ,https://www.news-medical.net/health/What-are-Aromatase-Inhibitors ... What are Aromatase Inhibitors?. News-Medical. https://www.news-medical.net/health/What-are-Aromatase-Inhibitors.aspx. ( ...
... aromatase inhibitors - are more effective than tamoxifen for reducing mortality among women with ER-positive breast cancer. ... Aromatase inhibitors lower estrogen levels by preventing the enzyme aromatase - found in fat tissue - from changing other ... Aromatase inhibitors reduced breast cancer mortality by 40%. For their study, the team analyzed the data of nine clinical ... Aromatase inhibitors remove only the tiny amount of estrogen that remains in the circulation of women after the menopause - but ...
Discontinuation and nonadherence were higher among breast cancer patients taking brand name aromatase inhibitors (BAIs) vs ... Aromatase inhibitor use has been shown to reduce the risk of breast cancer recurrence. However, studies reported only 40%-60% ... Discontinuation and nonadherence were higher among breast cancer patients taking brand name aromatase inhibitors (BAIs) vs ... Discontinuation and nonadherence were higher among breast cancer patients taking brand name aromatase inhibitors (BAIs) vs ...
Aromatase inhibitors and tamoxifen are two types of hormonal therapy.. A study found that women diagnosed with early-stage, ... The aromatase inhibitors can weaken bones and make women more likely to break a bone, though this is uncommon. Tamoxifen ... In other cases, women take tamoxifen for 2 or 3 years and then switch to an aromatase inhibitor until the hormonal therapy has ... Women who got tamoxifen for 2 to 3 years followed by an aromatase inhibitor had the same risk of cardiovascular problems as ...
More: What Are Aromatase Inhibitors?. In 2005, Breast Cancer Action launched an online survey to collect information from women ... Aromatase inhibitors (AIs) have quickly become standard treatments for postmenopausal women with estrogen-receptor-positive ... These reports are dedicated to the women who generously took the time to respond to BCAs Aromatase Inhibitor Side Effects ... In June 2008, BCA released the follow-up report, Side Effects Revisited: Womens Experiences with Aromatase Inhibitors based on ...
Tags: 50 to 64, 65 and older, Estrogen-Receptor Positive, Aromatase Inhibitors, Arimidex (chemical name: anastrozole), Aromasin ... Aromatase inhibitors arent commonly used to reduce recurrence risk in premenopausal women. Still, in some cases a ... "The treatment with aromatase inhibitors worked significantly better in the non-smoking patients," she continued. "However, we ... "Smokers who were treated with aromatase inhibitors had a three times higher risk of recurrence of breast cancer compared with ...
Aromatase inhibitors may cause muscle and joint aches and pains. Less common but more severe side effects of aromatase ... Both tamoxifen and aromatase inhibitors can cause side effects. Tamoxifen may cause hot flashes and increase the risk of blood ... All the women had been taking an aromatase inhibitor for at least 30 days and all had a joint pain score that was 3 or higher ... Aromatase inhibitors arent commonly used to reduce recurrence risk in premenopausal women. ...
Another aromatase inhibitor, androst-4-ene-3,6,17-trione, has been efficiently prepared using PCC on montmorillonite K10, under ... Improved syntheses of aromatase inhibitors and neuroactive steroids efficient oxidations and reductions at key positions for ... Using testosterone as starting material, a new short synthesis of an aromatase inhibitor, 4-OHA, has been achieved through ...
Taking the aromatase inhibitor exemestane (Aromasin) for primary prevention of breast cancer may weaken the bones, researchers ... Aromatase Inhibitor Linked to Bone Loss. Taking the aromatase inhibitor exemestane (Aromasin) for primary prevention of breast ... Taking the aromatase inhibitor exemestane (Aromasin) for primary prevention of breast cancer may weaken the bones, researchers ... Loss of bone density and fractures are known risks of aromatase inhibitors in breast cancer survivors taking the drugs to ...
SEARCH RESULTS for: Aromatase Inhibitors [Drug Class] (65 results) * Share : JavaScript needed for Sharing tools. Bookmark & ...
Aromatase inhibitors after Tamoxifen Ten Year Survival With Aromatase Inhibitor Use Evista as adjuvant therapy DCIS Hormone ... it is reasonable to believe that aromatase inhibitors should be effective.. Aromatase inhibitors prevent estrogen synthesis, ... Can aromatase inhibitors be used to prevent reccurrence of malignant mammary tumors in dogs? If so, which one is indicated, and ... Aromatase Inhibitors or Tamoxifen Canine Mammary Tumors & Spaying Drug/Herbal Interactions with Arimidex Tamoxifen Therapy for ...
Aromatase inhibitors may cause muscle and joint aches and pains. Less common but more severe side effects of aromatase ... Both tamoxifen and aromatase inhibitors can cause side effects. Tamoxifen may cause hot flashes and increase the risk of blood ... If youre currently taking an aromatase inhibitor and having joint pain, you may want to talk to your doctor about this study ... The women all had been taking an aromatase inhibitor for between 3 weeks and 3 months. All the women reported having moderate ...
Neoadjuvant aromatase inhibitor therapy promotes breast conservation and provides a rich context for biomarker research. ... There were some brief presentations related to aromatase inhibitors on Thursday morning. Heres a short summary of what was ...
Aromatase inhibitors work by inhibiting the action of the enzyme aromatase, which converts androgens into estrogens by a ... There are two types of aromatase inhibitors approved to treat breast cancer: Irreversible steroidal inhibitors, such as ... Chen S, Kao YC, Laughton CA (1997). "Binding characteristics of aromatase inhibitors and phytoestrogens to human aromatase". J ... inhibit the synthesis of estrogen via reversible competition for the aromatase enzyme. Available aromatase inhibitors (AIs) ...
c) a history of generalized musculoskeletal pain that began or worsened since starting treatment with the aromatase inhibitor. ... 3.Vitamin D threshold to prevent aromatase inhibitor-induced arthralgia: a prospective cohort study.Breast Cancer Res Treat. ... Fifty percent of women taking aromatase inhibitors reported musculoskeletal pain, and up to 30% reported fatigue. The results ... multiple studies confirm a reduction in side effects of aromatase inhibitors The most recent of the four studies was presented ...
Biological and clinical effects of aromatase inhibitors in neoadjuvant therapy.. Miller WR1, Dixon JM, Cameron DA, Anderson TJ. ... The results suggest that potent specific aromatase inhibitors will be valuable in treating hormone-dependent cancers. ...
... adjuvant treatment with aromatase inhibitors does not raise the risk for cardiovascular events, a researcher said. ... The aromatase inhibitors are rapidly replacing tamoxifen as the adjuvant treatment of choice for early breast cancer in ... Dickler said, "When youre comparing an [aromatase inhibitor] to tamoxifen, its easy to forget that tamoxifen does have lipid- ... Monnier concluded that comparisons of aromatase inhibitors with placebo may be more useful in determining the risks associated ...
The enzyme that is responsible for this conversion is aromatase, made primarily in fat and other tissue, especially in the ... Also, there will be information from trials testing aromatase inhibitors following 5 years of tamoxifen. The other aromatase ... There are ongoing trials that will anwer the questions of 2-3 years of tamoxifen followed by an aromatase inhibitor. For newly ... The first such study to be reported was a comparison of the aromatase inhibitor anastrozole (trade name Arimidex) to tamoxifen ...
If nonsteroidal aromatase Inhibitors are not working or patients are relapsing, then the use of steroidal aromatase inhibitors ... Aromatase inhibitors stops this conversion and lowers the levels of estrogen. Treating breast cancer with aromatase inhibitors ... "Aromatase inhibitors: Are there differences between steroidal and nonsteroidal aromatase inhibitors and do they matter?". ... Steroidal aromatase inhibitors irreversibly inhibit the enzyme by binding covalently to the binding site of aromatase so the ...
Aromatase inhibitors arent used to reduce recurrence risk in premenopausal women. In 2012 and 2013, large studies found that ... So researchers wanted to know if taking an aromatase inhibitor for 10 years would offer more benefits than taking one for 5 ... Mamounas also said that women younger than 60 also may get benefits from extended aromatase inhibitor therapy because they have ... "The study showed that extended adjuvant therapy with an aromatase inhibitor results in a small but potentially important ...
This topic contains 21 study abstracts on Aromatase Inhibitor Drugs indicating they may contribute to Breast Cancer, Drug- ... Problem Substances : Aromatase Inhibitor Drugs, Letrozole (trade name Femera). Adverse Pharmacological Actions : Endocrine ... 24 Abstracts with Aromatase Inhibitor Drugs Research. Filter by Study Type. Animal Study. ... The aromatase inhibitor letrozole has endocrine disruptive properties on hypothalamic-pituitary output in normal women.Feb 24, ...
Aromatase inhibitors, when used for up to three years in combination with growth hormone, may effectively and safely help very ... Aromatase Inhibitor, Growth Hormone, Adolescent, Boys, Puberty, Clinical Trial, Endocrinology, Endocrine Society, ENDO 2016 ... Newswise - Boston, MA- Aromatase inhibitors, when used for up to three years in combination with growth hormone, may ... "This work provides the longest treatment and follow up reported using aromatase inhibitors (AIs) in adolescent males, showing ...
... by interfering with an aromatase enzyme. Aromatase inhibitors are used as a type of hormone therapy for postmenopausal women ... aromatase inhibitor listen (uh-ROH-muh-tays in-HIH-bih-ter) A drug that prevents the formation of estradiol, a female hormone, ... by interfering with an aromatase enzyme. Aromatase inhibitors are used as a type of hormone therapy for postmenopausal women ...
... an aromatase inhibitor currently used to prevent breast cancer recurrence in postmenopausal women, shows promise in the ... "This study demonstrates the potential of aromatase inhibitors to significantly and rapidly reduce disease severity and pain, ... an aromatase inhibitor currently used to prevent breast cancer recurrence in postmenopausal women, shows promise in the ... We need to attack the root problem - the aromatase - in order to eliminate this cycle, halt the local production of estrogen ...
  • Less common but more severe side effects of aromatase inhibitors are heart problems, osteoporosis, and broken bones. (breastcancer.org)
  • Biological and clinical effects of aromatase inhibitors in neoadjuvant therapy. (nih.gov)
  • Hot flashes, night sweats, and joint pain are common side effects of aromatase inhibitors. (breastcancer.org)
  • Howell A, Cuzick J (2005) Vascular effects of aromatase inhibitors: data from clinical trials. (springer.com)
  • Joint pain (arthralgia) and muscle pain (myalgia) are common side effects of aromatase inhibitors [ 85-87 ]. (komen.org)
  • Patients also need to consider the side effects of aromatase inhibitors and the cost of the drug. (facingourrisk.org)
  • One of the side effects of aromatase inhibitors is the development of joint pain, a complication known as the Arthralgia Syndrome. (clinicaltrials.gov)
  • About 46 percent of women taking aromatase inhibitors have joint pain and about 15 percent have muscle pain [ 85-87 ]. (komen.org)
  • Aromatase inhibitors can induce an arthralgia syndrome. (greenmedinfo.com)
  • Although the side effect profile of aromatase inhibitors is well known, including common side effects like arthralgia, bone pain, arthritis, hot flashes, and more serious problems like osteoporosis, we present a case of an uncommon side effect of these medications. (hindawi.com)
  • Breast cancer survivors who are prescribed an adjuvant aromatase inhibitor (AI) want ongoing communication with their oncology clinician about the potential for arthralgia and how these joint adverse effects can be managed through regular physical activity, a study published online ahead of print in the journal Supportive Care in Cancer has shown. (oncologynurseadvisor.com)
  • Aromatase inhibitor associated arthralgia: the importance of oncology provider-patient communication about side effects and potential management through physical activity [published online ahead of print January 12, (oncologynurseadvisor.com)
  • Aromatase inhibitors (AIs) are most commonly used for breast cancer patients with hormone receptor positive disease. (hindawi.com)
  • They seek to evaluate the application of Entinostat for the reduction, or prevention of, treatment resistance to aromatase inhibitors in hormone receptor positive breast cancer. (wikipedia.org)
  • Ligand and Structure-Based Drug Designing approaches (LBDD and SBDD) are involved in development of active and more specific Nonsteroidal Aromatase Inhibitors (NSAIs). (igi-global.com)
  • Fadrozole (INN), sold under the brand name Afema (by Novartis), is a selective, nonsteroidal aromatase inhibitor which is or has been used in Japan for the treatment of breast cancer. (wikipedia.org)
  • Norendoxifen, also known as N,N-didesmethyl-4-hydroxytamoxifen, is a nonsteroidal aromatase inhibitor (AI) of the triphenylethylene group that was never marketed. (wikipedia.org)
  • Abstract S5-07: Aromatase inhibitors and endothelial function: Is there an association with early cardiovascular disease? (aacrjournals.org)
  • Anne Hudson Blaes, MD , of the University of Minnesota, discusses the association between aromatase inhibitors, endothelial function, and early heart disease (Abstract S5-07). (ascopost.com)
  • We are not aware of any studies published on the effect of aromatase inhibitors in dogs with mammary carcinoma, but based on the fact that many of these tumors are estrogen-dependent, express estrogen receptors, and respond to tamoxifen, it is reasonable to believe that aromatase inhibitors should be effective. (oncolink.org)
  • A single-arm trial of duloxetine-up to 120 mg/d- showed clinically significant improvement in pain scores in patients on aromatase inhibitors. (ascopost.com)