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

Tindall DJ, Chang CH, Lobl TJ, Cunningham GR (1984). "Androgen antagonists in androgen target tissues". Pharmacology & ... Lerner LJ (1975). "Androgen antagonists". Pharmacology & Therapeutics B. 1 (2): 217-231. doi:10.1016/0306-039X(75)90006-9. PMID ... 11α-OHP was investigated as a topical antiandrogen for the treatment of androgen-dependent skin conditions in the early 1950s, ...

Tindall DJ, Chang CH, Lobl TJ, Cunningham GR (1984). "Androgen antagonists in androgen target tissues". Pharmacol Ther. 24 (3 ... Singh, Shankar; Gauthier, Sylvain; Labrie, Fernand (2000). "Androgen Receptor Antagonists (Antiandrogens) Structure-Activity ... In addition, although CPA reduces androgen production in the gonads, it can increase the production of adrenal androgens, in ... Similar depressive changes have been observed with castration, and may be a consequence of androgen deprivation in men. In ...

... is an antiandrogen, or an antagonist of the androgen receptor (AR), the biological target of the androgen sex ... ISBN 978-3-642-80859-3. Tindall DJ, Chang CH, Lobl TJ, Cunningham GR (1984). "Androgen antagonists in androgen target tissues ... Thus we are left with CPA as the only anti-androgen that is already on the market in several countries. Elks J (14 November ... eds.). Androgens II and Antiandrogens / Androgene II und Antiandrogene. Springer Science & Business Media. pp. 491-492, 516-517 ...

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

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

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

They are typically antagonists of the androgen receptor (AR) and act both by blocking the effects of androgens like ... Specifically acts as an AR antagonist, weak antigonadotropin, and weak steroidogenesis inhibitor. Used for androgen-dependent ... There are many different androgen blockers used for transition care. Spironolactone, an aldosterone receptor antagonist, is ... ISBN 978-1-60761-471-5. Singh SM, Gauthier S, Labrie F (2000). "Androgen receptor antagonists (antiandrogens): structure- ...

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

... acts as a selective antagonist of the androgen receptor (AR), competing with androgens like testosterone and ... Masiello D, Cheng S, Bubley GJ, Lu ML, Balk SP (July 2002). "Bicalutamide functions as an androgen receptor antagonist by ... Sundblad C, Landén M, Eriksson T, Bergman L, Eriksson E (February 2005). "Effects of the androgen antagonist flutamide and the ... In contrast to GnRH agonists, GnRH antagonists don't cause an initial androgen surge, and are gradually replacing GnRH agonists ...

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

Similarly to flutamide, AA560 is a selective antagonist of the androgen receptor (AR) and consequently shows progonadotropic ... Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): structure-activity ... Rasmusson GH (September 1986). "Chemical Control of Androgen Action.". Annual Reports in Medicinal Chemistry. Vol. 21. Academic ...

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

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

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

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

... acts as a selective antagonist of the androgen receptor (AR), preventing the effects of androgens like testosterone ... Nilutamide acts as a selective competitive silent antagonist of the AR (IC50 = 412 nM), which prevents androgens like ... Kemppainen JA, Wilson EM (July 1996). "Agonist and antagonist activities of hydroxyflutamide and Casodex relate to androgen ... 11-. ISBN 978-981-256-920-2. Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): ...

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

Kemppainen JA, Wilson EM (July 1996). "Agonist and antagonist activities of hydroxyflutamide and Casodex relate to androgen ... Rathkopf D, Scher HI (2013). "Androgen receptor antagonists in castration-resistant prostate cancer". Cancer Journal. 19 (1): ... ISBN 978-1-60327-829-4. Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): ... "Androgen receptor antagonists for prostate cancer therapy". Endocrine-Related Cancer. 21 (4): T105-18. doi:10.1530/ERC-13-0545 ...

Kemppainen JA, Wilson EM (July 1996). "Agonist and antagonist activities of hydroxyflutamide and Casodex relate to androgen ... Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): structure-activity ... a steroidal androgen receptor antagonist". Journal of Steroid Biochemistry. 33 (6): 1133-1138. doi:10.1016/0022-4731(89)90420-2 ... differential effects on high-androgen responder and low-androgen responder muscle groups". Endocrinology. 154 (12): 4594-4606. ...

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

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

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

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

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

Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): structure-activity ... List of androgens/anabolic steroids Hill RA, Makin HL, Kirk DN, Murphy GM (23 May 1991). Dictionary of Steroids. CRC Press. pp ... Androgens and anabolic steroids, Androstanes, Enones, All stub articles, Steroid stubs, Genito-urinary system drug stubs, ...

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

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

... is an antiandrogen, and acts as an antagonist of the androgen receptor, the biological target of androgens like ... Apalutamide acts as a selective competitive silent antagonist of the androgen receptor (AR), via the ligand-binding domain, and ... Kawahara T, Miyamoto H (June 2014). "Androgen Receptor Antagonists in the Treatment of Prostate Cancer". Clinical Immunology, ... Rathkopf D, Scher HI (2013). "Androgen receptor antagonists in castration-resistant prostate cancer". Cancer Journal. 19 (1): ...

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