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

It acts as a potent competitive antagonist of the androgen receptor (AR) (Ki = 10 nM; IC50Tooltip half-maximal inhibitory ... It may have some weak partial agonist activity at the androgen receptor. BMS-641988 is transformed by CYP3A4 into BMS-570511, ... Vasaitis TS, Njar VC (April 2010). "Novel, potent anti-androgens of therapeutic potential: recent advances and promising ... a novel and potent inhibitor of androgen receptor signaling for the treatment of prostate cancer". Cancer Res. 69 (16): 6522-30 ...

Similarly to bicalutamide, the drug acts as a selective antagonist of the androgen receptor (AR). However, unlike bicalutamide ... it is a reversible covalent antagonist and stays bound to the receptor for a far longer amount of time. As a result of this ... so 5N-bicalutamide would appear to be among the most potent AR antagonists to have been developed thus far. Cyanonilutamide N- ... The emperor of all anti-androgens". Transl Androl Urol. 2 (2): 119-120. doi:10.3978/j.issn.2223-4683.2012.09.04. PMC 3785324. ...

Flutamide, a pure antagonist of the androgen receptor, is effective in treating acne in women. It appears to reduce acne ... Bicalutamide, a pure androgen receptor antagonist with the same mechanism as flutamide and with comparable or superior ... Both androgens and IGF-1 seem to be essential for acne to occur, as acne does not develop in individuals with complete androgen ... Pregnancy can increase androgen levels, and consequently, oily sebum synthesis. Acne can be a side effect of testosterone ...

... has been shown to be an antagonist toward androgen and estrogen receptors in vitro. Some work has shown that organic ... Ma, R.; Cotton, B.; Lichtensteiger, W.; Schlumpf, M. (2003). "UV Filters with Antagonistic Action at Androgen Receptors in the ... androgen receptor (AR), and progesterone receptor (PR) in reporter gene bioassays". Toxicol. Sci. 83 (2): 264-272. doi:10.1093/ ...

Non-steroidal selective androgen receptor antagonists, developed as a treatment for androgen-sensitive prostate cancer, are ... ANDROGEN RECEPTOR BLOCKERS: Androgen receptor blockers bind directly to the androgen receptor and either competitively inhibit ... Gauthier S, Martel C, Labrie F (October 2012). "Steroid derivatives as pure antagonists of the androgen receptor". The Journal ... ISBN 978-3-662-45138-0. Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): ...

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

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

It acts as a selective competitive silent antagonist of the androgen receptor (AR), the biological target of androgens like ... Darolutamide is a nonsteroidal antiandrogen (NSAA), and acts as a selective antagonist of the androgen receptor (AR). It has ... In addition to its actions as an AR antagonist, darolutamide has been found to act as a silent antagonist of the progesterone ... Darolutamide is approved for use concurrently with a gonadotropin-releasing hormone (GnRH) agonist or antagonist or bilateral ...

Alternatively, the combination of the androgen receptor antagonist bicalutamide and the aromatase inhibitor anastrozole may be ...

At high concentrations, BPA also binds to and acts as an antagonist of the androgen receptor (AR). In addition to receptor ...

July 2013). "An androgen receptor N-terminal domain antagonist for treating prostate cancer". The Journal of Clinical ... Monaghan AE, McEwan IJ (2016). "A sting in the tail: the N-terminal domain of the androgen receptor as a drug target". Asian ... Martinez-Ariza G, Hulme C (2015). "Recent advances in allosteric androgen receptor inhibitors for the potential treatment of ... of the androgen receptor (AR) developed by ESSA Pharmaceuticals and was under investigation for the treatment of prostate ...

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

It is a weak competitive antagonist of the androgen receptor (AR) and a potent 5α-reductase inhibitor. Structurally, ... Dehennin L (February 1993). "Secretion by the human testis of epitestosterone, with its sulfoconjugate and precursor androgen 5 ... is an endogenous steroid and an epimer of the androgen sex hormone testosterone. ...

This initial flare may be treated by co-prescribing/co-administering an androgen receptor antagonist such as bicalutamide ( ... It may also be used in the treatment of male-to-female transgender people and is favoured above other anti-androgens in some ...

... is an antiandrogen, and hence is an antagonist of the androgen receptor, the biological target of androgens like ... Oxendolone is not a silent antagonist of the androgen receptor but is rather predominantly antagonistic with weak agonistic ... Sudo K, Yamazaki I, Masuoka M, Nakayama R (1979). "Anti-androgen TSAA-291. IV. Effects of the anti-androgen TSAA-291 (16 beta- ... Masuoka M, Masaki T, Yamazaki I, Hori T, Nakayama R (1979). "Anti-androgen TSAA-291. III. Hormonal spectra of anti-androgen ...

It is a selective androgen receptor antagonist with reduced brain distribution compared to the structurally related ...

However, it has approximately three-fold lower potency as an antagonist of the androgen receptor (AR) relative to CPA. Like CPA ... Thus we are left with CPA as the only anti-androgen that is already on the market in several countries. Hughes A, Hasan SH, ... 27 November 2013). Androgens II and Antiandrogens / Androgene II und Antiandrogene. Springer Science & Business Media. pp. 241- ... 27 November 2013). Androgens II and Antiandrogens / Androgene II und Antiandrogene. Springer Science & Business Media. pp. 279 ...

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

It is a known endocrine disruptor (androgen receptor antagonist)[citation needed] which interferes with the sexual ... "The fungicide procymidone alters sexual differentiation in the male rat by acting as an androgen-receptor antagonist in vivo ...

... a term which can refer more specifically to antagonists of the androgen receptor. Finasteride results in a decrease of ... "Aldosterone antagonists in addition to renin angiotensin system antagonists for preventing the progression of chronic kidney ... Androgens and estrogens may be involved in the cause of hidradenitis suppurativa (acne inversa). Two case series have reported ... It is an analogue of androgen steroid hormones like testosterone and DHT. As an unconjugated steroid, finasteride is a highly ...

... cancer that is not responding to first-line androgen deprivation therapy or treatment with androgen receptor antagonists. ... With the nonsteroidal androgen synthesis inhibitor ketoconazole as a model, they developed abiraterone acetate, filing a patent ... Small EJ (November 2014). "Can targeting the androgen receptor in localized prostate cancer provide insights into why men with ... Tindall DJ, Mohler J (20 April 2009). Androgen Action in Prostate Cancer. Springer Science & Business Media. pp. 748-. ISBN 978 ...

Similarly to abiraterone acetate, seviteronel has also been found to act to some extent as an antagonist of the androgen ... It is a nonsteroidal CYP17A1 inhibitor and works by inhibiting the production of androgens and estrogens in the body. As of ... Stein MN, Patel N, Bershadskiy A, Sokoloff A, Singer EA (2014). "Androgen synthesis inhibitors in the treatment of castration- ... Seviteronel is a nonsteroidal antiandrogen, acting specifically as an androgen synthesis inhibitor via inhibition of the enzyme ...

... competitive silent antagonist of the androgen receptor (AR). Both agents show much higher affinity and more potent inhibition ... 4-. ISBN 978-0-12-803201-5. ODM-201 - New generation androgen receptor inhibitor targeting resistance mechanisms to androgen ... a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer ... Fizazi K, Albiges L, Loriot Y, Massard C (2015). "ODM-201: a new-generation androgen receptor inhibitor in castration-resistant ...

2004). "Agonist-antagonist induced coactivator and corepressor interplay on the human androgen receptor". Mol. Cell. Endocrinol ...

... show irregular reproductive development due to their function as androgen receptor antagonists that inhibit androgen-activated ... Mar 2001). "Organophosphate antagonism of the androgen receptor". Toxicological Sciences. 60 (1): 1-2. doi:10.1093/toxsci/60.1. ...

... and bicyclic hydantoin-derived selective androgen receptor antagonists and agonists in human urine using LC-MS/MS". Analytical ... Gao W, Dalton JT (March 2007). "Expanding the therapeutic use of androgens via selective androgen receptor modulators (SARMs ... Selective androgen receptor modulators may also be used by athletes to assist in training and increase physical stamina and ... LGD-2226 is an orally active, potent and selective agonist for androgen receptors which was shown to have anabolic effects in ...

... and bicyclic hydantoin-derived selective androgen receptor antagonists and agonists in human urine using LC-MS/MS". Analytical ... Enobosarm, also known as ostarine or MK-2866, is a selective androgen receptor modulator (SARM) developed by GTx, Inc. for the ... ISBN 978-0-12-814082-6. Fonseca GW, Dworatzek E, Ebner N, Von Haehling S (August 2020). "Selective androgen receptor modulators ... Zhang X, Lanter JC, Sui Z (September 2009). "Recent advances in the development of selective androgen receptor modulators". ...

... and bicyclic hydantoin-derived selective androgen receptor antagonists and agonists in human urine using LC-MS/MS". Analytical ... Gao W, Dalton JT (March 2007). "Expanding the therapeutic use of androgens via selective androgen receptor modulators (SARMs ... Selective androgen receptor modulators may also be used by athletes to assist in training and increase physical stamina and ... November 2003). "Bone anabolic effects of S-40503, a novel nonsteroidal selective androgen receptor modulator (SARM), in rat ...

... and bicyclic hydantoin-derived selective androgen receptor antagonists and agonists in human urine using LC-MS/MS". Analytical ... Gao W, Dalton JT (March 2007). "Expanding the therapeutic use of androgens via selective androgen receptor modulators (SARMs ... Selective androgen receptor modulators may also be used by athletes to assist in training and increase physical stamina and ... This means there is a clinical need for selective androgen receptor modulators, which produce anabolic effects in some tissues ...

... whereas LHRH antagonists decrease directly the amount of testosterone. LHRH agonists and antagonists used in androgen ... Androgen deprivation therapy (ADT), also called androgen ablation therapy or androgen suppression therapy, is an antihormone ... Prostate cancer cells usually require androgen hormones, such as testosterone, to grow. ADT reduces the levels of androgen ... The therapy can also eliminate cancer cells by inducing androgen deprivation-induced senescence. Lowering androgen levels or ...