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List Of Steroidal Antiandrogens
This is a list of steroidal antiandrogens. Progesterone derivatives * 11α-Hydroxyprogesterone = 11α-hydroxyprogesterone * Chlormadinone acetate = 17α-acetoxy-6-chloro-δ6-progesterone * Clometerone (L-38000) = 6α-chloro-16α-methylprogesterone * Cyproterone (SH-80881) = 1,2α-methylene-6-chloro-δ6-17α-hydroxyprogesterone * Cyproterone acetate = 1,2α-methylene-6-chloro-δ6-17α-acetoxyprogesterone * Edogestrone (PH-218) = 17α-acetoxy-3,3-ethylenedioxy-6-methylpregn-5-en-20-one * Medrogestone = 6,17α-dimethyl-δ6-progesterone * Megestrol acetate = 17α-acetoxy-δ6-6-methylprogesterone * Nomegestrol acetate = 17α-acetoxy-δ6-6-methyl-19-norprogesterone * Osaterone acetate (TZP-4238) = 17α-acetoxy-6-chloro-2-oxa-δ6-progesterone Testosterone derivatives * Abiraterone (CB-7598) = 17-(3-pyridinyl)androsta-5,16-dien-3β-ol * Abiraterone acetate = 17-(3-pyridinyl)androsta-5,16-dien-3β-ol acetate * Benorterone (SKF-7690, FC-612) = 17α-methyl-''B''-nortestosterone * BOMT ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cyproterone Acetate
Cyproterone acetate (CPA), sold alone under the brand name Androcur or with ethinylestradiol under the brand names Diane or Diane-35 among others, is an antiandrogen and progestin medication used in the treatment of androgen-dependent conditions such as acne, excessive body hair growth, early puberty, and prostate cancer, as a component of feminizing hormone therapy for transgender women, and in birth control pills. It is formulated and used both alone and in combination with an estrogen. CPA is taken by mouth one to three times per day. Common side effects of high-dose CPA in men include gynecomastia (breast development) and feminization. In both men and women, possible side effects of CPA include low sex hormone levels, reversible infertility, sexual dysfunction, fatigue, depression, weight gain, and elevated liver enzymes. At very high doses in older individuals, significant cardiovascular complications can occur. Rare but serious adverse reactions of CPA ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Delanterone
Delanterone () (developmental code name GBR-21162), also known as 1α-methylandrosta-4,16-dien-3-one, is a steroidal antiandrogen described as an anti-acne agent which was never marketed. The compound showed poor efficacy as an antiandrogen ''in vivo'' in animals, suggestive of low activity or a short terminal half-life, and likely in relation to this was not further developed. It was described and characterized in the literature in 1977. See also * Steroidal antiandrogen A steroidal antiandrogen (SAA) is an antiandrogen with a steroidal chemical structure. They are typically antagonists of the androgen receptor (AR) and act both by blocking the effects of androgens like testosterone and dihydrotestosterone (DH ... * List of steroidal antiandrogens References Androstanes Anti-acne preparations Cyclopentenes Steroidal antiandrogens {{dermatologic-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Canrenone
Canrenone, sold under the brand names Contaren, Luvion, Phanurane, and Spiroletan, is a steroidal antimineralocorticoid of the spirolactone group related to spironolactone which is used as a diuretic in Europe, including in Italy and Belgium. It is also an important active metabolite of spironolactone, and partially accounts for its therapeutic effects. Medical uses Canrenone is mainly used as a diuretic. Canrenone has been found to be effective in the treatment of hirsutism in women. Heart failure Two studies of canrenone in people with heart failure have shown a mortality benefit compared to placebo. In the evaluation which studied people with chronic heart failure (CHF), people that were treated with canrenone displayed a lower number of deaths compared to the placebo group, indicating a death and morbidity benefit of the medication. One study compared 166 treated with canrenone to 336 given conventional therapy lasting 10 years. Differences in systolic and diastolic blo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SC-8109
SC-8109 is a steroidal antimineralocorticoid of the spirolactone group which was never marketed. It is a potent antagonist of the mineralocorticoid receptor and is more potent than the related drug SC-5233 (of which SC-8109 is the 19-nor analogue). However, SC-8109 was found to have relatively low oral bioavailability and potency, though it nonetheless produced a mild diuretic effect in patients with congestive heart failure. Spironolactone (SC-9420; Aldactone), another spirolactone, followed and had both good oral bioavailability and potency, and was the first antimineralocorticoid to be marketed. In addition to its antimineralocorticoid activity, SC-8109 shows potent progestogenic activity, with similar potency relative to that of progesterone. Its analogue, SC-5233, possesses similar but less potent progestogenic activity. In addition, SC-5233 has been assessed and found to possess some antiandrogenic activity, antagonizing the effects of testosterone in animals, and SC-8109 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SC-5233
SC-5233, also known as 6,7-dihydrocanrenone or 20-spirox-4-ene-3,20-dione, is a synthetic, steroidal antimineralocorticoid of the spirolactone group which was developed by G. D. Searle & Company in the 1950s but was never marketed. It was the first synthetic antagonist of the mineralocorticoid receptor to have been identified and tested in humans. The drug was found to lack appreciable oral bioavailability and to be of low potency when administered parenterally, but it nonetheless produced a mild diuretic effect in patients with congestive heart failure. SC-8109, the 19-nor (19-demethyl) analogue, was developed and found to have improved oral bioavailability and potency, but still had low potency. Spironolactone (SC-9420; Aldactone) followed and had both good oral bioavailability and potency, and was the first synthetic antimineralocorticoid to be marketed. It has about 46-fold higher oral potency than SC-5233. SC-5233 is the propionic acid lactone of testosterone (androst-4 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Zanoterone
Zanoterone (, ) (former developmental code name WIN-49596), also known as (5α,17α)-1'-(methylsulfonyl)-1'-H-pregn-20-yno,2-cyrazol-17-ol, is a steroidal antiandrogen which was never marketed. It was investigated for the treatment of benign prostatic hyperplasia (BPH) but failed to demonstrate sufficient efficacy in phase II clinical trials, and also showed an unacceptable incidence rate and severity of side effects (e.g., breast pain and gynecomastia). As such, it was not further developed. Zanoterone was derived from 5α-dihydroethisterone (5α-dihydro-17α-ethynyltestosterone). It is an antagonist of the androgen receptor (Ki = 2.2 μM; compared to metribolone = 2.2%), and with the exception of antiprogestogenic activity in rat and rabbit models, is devoid of other hormonal activities. Zanoterone does not inhibit 5α-reductase, aromatase, or 3α- or 3β-hydroxysteroid dehydrogenase ''in vitro''. The drug significantly increases testosterone and estradiol levels in m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Trimethyltrienolone
Trimethyltrienolone (TMT), also known by its developmental code name R-2956 or RU-2956, is an antiandrogen medication which was never introduced for medical use but has been used in scientific research. Side effects Due to its close relation to metribolone (methyltrienolone), it is thought that TMT may produce hepatotoxicity. Pharmacology Pharmacodynamics TMT is a selective and highly potent competitive antagonist of the androgen receptor (AR) with very low intrinsic/ partial androgenic activity and no estrogenic, antiestrogenic, progestogenic, or antimineralocorticoid activity. The drug is a derivative of the extremely potent androgen/anabolic steroid metribolone (R-1881; 17α-methyltrenbolone), and has been reported to possess only about 4-fold lower affinity for the AR in comparison. In accordance, it has relatively high affinity for the AR among steroidal antiandrogens, and almost completely inhibits dihydrotestosterone (DHT) binding to the AR ''in vitro'' at a mere 10 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Topterone
Topterone (, ) (developmental code name WIN-17665), also known as 17α-propyltestosterone (or simply propyltestosterone) or as 17α-propylandrost-4-en-17β-ol-3-one, is a steroidal antiandrogen that was first reported in 1978 and was developed for topical administration but, due to poor effectiveness, was never marketed. See also * Steroidal antiandrogen * List of steroidal antiandrogens This is a list of steroidal antiandrogens. Progesterone derivatives * 11α-Hydroxyprogesterone = 11α-hydroxyprogesterone * Chlormadinone acetate = 17α-acetoxy-6-chloro-δ6-progesterone * Clometerone (L-38000) = 6α-chloro-16α-methylproges ... References Abandoned drugs Androstanes Anti-acne preparations Steroidal antiandrogens {{Dermatologic-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Rosterolone
Rosterolone () (developmental code name SH-434), also known as 17α-propylmesterolone or 1α-methyl-17α-propyl-5α-androstan-17β-ol-3-one, is a steroidal antiandrogen which was first described in 1984 and was developed for topical administration but was never marketed. It has shown some efficacy in the treatment of acne, and lacks systemic effects with either topical or systemic administration. Rosterolone is a derivative of mesterolone, which, in contrast, is an androgen and anabolic steroid. See also * Steroidal antiandrogen -chemical * List of steroidal antiandrogens This is a list of steroidal antiandrogens. Progesterone derivatives * 11α-Hydroxyprogesterone = 11α-hydroxyprogesterone * Chlormadinone acetate = 17α-acetoxy-6-chloro-δ6-progesterone * Clometerone (L-38000) = 6α-chloro-16α-methylproges ... References Abandoned drugs Androstanes Anti-acne preparations Steroidal antiandrogens {{dermatologic-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oxendolone
Oxendolone, sold under the brand names Prostetin and Roxenone, is an antiandrogen and progestin medication which is used in Japan in the treatment of enlarged prostate. However, this use is controversial due to concerns about its clinical efficacy. Oxendolone is not effective by mouth and must be given by injection into muscle. Oxendolone is an antiandrogen, and hence is an antagonist of the androgen receptor, the biological target of androgens like testosterone and dihydrotestosterone. It is also a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone. Due to its progestogenic activity, oxendolone has antigonadotropic effects. Oxendolone has no other important hormonal activity... Oxendolone was introduced for medical use in 1981. It is used only in Japan. Medical uses Oxendolone is used in the treatment of benign prostatic hyperplasia (BPH) in Japan. It has been used at a dos ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mifepristone
Mifepristone, also known as RU-486, is a medication typically used in combination with misoprostol to bring about a medical abortion during pregnancy and manage early miscarriage. This combination is 97% effective during the first 63 days of pregnancy. It is also effective in the second trimester of pregnancy. Effectiveness should be verified two weeks after use. It is taken by mouth. Common side effects include abdominal pain, feeling tired, and vaginal bleeding. Serious side effects may include heavy vaginal bleeding, bacterial infection, and birth defects if the pregnancy does not end. If used, appropriate follow up care needs to be available. Mifepristone is an antiprogestogen. It works by blocking the effects of progesterone, making both the cervix and uterine vessels dilate and causing uterine contraction. Mifepristone was developed in 1980 and came into use in France in 1987. It became available in the United States in 2000. It is on the World Health Organization' ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Metogest
Metogest (INN, USAN) (developmental code name SC-14207), also known as 16,16-dimethyl-19-nortestosterone, is a steroidal antiandrogen that was patented in 1975 and investigated as a treatment for acne but was never marketed. See also * Steroidal antiandrogen * List of steroidal antiandrogens This is a list of steroidal antiandrogens. Progesterone derivatives * 11α-Hydroxyprogesterone = 11α-hydroxyprogesterone * Chlormadinone acetate = 17α-acetoxy-6-chloro-δ6-progesterone * Clometerone (L-38000) = 6α-chloro-16α-methylproges ... References Anti-acne preparations Estranes Steroidal antiandrogens {{dermatologic-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
