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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 individuals ...
Relative to steroidal antiandrogens like cyproterone acetate and spironolactone, bicalutamide has better selectivity in its action, superior efficacy as an antagonist of the androgen receptor, and better tolerability. Bicalutamide also shows a better safety profile than cyproterone acetate.
Androgen receptor antagonistic potency of spironolactone, cyproterone acetate, and flutamide in castrated male rats treated with exogenous testosterone (as measured by inhibition of androgen-dependent ventral prostate weight). [27] Spironolactone is an antagonist of the AR, the biological target of androgens like testosterone and DHT.
Spironolactone is considered to be a first-line treatment for hirsutism, finasteride and the steroidal antiandrogen cyproterone acetate are considered to be second-line treatments, and flutamide is no longer recommended for hirsutism due to liver toxicity concerns. [68]
1967: Cyproterone acetate was first studied clinically, to treat sexual deviance in men [225] 1969: Cyproterone acetate was first studied in the treatment of acne, hirsutism, seborrhea, and scalp hair loss in women [226] 1969: The antiandrogenic activity of spironolactone is discovered [227]
Testosterone, the major endogenous androgen and the target mediator of antiandrogens.. This is a list of antiandrogens, [1] or drugs that prevent the effects of androgens like testosterone and dihydrotestosterone (DHT). [2]
A steroidal antiandrogen (SAA) is an antiandrogen with a steroidal chemical structure. [1] [2] [3] They are typically antagonists of the androgen receptor (AR) and act both by blocking the effects of androgens like testosterone and dihydrotestosterone (DHT) and by suppressing gonadal androgen production.
Cyproterone, also known by its developmental code name SH-80881, is a steroidal antiandrogen which was studied in the 1960s and 1970s but was never introduced for medical use. [ 1 ] [ 2 ] [ 3 ] It is a precursor of cyproterone acetate (CPA), an antiandrogen, progestin , and antigonadotropin which was introduced instead of cyproterone and is ...