酢酸シプロテロン

外観

白色～ほとんど白色粉末～結晶

効能

アンドロゲン受容体拮抗薬

説明

Cyproterone acetate (CPA) is an androgen receptor antagonist. It binds to human androgen receptors (K_i = 14 nM) and inhibits dihydrotestosterone-induced androgen receptor activation in CV-1 cells (IC₅₀ = 26 nM). CPA (30 mg/kg) decreases ventral prostate weight in castrated immature rats. It also suppresses accessory sexual glands and fertility in adult male rats when administered at a dose of 10 mg/kg. CPA (0.3 μM) also induces apoptosis in primary adult female rat hepatocytes. Formulations containing cyproterone acetate have been used in the treatment of androgenization in females.

化学的特性

Crystalline Solid

使用

Cyproterone acetate (CPA) has been shown to exert gestagenic and glucocorticoid effects. Because it inhibits the negative diencephalic pituitary testicular feedback system, it lowers luteinizing hormone (LH) and testosterone production and plasma levels. cyproterone acetate is both an anti-androgen and a progestogen. CPA is used in combined birth control pills, in the treatment of androgen-dependent skin and hair conditions such as acne (Combined with estrogen), seborrhea, excessive hair growth, and scalp hair loss, high androgen levels, in transgender hormone therapy, to treat prostate cancer, to reduce sex drive in sex offenders or men with paraphilias or hypersexuality, to treat early puberty, and for other uses. It is used both at low doses and at higher doses.

適応症

Cyproterone acetate is a progestational antiandrogen that blocks androgen receptor binding and suppresses androgen-sensitive tissues. It is available in a topical form in Europe for the treatment of hirsutism.