Pharmacological Basis for Clinical Use of Antiandrogens

    F. Neumann
    TLDR Cyproterone acetate is used to treat conditions like prostate cancer, early puberty, excessive sexual drive, and female androgenization by blocking male sex hormones.
    Cyproterone acetate (CPA), discovered in the early 1960s, was the first clinically significant antiandrogen. It affected all androgen target organs and functions, including inhibiting accessory sexual gland function, spermatogenesis, libido, puberty onset, bone maturation, sebaceous gland function, and male sexual differentiation. CPA also had progestogenic effects, inhibiting gonadotrophin secretion, which was particularly useful in treating dermatological disorders in women. While CPA exhibited glucocorticoid-like properties in animals, these effects were only observed in children with high-dose therapy for precocious puberty and not in adults. Proven clinical uses for CPA included treating prostatic carcinoma, precocious puberty, hypersexuality, sexual deviations, and androgenization in women (e.g., hirsutism, acne, seborrhoea oleosa, and androgenetic alopecia).
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