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API Female Sex Cyproterone Acetate Cyproterone¹

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Product Description API Female Sex Cyproterone Acetate CyproteroneProduct DescriptionProduct DetailsProduct NameCyproteroneApperanceWhite PowderCAS2098-66-0MFC22H27ClO3MW374.9Cyproterone acetate (CPA), identified by CAS registry number 2098-66-0, is a synthetic steroidal antiandrogen and progestogen derived from 17α-hydroxyprogesterone. Its molecular formula is C22H27ClO3, with a molecular weight of 416.94 g/mol. Structurally, it features a 1,2α-methylene substitution on the progesterone skeleton and a atom at position C6, along with a 17α-acetoxy group critical for its progestogenic activity. CPA typically presents as a white to slightly yellowish crystalline powder, exhibiting polymorphism. It is practically insoluble in water but demonstrates good solubility in organic solvents such as ethanol and dimethyl sulfoxide (DMSO), reflecting its high lipophilicity. The compound is highly stable under standard storage conditions (room temperature, protected from light and moisture), though it may degrade under strong UV exposure or extreme pH. Synthesized through multi-step chemical modification of steroid intermediates, CPA is characterized by its dual pharmacological actions: potent competitive inhibition of androgen receptors (AR) and strong progestogenic activity via progesterone receptor (PR) agonism. This dual functionality underpins its unique endocrine profile, distinguishing it from non-steroidal antiandrogens. Its pharmacokinetics include high oral bioavailability due to lipophilicity, extensive hepatic metabolism (primarily via CYP3A4 hydroxylation and conjugation), and a prolonged terminal half-life of approximately 38–46 hours. A critical feature is its ability to suppress secretion (LH/FSH) via negative feedback at the hypothalamic-pituitary axis, leading to reduced testicular synthesis.Application&FunctionCyproterone acetate functions primarily as a potent antiandrogen and progestogen, exerting its effects through two complementary mechanisms: competitive blockade of androgen receptors in target tissues (e.g., prostate, skin, hair follicles) and central suppression of production via inhibition of release. By binding to AR with high affinity, CPA prevents dihydro (DHT) and from activating androgen-responsive genes, inhibiting cell proliferation and androgen-dependent processes. Concurrently, its progestogenic action on the pituitary suppresses (LH) secretion, reducing testicular Leydig cell stimulation and systemic levels by up to 70–80%. This dual suppression makes CPA exceptionally effective in managing androgen-dependent conditions. Its primary clinical application is in the treatment of advanced prostate cancer, where it is used as palliative therapy (often combined with a analogue or estrogen) to reduce tumor growth and alleviate symptoms. CPA is also extensively prescribed for severe androgenization in women, including androgenetic alopecia, moderate-to-severe hirsutism, and acne vulgaris resistant to conventional treatments, typically administered in combination with ethinyl estradiol in oral contraceptives (e.g., Diane-35, co-cyprindiol). Furthermore, it is a cornerstone of feminizing hormone therapy for transgender women, reducing androgen effects (body hair, scalp hair loss) while supporting estrogen-mediated feminization. Off-label uses include managing paraphilias and hypersexuality through libido reduction. Key safety considerations include dose-dependent hepatotoxicity (including rare hepatitis and liver tumors), increased thrombotic risk, depression, adrenal suppression, and potential bone mineral density loss with long-term use. It is available in oral tablets (50–100 mg) and compounded formulations, with therapy requiring regular monitoring of liver function, electrolytes, and hematological parameters.Specification

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