Galeterone

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable small-molecule androgen receptor modulator and CYP17 lyase inhibitor with potential antiandrogen activity. Galeterone exhibits three distinct mechanisms of action: 1) as an androgen receptor antagonist, 2) as a CYP17 lyase inhibitor and 3) by decreasing overall androgen receptor levels in prostate cancer tumors, all of which may result in a decrease in androgen-dependent growth signaling. Localized to the endoplasmic reticulum (ER), the cytochrome P450 enzyme CYP17 (P450C17 or CYP17A1) exhibits both 17alpha-hydroxylase and 17,20-lyase activities, and plays a key role in the steroidogenic pathway that produces progestins, mineralocorticoids, glucocorticoids, androgens, and estrogens.

**Synonyms:** - Androsta-5,16-dien-3-ol, 17-(1h-benzimidazol-1-yl)-, (3beta)- - GALETERONE - Specific Androgen Receptor Modulator/CYP17 Lyase Inhibitor TOK-001 - TOK 001 - TOK-001 - TOK001 - VN/124 - VN/124-1