Androgen biosynthesis inhibitors
ATC code: L02BX03 (Abiraterone)
Brand names
Zytiga, Yonsa, Abiraterona Glenmark, Abiraterona Sandoz, Abiraterona Normon
Selective irreversible inhibitor of CYP17, the enzyme key to androgen biosynthesis in the adrenals, testes, and prostate tumor tissue. Blocks 17α-hydroxylase and C17,20-lyase. Lowers testosterone and DHEA below castration levels, overcoming hormonal therapy resistance in metastatic prostate cancer previously considered inoperable. Used only in combination with prednisolone to suppress compensatory ACTH rise and mineralocorticoid side effects.
First line
Metastatic castration-resistant prostate cancer (mCRPC) and metastatic hormone-sensitive (mHSPC) per ESMO 2024 and Spanish SEOM 2023. In mHSPC used as first-line with androgen deprivation (LATITUDE, NEJM 2017 showed 16.8-month median overall survival increase). Dose 1000 mg (4×250 mg tablets) once daily on empty stomach + 5 mg 1-2 times daily. Alternative – enzalutamide or apalutamide (docetaxel for visceral metastases).
The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.
Not recommended
Abiraterone is used by amateur AAS cyclers for total endogenous-androgen blockade. NCCN 2024 and the AEMPS Ficha Técnica confine abiraterone to metastatic castration-resistant and metastatic hormone-sensitive prostate cancer with prednisone. Approved athlete indications do not exist. Use without concomitant glucocorticoid causes mineralocorticoid syndrome, hypokalemia, edema and hypertension.
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Male use only. Contraindicated in women. Female partners of male patients with reproductive potential use barrier contraception throughout therapy and 3 weeks after.
Not used in women.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Abiraterone is evaluated for the following indications with varying evidence strength: Prostate cancer (evidence tier A), Athletic endurance (evidence tier F). See the full indication matrix with dosing and citations above on this page.
Common side effects of Abiraterone (≥ 1 in 100): Hypertension, Hypokalemia, Peripheral edema, Fatigue, ALT/AST elevation, Joint pain. See the Safety section for uncommon and serious reactions.
FDA category X. Male use only. Contraindicated in women. Female partners of male patients with reproductive potential use barrier contraception throughout therapy and 3 weeks after.
Not used in women.
Abiraterone is contraindicated in: Hypersensitivity; Severe hepatic impairment (Child-Pugh C); Pregnant partner or conception potential without barrier contraception; Spironolactone combination. Full list in the Safety section.