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Abiraterone acetate is a hormonal treatment for metastatic prostate cancer that shuts down androgen synthesis throughout the body rather than only in the testes.
- A hormonal treatment for metastatic prostate cancer
- Shuts down androgen synthesis body wide, not only the testes
- Blocks CYP17A1, the enzyme upstream of testosterone
- Works as one moving part of a prostate cancer regimen
- Documented here so the pharmacology is on the record
- Abiraterone was designed at the Institute of Cancer Research as a mechanism-based steroidal inhibitor of CYP17A1, reported with an IC50 of about 4 nM against human testicular 17-alpha-hydroxylase [1].
- COU-AA-301 randomised 1,195 men with metastatic castration-resistant prostate cancer after docetaxel and improved median overall survival from 10.9 to 14.8 months (HR 0.65), proving that castration-resistant disease is still androgen-driven [2].
- COU-AA-302 extended the benefit to the pre-chemotherapy setting, improving radiographic progression-free survival and overall survival [3].
- LATITUDE [5] and STAMPEDE [6], published back to back in NEJM in 2017, moved abiraterone into hormone-sensitive metastatic disease: LATITUDE reduced the risk of death by 38% and STAMPEDE by 37% when abiraterone was added to androgen deprivation therapy.
- Abiraterone's efficacy is not purely CYP17 blockade: its Delta-4-abiraterone metabolite is a potent androgen receptor antagonist and also inhibits 3-beta-HSD, so the drug is effectively multi-target [4].
- Food increases abiraterone acetate exposure enormously; up to about a tenfold rise in AUC and a seventeenfold rise in Cmax with a high-fat meal; which is why the tablet must be taken on an empty stomach, one hour before or two hours after food.
Mechanism
It is a of abiraterone, an irreversible inhibitor of CYP17A1, the enzyme performing both the 17-alpha-hydroxylase and the 17,20-lyase steps of androgen synthesis in the testes, the adrenals and the tumour itself. Blocking that step backs up mineralocorticoid precursors, which is why prednisone is given alongside and why hypertension, fluid retention and low potassium are expected effects rather than surprises.
receptor fingerprint
CYP17A1 (17-alpha-hydroxylase/C17,20-lyase)Selective, mechanism-based (essentially irreversible) steroidal inhibitor
(AR, NR3C4)Direct antagonist at higher concentrations; the Delta-4-abiraterone (D4A) metabolite is a more potent AR antagonist
3-beta-hydroxysteroid dehydrogenase (HSD3B1/HSD3B2)Inhibited by abiraterone and by D4A
Esterases ( activation) and CYP3A4/SULT2A1 (clearance)Substrate
Mineralocorticoid pathway (ACTH-driven accumulation of deoxycorticosterone and corticosterone upstream of the CYP17 block)Secondary consequence of CYP17 inhibition
Safetyrisks and cautions, not medical advice
a hormonal antineoplastic that must be co-prescribed with a corticosteroid and monitored for hypertension, low potassium and liver injury
Subjective profileweighing the evidence above
Nothing about this belongs in a parcel. Abiraterone works as one moving part of a prostate cancer regimen; shutting down CYP17A1 backs up mineralocorticoid precursors, which is why a corticosteroid is prescribed alongside it and why potassium, blood pressure and liver enzymes are checked on a schedule rather than when someone feels unwell. The page exists so the pharmacology is documented; it is not a shopping entry, and no supplier is listed beside it.
Resources
No suppliers are provided for compounds like this. This entry is here for reference.
Research
- 1995first citedNovel steroidal inhibitors of human cytochrome P45017 alpha (17 alpha-hydroxylase-C17,20-lyase)…
- 2011controlled trialAbiraterone and increased survival in metastatic prostate cancer
- 2017most recentAbiraterone plus Prednisone in Metastatic, Castration-Sensitive Prostate Cancer
- 1.Novel steroidal inhibitors of human cytochrome P45017 alpha (17 alpha-hydroxylase-C17,20-lyase): potential agents for the treatment of prostatic cancer
- 2.Abiraterone and increased survival in metastatic prostate cancer
- 3.Abiraterone in metastatic prostate cancer without previous chemotherapy
- 4.Androgen receptor antagonism drives cytochrome P450 17A1 inhibitor efficacy in prostate cancer
- 5.Abiraterone plus Prednisone in Metastatic, Castration-Sensitive Prostate Cancer
- 6.Abiraterone for Prostate Cancer Not Previously Treated with Hormone Therapy
6 listed here; entry last updated August 2026
Reviews
My notesprivate to this device
Notes and cautions
- Abiraterone acetate carries no boxed warning but must always be given with prednisone or prednisolone, because blocking CYP17 raises ACTH and produces a syndrome of mineralocorticoid excess: fluid retention, hypertension and hypokalaemia, which the corticosteroid suppresses.
- Hepatotoxicity is the most serious dedicated warning; marked transaminase and bilirubin rises and rare fatal hepatic failure occur, so liver function must be checked every two weeks for the first three months and monthly thereafter, with interruption and dose reduction or permanent discontinuation for severe elevations.
- Adrenocortical insufficiency can emerge if the corticosteroid is interrupted or during intercurrent stress, infection or surgery, when increased corticosteroid cover is needed.
- Blood pressure, serum potassium and fluid status should be checked at least monthly, and caution is required in patients with a history of cardiovascular disease, since the trials excluded those with recent myocardial infarction or serious arrhythmia.
- The drug is contraindicated in pregnancy, women who are or may be pregnant should not handle uncoated tablets, and it must be taken on an empty stomach because food raises exposure severalfold.