Abiraterone acetate, a novel adrenal inhibitor in metastatic castration-resistant prostate cancer

Curr Oncol Rep. 2011 Apr;13(2):92-6. doi: 10.1007/s11912-011-0153-4.


The androgen receptor remains the key player in patients with castration-resistant prostate cancer (CRPC). Available agents capable of blocking early adrenal androgen production have limited activity and can lead to significant toxicities. Abiraterone acetate, a pregnenolone analog, is a small molecule that irreversibly inhibits CYP17, a rate-limiting enzyme in androgen biosynthesis. Several clinical trials have demonstrated the safety and efficacy of this compound in men with metastatic CRPC. Recently, a randomized phase 3 trial evaluating abiraterone acetate in docetaxel-refractory CRPC patients demonstrated a survival improvement over placebo-treated patients (14.8 vs 10.9 months; HR 0.646; P < 0.0001). A similar trial in the pre-chemotherapy setting has completed accrual and is undergoing analysis. Here we review the rationale and clinical development of abiraterone acetate in men with CRPC.

Publication types

  • Review

MeSH terms

  • Adrenal Glands / drug effects*
  • Adrenal Glands / metabolism
  • Androgen Antagonists / therapeutic use
  • Androgens / biosynthesis
  • Androstenes
  • Androstenols / therapeutic use*
  • Antineoplastic Agents / therapeutic use
  • Clinical Trials, Phase III as Topic
  • Humans
  • Male
  • Orchiectomy
  • Prostatic Neoplasms / drug therapy*
  • Prostatic Neoplasms / metabolism
  • Prostatic Neoplasms / surgery
  • Randomized Controlled Trials as Topic
  • Steroid 17-alpha-Hydroxylase / antagonists & inhibitors


  • Androgen Antagonists
  • Androgens
  • Androstenes
  • Androstenols
  • Antineoplastic Agents
  • Steroid 17-alpha-Hydroxylase
  • abiraterone