ACE-232

ACE-232 is a novel, orally active, and highly selective small molecule inhibitor of Cholesterol side chain cleavage enzyme (CYP11A1), developed by Acerand Therapeutics. Its primary mechanism is the inhibition of CYP11A1, which plays a key role in steroidogenesis. By targeting this enzyme, ACE-232 aims to overcome resistance to androgen receptor pathway inhibitors in prostate cancer—particularly in hormone-sensitive or castration-resistant forms. Preclinical studies have demonstrated potent activity and favorable pharmacokinetics and safety profiles. The drug is currently being evaluated as both monotherapy and combination therapy for prostate cancer, with its first-in-human Phase 1 clinical trial approved by the US FDA for metastatic castration-resistant prostate cancer[1][2][4][5].