INDIANAPOLIS — Acerand Therapeutics has announced the launch of its first clinical trial in humans for ACE-232, a novel oral CYP11A1 inhibitor designed to treat metastatic castration-resistant prostate cancer (mCRPC). The first patient has been dosed in the Phase I study, marking a major milestone for the biotech company’s global oncology program.
The trial, registered as NCT06801236, is being conducted across sites in the United States and China and is structured in two parts: a dose-escalation phase (Phase IA) and a dose-optimization phase (Phase IB). The primary goals are to assess the safety, tolerability, pharmacokinetics, and pharmacodynamics of ACE-232, as well as to identify the recommended dose for Phase II development.
Dr. Emmanuel Antonarakis, Director of Genitourinary Oncology at the Masonic Cancer Center, University of Minnesota, is leading the study as the global coordinating principal investigator. “This is an exciting and important step forward,” said Dr. Antonarakis, commending the Acerand team, trial staff, and the first patient enrolled.
Preclinical studies suggest ACE-232 offers superior potency and a favorable pharmacokinetic profile when compared to other CYP11A1 inhibitors under investigation, including Opevesostat (MK-5684). The drug has shown strong efficacy and tolerability in preclinical models, providing a promising therapeutic window for continued development.
ACE-232 works by selectively inhibiting CYP11A1, a critical enzyme in the biosynthesis of steroid hormones. By targeting this pathway, the therapy is intended to block androgen production—a key driver in advanced prostate cancer, particularly in patients resistant to existing treatments like enzalutamide or abiraterone.
This trial represents Acerand’s first clinical study in the U.S. and underscores the company’s broader strategy to develop innovative small-molecule cancer therapies that address unmet needs worldwide.
