The first patient was dosed in a Phase I clinical trial for ACE-232, a novel oral CYP11A1 inhibitor aimed at treating metastatic castration-resistant prostate cancer (mCRPC). The trial, registered as NCT06801236, marks the company’s first clinical study in the United States and represents a key step in its global oncology strategy.

The first-in-human study is being conducted across multiple sites in the U.S. and China, and is structured in two parts: dose escalation (Phase IA) and dose optimization (Phase IB). The trial’s main goals are to evaluate the safety, tolerability, pharmacokinetics, pharmacodynamics, and preliminary efficacy of ACE-232, ultimately determining a recommended Phase II dose. Professor Emmanuel Antonarakis, Director of Genitourinary Oncology at the Masonic Cancer Center, University of Minnesota, serves as global coordinating principal investigator.

Preclinical data suggest ACE-232 offers a superior profile compared to earlier CYP11A1 inhibitors such as MK-5684 (Opevesostat, ODM-208), demonstrating potent activity, a favorable pharmacokinetic curve, and excellent tolerability. ACE-232 works by selectively inhibiting CYP11A1, a key enzyme in the adrenal steroid hormone synthesis pathway, aiming to suppress androgen production in treatment-resistant prostate cancer.

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