Acerand Therapeutics has initiated dosing of the first patient in its first-in-human Phase I clinical trial of ACE-232, a novel oral inhibitor of CYP11A1, for patients with metastatic castration-resistant prostate cancer (mCRPC). The trial (NCT06801236) represents a significant milestone for the clinical-stage biotech company, marking its first clinical study in the United States.
Trial Design and Objectives
The multicenter Phase I study is being conducted in both the United States and China, comprising two distinct phases: a dose-escalation phase (Phase IA) and a dose-optimization phase (Phase IB). The primary objectives are to evaluate the safety, tolerability, pharmacokinetics (PK), pharmacodynamics (PD), as well as preliminary clinical activity of ACE-232, and to determine the recommended Phase II dose (RP2D).
Professor Emmanuel Antonarakis, Director of Genitourinary Oncology at Masonic Cancer Center, University of Minnesota, is serving as the global coordinating Principal Investigator for the study. "I would like to congratulate the Acerand team, the research staff, and the first patient for helping us to reach this important milestone," says Dr. Antonarakis.
Preclinical Performance and Differentiation
Preclinical data demonstrated that ACE-232 possesses superior potency, efficacy, and pharmacokinetic properties compared to other investigational CYP11A1 inhibitors, including MK-5684 (Opevesostat, formerly known as ODM-208). The compound exhibited a flat PK curve and long half-life profile, along with excellent tolerability in preclinical models, presenting a wide therapeutic window for clinical development.
Mechanism of Action
ACE-232 is a highly potent and selective small-molecule inhibitor of CYP11A1, a key adrenal enzyme involved in the first and rate-limiting step of steroid hormone biosynthesis. By targeting CYP11A1, ACE-232 aims to suppress the production of androgens and other steroid hormones, offering a novel therapeutic mechanism for the treatment of androgen-dependent prostate cancer, including cases resistant to enzalutamide or abiraterone.
Strategic Significance
The initiation of this trial highlights Acerand's strategic commitment to the global development of innovative cancer therapies that address major unmet medical needs. The company, which maintains research and development hubs in Shanghai, China, and Indianapolis, USA, leverages its proprietary innovation platform and operational efficiency to deliver a highly differentiated pipeline of drug candidates from discovery to clinical trials.
