Shanghai (China) and Indianapolis (US), Jan. 10th, 2025 – Acerand Therapeutics is pleased to announce that on January 10 of 2025, the U.S. Food and Drug Administration (FDA) granted approval for the first-in-human, open-label, multi-center Phase I study of its novel CYP11A1 inhibitor, ACE-232.

ACE-232 is a novel, orally active, and highly selective inhibitor of CYP11A1 developed to target both localized or metastatic hormone-sensitive or castration-resistant prostate cancer. It can effectively overcome acquired resistance to androgen receptor pathway inhibitors (ARPI, abiretarone or enzalutamide) due to AR-LBD mutations or amplification. Preclinical studies have shown that ACE-232 exhibits excellent in vitro and in vivo potency, and a favorable pharmacokinetic and safety profile, with best-in-class potential. Based on these promising results, Acerand Therapeutics will promptly launch a Phase 1 study in the U.S. to further evaluate the potential of ACE-232 as both a monotherapy and combination therapy.

Remarks by Dr. Genshi Zhao, Acerand Co-Founder, President and CSO:

We are excited to announce that the FDA has approved the clinical trial application for our CYP11A1 inhibitor, ACE-232. As we know, prostate cancer is one of the leading causes of cancer-related morbidity and mortality worldwide in men. While prostate cancer initially responds to androgen deprivation therapy (ADT), progression eventually occurs, leading to the development of metastatic castration-resistant prostate cancer (mCRPC), a terminal stage of the disease. Effectively managing prostate cancer from its early non-metastatic, hormone-sensitive stage to the advanced metastatic, castration-resistant stage remains a significant challenge. With ACE-232’s outstanding preclinical properties, we are highly confident that ACE-232 will provide a new, effective therapeutic option, with the potential to treat the entire spectrum of androgen-dependent prostate cancers, delivering significant clinical benefits to patients.