OST11098 is a newly developed, orally bioavailable, and highly selective CYP11A1 inhibitor showing strong potential for the treatment of castration-resistant prostate cancer (CRPC). Resistance to next-generation hormone agents (NHAs) like abiraterone and enzalutamide remains a major clinical challenge, and OST11098 is designed to address this unmet need. By targeting CYP11A1 — an enzyme critical for the first step in steroid hormone biosynthesis — OST11098 blocks the production of pregnenolone, shutting down the androgen receptor (AR) signaling axis that fuels prostate cancer progression.

Preclinical studies demonstrate that OST11098 inhibits pregnenolone biosynthesis at low nanomolar concentrations in vitro and shows robust dose-dependent pharmacokinetics and pharmacodynamics in vivo. In CRPC xenograft mouse models, including models resistant to standard NHAs, OST11098 exhibited significant anti-tumor efficacy. Importantly, the drug also displayed a clean safety profile and favorable pharmacokinetic properties in preclinical testing.

The findings suggest that OST11098 could represent a new class of therapeutic agents capable of overcoming resistance to existing hormonal therapies in CRPC. Its strong preclinical performance supports further clinical development aimed at improving outcomes for patients facing advanced, treatment-resistant prostate cancer.

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