Opevesostat — Investigational Agent
Other · Phase 3 · Merck (MSD) / originated Orion Corporation
Mechanism of Action
Oral, non-steroidal, selective inhibitor of CYP11A1, the first and rate-limiting enzyme of steroidogenesis (cholesterol side-chain cleavage). By blocking CYP11A1, opevesostat suppresses production of ALL steroid hormones — androgens (including those from adrenal and intratumoral synthesis) as well as their upstream precursors — thereby overcoming resistance driven by androgen receptor ligand-binding-domain mutations. Because it also suppresses cortisol and aldosterone, glucocorticoid (and mineralocorticoid) replacement is mandatory.
Investigational Indications
- Metastatic castration-resistant prostate cancer (mCRPC), particularly with AR ligand-binding-domain mutations