Drug intelligence / Profile preview

opevesostat

Development stage
Phase 3
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

Opevesostat is an orally bioavailable, non-steroidal, selective inhibitor of cytochrome P450 side-chain cleavage enzyme (CYP11A1), developed for the treatment of metastatic castration-resistant prostate cancer (mCRPC). By inhibiting CYP11A1, it blocks the first and rate-limiting step in steroid hormone biosynthesis, preventing the synthesis of all steroid hormones and their precursors that may activate androgen receptor signaling pathways. This mechanism aims to suppress tumor growth in hormone-dependent cancers such as mCRPC, particularly in patients who have progressed after prior hormonal therapies and chemotherapy. Opevesostat is currently being evaluated in multiple Phase 3 clinical trials for mCRPC[2][3][4][6][8].

Other names
opevesostat tosilate2-(Isoindolin-2-ylmethyl)-5-[[1-(methylsulfonyl)-4-piperidyl]methoxy]-4H-pyran-4-one
02

Targets

CYP11A1 (Cholesterol side chain cleavage enzyme)

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