opevesostat + carbamazepine

This is a **combination of opevesostat (MK-5684)**, a selective, oral inhibitor of **CYP11A1** being developed primarily for the treatment of metastatic castration-resistant prostate cancer (mCRPC), and **carbamazepine**, an established small molecule anticonvulsant used for epilepsy, trigeminal neuralgia, and bipolar disorder. Opevesostat acts by inhibiting the first rate-limiting step in steroid hormone biosynthesis, impacting androgen synthesis in hormone-driven malignancies. Carbamazepine is a sodium channel blocker and a strong inducer of CYP3A4, which can significantly alter the pharmacokinetics of co-administered drugs like opevesostat through enzyme induction. This combination does not represent a marketed therapy but has been tested in drug-drug interaction (DDI) studies to investigate mutual metabolic effects and pharmacokinetics in healthy volunteers.

Brand names

Tegretol XR (for carbamazepine)