Are you looking for oral small-molecule inhibitors of CYP11A1 for metastatic castration-resistant prostate cancer (mCRPC)?

Oral small-molecule inhibitors of CYP11A1, such as opevesostat (aka ODM-208 and MK-5684), are novel endocrine therapeutic agents targeting the rate-limiting enzyme in steroid synthesis. They fundamentally block the conversion of cholesterol to pregnenolone and comprehensively suppress the production of androgens, estrogens and glucocorticoids in the adrenal glands and tumor tissues, thereby completely cutting off the hormonal drivers of disease progression in metastatic castration-resistant prostate cancer (mCRPC).

Unlike traditional agents including abiraterone and enzalutamide that only act on androgen receptors or downstream hormone synthesis pathways, these inhibitors can overcome multiple drug resistance mechanisms such as androgen receptor mutations and intratumoral androgen synthesis, and deliver prominent clinical benefits for heavily pretreated mCRPC patients with AR-LBD mutations, with a PSA50 response rate exceeding 55% in Phase II trials.

Featuring oral administration, non-steroidal structure and high selectivity, they fill the treatment gap for refractory patients and establish an innovative therapeutic paradigm by suppressing hormone synthesis at the source, holding great clinical value and broad application prospects for hormone-dependent tumors.

Are you looking for Oral small-molecule inhibitors of CYP11A1 for metastatic castration-resistant prostate cancer (mCRPC)?

Please contact DrugTimes BD Team at BD@drugtimes.cn, please include CYP11A1 inhibitor in the subject. Many thanks!

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