Chemistry:Opevesostat
Opevesostat is an investigational new drug being developed for the treatment of metastatic castration-resistant prostate cancer (mCRPC).[1] It is a steroidogenesis inhibitor, selectively targeting CYP11A1 (cholesterol side-chain cleavage enzyme)[2][3] discovered by Orion Corporation and currently undergoing clinical development by Merck & Co., Inc. Opevesostat's mechanism of action involves suppressing the production of steroid hormones and their precursors that may activate the androgen receptor signaling pathway, which is crucial in prostate cancer progression. As of 2024, opevesostat is being evaluated in two Phase 3 clinical trials, OMAHA-003[4] and OMAHA-004[5] which are assessing its efficacy and safety in combination with hormone replacement therapy for patients with mCRPC who have failed prior treatments.[6][7][8]
References
- ↑ "Opevesostat - Orion". AdisInsight. Springer Nature Switzerland AG. https://adisinsight.springer.com/drugs/800050472.
- ↑ "Steroidogenic cytochrome P450 enzymes as drug target". Toxicological Research 40 (3): 325–333. July 2024. doi:10.1007/s43188-024-00237-0. PMID 38911541. Bibcode: 2024ToxRe..40..325K.
- ↑ "Steroidogenesis inhibitor opevesostat (MK-5684) for metastatic castration-resistant prostate cancer: OMAHA-003 and OMAHA-004 trial designs". Future Oncology: 1–8. February 2026. doi:10.1080/14796694.2025.2595914. PMID 41732008.
- ↑ Clinical trial number NCT06136624 for "A Phase 3 Randomized, Open-label Study of MK-5684 Versus Alternative Abiraterone Acetate or Enzalutamide in Participants With Metastatic Castration-resistant Prostate Cancer (mCRPC) Previously Treated With Next-generation Hormonal Agent (NHA) and Taxane-based Chemotherapy (OMAHA-003)" at ClinicalTrials.gov
- ↑ Clinical trial number NCT06136650 for "MK-5684-004: A Phase 3, Randomized, Open-label Study of Opevesostat Versus Alternative Abiraterone Acetate or Enzalutamide in Participants With Metastatic Castration-resistant Prostate Cancer (mCRPC) That Progressed On or After Prior Treatment With One Next-generation Hormonal Agent (NHA) (OMAHA-004)" at ClinicalTrials.gov
- ↑ "Merck and Orion Announce Mutual Exercise of Option Providing Merck Global Exclusive Rights to Opevesostat". July 2024. https://www.stocktitan.net/news/MRK/merck-and-orion-announce-mutual-exercise-of-option-providing-merck-9zanb1tr0six.html.
- ↑ "Inside Information: Orion and MSD Announce Mutual Exercise of Option Providing MSD Global Exclusive Rights to Opevesostat". https://www.orion.fi/en/newsroom/all-news/releases/stock-releases/2024/inside-information-orion-and-msd-announce-mutual-exercise-of-option-providing-msd-global-exclusive-rights-to-opevesostat-an-investigational-cyp11a1-inhibitor-for-the-treatment-of-metastatic-castration-resistant-prostate-cancer/.
- ↑ "Merck and Orion Announce Mutual Exercise of Option Providing Merck Global Exclusive Rights to Opevesostat". https://www.merck.com/news/merck-and-orion-announce-mutual-exercise-of-option-providing-merck-global-exclusive-rights-to-opevesostat-an-investigational-cyp11a1-inhibitor-for-the-treatment-of-metastatic-castration-resistant-pr/.
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