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Mesutoclax (ABBV-167) is an investigational, potent, and selective small molecule inhibitor of B-cell lymphoma 2 (BCL-2), an anti-apoptotic protein frequently overexpressed in various hematologic malignancies. Developed by AbbVie, mesutoclax is designed to induce apoptosis in cancer cells by selectively binding to the BH3-binding groove of BCL-2, thereby preventing it from sequestering pro-apoptotic proteins such as BIM and BAX. This mechanism effectively lowers the threshold for programmed cell death in malignant cells. Mesutoclax is currently being evaluated in Phase 1 clinical trials for the treatment of acute myeloid leukemia (AML), multiple myeloma (MM), and myelodysplastic syndromes (MDS). While it shares a similar mechanism of action with the first-in-class BCL-2 inhibitor venetoclax, mesutoclax is a chemically distinct entity being explored for its specific pharmacokinetic profile and potential efficacy in combination regimens.
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