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xevinapant
- Development stage
- Phase 3
- Lead developer
- Merck
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Xevinapant is an orally available, small-molecule inhibitor of apoptosis proteins (IAPs), acting as a mimetic of the natural second mitochondrial-derived activator of caspases (Smac). By binding to the Smac binding groove on IAPs—including X chromosome-linked IAP (XIAP) and cellular IAP1/2—xevinapant blocks their anti-apoptotic activity, thereby restoring cancer cell sensitivity to apoptosis. This mechanism enhances the effects of chemotherapy and radiotherapy by overcoming tumor cell resistance. Xevinapant also has immunomodulatory properties and may synergize with immune checkpoint inhibitors. It is under investigation primarily for locally advanced squamous cell carcinoma of the head and neck (LA SCCHN), but has also been studied in other cancers such as non-small-cell lung cancer, ovarian cancer, glioma, acute myeloid leukemia, lymphoma, solid tumors, and triple negative breast cancer[1][2][4][5][6][7].
- Brand names
- Xevinapant
- Other names
- xevinapant
02
Targets
BIRC2 (Cellular inhibitor of apoptosis protein 1)XIAP (Baculoviral IAP repeat-containing protein 4)BIRC3 (Baculoviral IAP repeat-containing protein 3)
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