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vepafestinib
- Development stage
- Phase 2
- Lead developer
- Taiho Pharmaceutical
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Vepafestinib (TAS0953/HM06) is a next-generation, orally bioavailable, selective inhibitor of the proto-oncogene receptor tyrosine kinase rearranged during transfection (RET). It targets wild-type RET as well as fusion products and mutated forms associated with oncogenic driver alterations. Vepafestinib is designed to overcome resistance mutations in RET, including the G810 mutation, and demonstrates superior brain penetration compared to first-generation selective RET inhibitors. Its primary indications are advanced or metastatic non-small cell lung cancer (NSCLC), papillary thyroid cancer, medullary thyroid cancer, and other solid tumors harboring RET gene abnormalities. The drug is currently being evaluated in phase 1/2 clinical trials for patients with advanced solid tumors with RET gene abnormalities[1][2][5][6][7].
- Brand names
- vepafestinib
- Other names
- RET inhibitor TAS0953/HM06
02
Targets
RET (Rearranged during transfection receptor tyrosine kinase)
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