zipalertinib + pimitespib

TAS6417 + TAS-116 is a combination therapy being developed by Taiho Pharmaceutical for the treatment of non-small cell lung cancer (NSCLC). The combination consists of zipalertinib (TAS6417), a potent and irreversible small molecule inhibitor of the epidermal growth factor receptor (EGFR) that specifically targets exon 20 insertion mutations, and pimitespib (TAS-116), an oral selective inhibitor of heat shock protein 90 (HSP90) α and β. HSP90 is a molecular chaperone that stabilizes various oncogenic proteins, including mutated EGFR. By inhibiting HSP90, pimitespib induces the degradation of these client proteins, which may enhance the efficacy of zipalertinib and help overcome resistance in EGFR-mutant lung cancers. The combination is currently undergoing Phase 1 clinical evaluation.

Other names

TAS6417 + TAS-116zipalertinib + pimitespibCLN-081 + TAS-116