Bozitinib (Vebreltinib; formerly APL-101/PLB-1001, CBT-101) is a novel, an ATP-competitive, and highly selective c-MET kinase inhibitor with blood-brain barrier permeability. Bozitinib (PLB-1001) binds to the conventional ATP-binding pocket of the tyrosine kinase superfamily. It is currently under investigation in phase I/II trials as a single agent in patients with solid tumors, NSCLC, and glioblastomas, and in combination with PD-L1 inhibitors in patients with hepatocellular carcinoma and renal cell carcinoma. The drug has demonstrated anticancer effects in a variety of human xenograft tumor models with MET dysregulation and has shown promise in glioblastoma owing to its ability to cross the blood–brain barrier. The safety and preliminary efficacy of the drug have been demonstrated in a limited number of patients with chemotherapy-resistant, MET-altered gliomas. A phase II trial is evaluating bozitinib in patients with NSCLC harboring MET exon 14 skipping in China (NCT04258033).

纯度：≥98%

CAS：1440964-89-5