HQP8361 / Merck (MSD), Ascentage Pharma - LARVOL DELTA

The novel MET inhibitor, HQP8361, possesses single agent activity and enhances therapeutic efficacy of AZD9291 (osimertinib) against AZD9291-resistant NSCLC cells with activated MET. (PubMed, Am J Cancer Res) - "HQP8361 (MK8033) is a novel and selective MET kinase inhibitor that has completed a phase I clinical trial. Moreover, the combination also very effectively inhibited the growth of HCC827/AR xenografts in nude mice. These preclinical findings support the potential of HQP8361 in the treatment of NSCLCs with MET amplification or highly activated MET and, when combined with AZD9291, in overcoming acquired resistance to EGFR-TKIs due to MET amplification."

Clinical • Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

First-in-human phase I dose escalation study of MK-8033 in patients with advanced solid tumors. (PubMed, Invest New Drugs) - "Conclusion MK-8033 was well tolerated with no significant toxicity issues, albeit with limited clinical activity. Unfortunately, the company decided to discontinue further clinical development of MK-8033."

Clinical • Journal • P1 data