Preclinical development of HQP1351 a multikinase inhibitor targeting a broad spectrum of mutant KIT kinases for the treatment of imatinib-resistant gastrointestinal stromal tumors

摘要

BackgroundImatinib shows limited efficacy in patients with gastrointestinal stromal tumors (GISTs) carrying secondary KIT mutations. HQP1351, an orally bioavailable multikinase BCR-ABL inhibitor, is currently in clinical trials for the treatment of T315I mutant chronic myelogenous leukemia (CML), but the potential application in imatinib-resistant GISTs carrying secondary KIT mutations has not been explored.