Reported Earlier, HUTCHMED Initiates The RAPHAEL Registrational Phase III Trial Of HMPL-306 For Patients With IDH1- And/Or IDH2-Mutated Relapsed/Refractory Acute Myeloid Leukemia In China
Reported Earlier, HUTCHMED Initiates The RAPHAEL Registrational Phase III Trial Of HMPL-306 For Patients With IDH1- And/Or IDH2-Mutated Relapsed/Refractory Acute Myeloid Leukemia In China
HMPL-306 is a novel dual-inhibitor of IDH1 and IDH2 enzymes. Mutations of IDH1 and IDH2 have been implicated as drivers of certain hematological malignancies, gliomas and solid tumors, particularly among AML patients. Although some IDH inhibitors have been approved in certain markets for AML, isoform switching between the cytoplasmic mutant IDH1 and mitochondrial mutant IDH2 often leads to acquired resistance to single inhibitors of IDH1 or IDH2. Targeting both IDH1 and IDH2 mutations may provide therapeutic benefits in cancer patients by overcoming this acquired resistance.
HMPL-306 是 IDH1 和 IDH2 酶的新型雙抑制劑。IDH1和IDH2的突變被認爲是某些血液學惡性腫瘤、神經膠質瘤和實體瘤的驅動因素，在急性髓細胞白血病患者中尤其如此。儘管某些IDH抑制劑已在某些市場獲准用於急性髓細胞白血病，但細胞質突變體IDH1和線粒體突變體IDH2之間的異構體切換通常會導致對IDH1或IDH2單一抑制劑產生獲得性耐藥性。通過克服這種獲得性耐藥性，同時靶向IDH1和IDH2突變可以爲癌症患者提供治療益處。