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 酶的新型双抑制剂。IDH1和IDH2的突变被认为是某些血液学恶性肿瘤、神经胶质瘤和实体瘤的驱动因素,在急性髓细胞白血病患者中尤其如此。尽管某些IDH抑制剂已在某些市场获准用于急性髓细胞白血病,但细胞质突变体IDH1和线粒体突变体IDH2之间的异构体切换通常会导致对IDH1或IDH2单一抑制剂产生获得性耐药性。通过克服这种获得性耐药性,同时靶向IDH1和IDH2突变可以为癌症患者提供治疗益处。