作者
Timothy P. Hughes,Michael J. Mauro,Jorge Cortes,Hironobu Minami,Delphine Réa,Daniel J. DeAngelo,Massimo Breccia,Yeow Tee Goh,Moshe Talpaz,Andreas Hochhaus,Philipp le Coutre,Oliver G. Ottmann,Michael C. Heinrich,Juan Luis Steegmann,Michael W. Deininger,Jeroen Janssen,François Xavier Mahon,Yosuke Minami,David T. Yeung,David M. Ross,Martin S. Tallman,Jae H. Park,Brian J. Druker,David Hynds,Yuyan Duan,Christophe Meille,Florence Hourcade‐Potelleret,K. Gary J. Vanasse,Fabian Lang,Dong Wook Kim
摘要
Asciminib is an allosteric inhibitor that binds a myristoyl site of the BCR-ABL1 protein, locking BCR-ABL1 into an inactive conformation through a mechanism distinct from those for all other ABL kinase inhibitors. Asciminib targets both native and mutated BCR-ABL1, including the gatekeeper T315I mutant. The safety and antileukemic activity of asciminib in patients with Philadelphia chromosome–positive leukemia are unknown.