髓系白血病
医学
白血病
阿布勒
癌症研究
酪氨酸激酶
内科学
受体
作者
Timothy P. Hughes,Michael J. Mauro,Jorge E. Cortés,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 J.W.M. Janssen,François-Xavier Mahon,Yosuke Minami,David T Yeung,David M. Ross
标识
DOI:10.1056/nejmoa1902328
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.
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