bafetinib

Bafetinib is a second-generation small molecule tyrosine kinase inhibitor developed for the treatment of Bcr-Abl positive leukemias and other cancers. It was rationally designed based on the structure of imatinib to improve potency and selectivity against Bcr-Abl kinase—including most imatinib-resistant mutations (except T315I)—and to target the Src family kinase Lyn. Bafetinib also inhibits Fyn kinase to some extent. The drug has demonstrated significant preclinical activity (25–55 times more potent than imatinib in vitro) and can cross the blood-brain barrier at levels sufficient for therapeutic effect in brain tumors. Clinical development has focused on chronic myeloid leukemia (CML), Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL), B-cell chronic lymphocytic leukemia (B-CLL), prostate cancer, and brain tumors such as glioblastoma multiforme. Orphan drug status was granted for CML in both the US and EU[2][4][10].

Other names

bafetinibNS-187NS187NS 187INNO-406INNO406INNO 406Lyn-IN-1Lyn-IN1Lyn-IN 1