Bafetinib (formerly known as INNO-406) is an orally bioavailable, rationally designed, dual Bcr-Abl and Lyn-kinase inhibitor. According to a study published in the journal Blood (Dec. 1, 2005), bafetinib is 25 to 55 times more potent than imatinib in vitro, and at least 10 times as effective as imatinib mesylate in suppressing the growth of Bcr-Abl bearing tumors. Bafetinib has demonstrated activity in 12 of 13 imatinib-resistant cell lines.
In addition to its Bcr-Abl inhibitory properties, Bafetinib is a potent and specific inhibitor of Lyn kinase. Upregulation of Lyn kinase activity is a well recognized cause of imatinib resistance. Lyn kinase activation has also been documented in a variety of solid tumors, including prostate cancer.
