Bafetinib
Bafetinib (NS-187) is an experimental cancer drug developed by Nippon Shinyaku and licensed to CytRx. It is an inhibitor of Lyn and Bcr-Abl. It reached phase II clinical trials in 2010. Development Imatinib was the first Bcr-Abl tyrosine-kinase inhibitor and was highly successful in treatment of chronic myelogenous leukemia, which had previous had no effective treatment. With the emerging resistance to imatinib treatment, alternative treatment was highly sought after. Bafetinib was created as an attempt for a more potent drug than imatinib, with efficacy against various point mutations in the Bcr-Abl kinase, with fewer adverse effects and with narrower kinase spectra, namely just Lyn and Bcr-Abl. In the search for a substance that fit the criteria mentioned, the crystal structure of imatinib bound to Abl was examined. This revealed a hydrophobic pocket around the phenyl ring adjacent to the piperazinylmethyl group of imatinib. Attempts to utilize this pocket to increase effi ...
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