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Molecular properties generated using the CDK
|No information available.|
|Summary of Clinical Use|
|Bafetinib has been assessed in two completed Phase II clinical trials for hormone-refractory prostate cancer (NCT01215799) and relapsed or refractory B-cell chronic lymphocytic leukemia (CLL; NCT01144260).
Both the US FDA and EMA have granted bafetinib orphan drug status for the treatment of Philadelphia chromosome-positive CML.
|Mechanism Of Action and Pharmacodynamic Effects|
|Bafetinib specifically binds to and inhibits the Bcr/Abl fusion protein tyrosine kinase, an abnormal enzyme produced by Philadelphia chromosomal translocation associated with chronic myeloid leukemia (CML) . It also inhibits the Src-family member Lyn tyrosine kinase, upregulated in imatinib-resistant CML cells and in a variety of solid cancer cell types . The inhibitory effect of bafetinib on these kinases may decrease cellular proliferation and induce apoptosis in tumor cells driven by their overexpression .|