Nilotinib

Abstract

Imatinib is used to treat chronic myeloid leukemia (CML), and it has now become the standard therapy. However, some patients do not respond to imatinib and this has become problematic clinically. Nilotinib (Tasigna®) is a more potent inhibitor of BCR-ABL than imatinib. Nilotinib was developed by modifying imatinib and improving its binding to BCR-ABL. It is used for the treatment of patients with CML in the chronic and accelerated phase who are resistant to, or intolerant of, imatinib. Nilotinib showed efficacy in inhibiting CML cells expressing imatinib-resistant BCR-ABL kinase mutations. However, one T315I mutation occurs most frequently and is highly resistant to nilotinib. Although nilotinib is well tolerated, it should be monitored for side effects like neutropenia, thrombocytopenia and lipase or bilirubin elevation.