Nilotinib-induced hyperbilirubinemia: Is it a negligible adverse event?

Posted by rob on June 26, 2009 under Uncategorized | Comments are off for this article

Chronic myelogenous leukemia (CML) is caused by rearrangement of the BCR-ABL oncogene. Imatinib inhibits the tyrosine kinase activity of the BCR-ABL protein and is an effective, frontline therapy for chronic-phase CML. However, 10–15% of patients with chronic-phase CML fail imatinib therapy because of primary or secondary resistance . The selective BCR-ABL inhibitor, nilotinib, was designed to fit into the ATP-binding site of the BCR-ABL protein with higher affinity than imatinib . In addition to being more potent than imatinib against wild-type BCR-ABL, nilotinib is significantly more active against most imatinib-resistant BCR-ABL mutants . The most common non-hematologic toxicities of nilotinib have been rash, pruritus, headache, nausea, and fatigue, with hyperbilirubinemia being a fre…