Nilotinib

Nilotinib, also known as AMN107 or Tasigna, is a tyrosine kinase inhibitor. It is an analog of imatinib with similar multiple kinase targets, but without inhibition of the Src gene. This gene regulates tyrosine kinase proteins that in turn affect whether cells multiply or die. Tyrosine kinase inhibitors interfere with cell communication and growth. Nilotinib is a selective BCR-ABL inhibitor that fits into the ATP-binding site of the BCR-ABL protein. It has a higher affinity for the BCR-ABl protein than imatinib. It is not only more potent than imatinib against wild-type BCR-ABL (IC50 < 30 nM), but also significantly active against 32/33 imatinib-resistant BCR-ABL mutants. Nilotinib was as potent as imatinib in inducing apoptosis (IC50 = 0.54 nM) and inhibiting proliferation (IC50 = 0.20 nM) of EOL-1 cells.