算是新藥,不過因為心臟副作用大,台灣目前比較少看到他

Nilotinib (AMN107, Novartis) is a new, orally active, aminopyrimidine-derivative tyrosine kinase inhibitor that is more potent against CML cells in vitro than is imatinib.8,9,10,11,12 Like imatinib, nilotinib functions through competitive inhibition at the ATP-binding site of BCR-ABL, leading to the inhibition of tyrosine phosphorylation of proteins that are involved in the intracellular signal transduction that BCR-ABL mediates. Nilotinib has a higher binding affinity and selectivity for the ABL kinase than does imatinib. It also has 20 to 50 times the inhibitory activity of imatinib in imatinib-sensitive CML cell lines and 3 to 7 times the activity in imatinib-resistant cell lines. Nilotinib was also active in 32 of 33 imatinib-resistant cell lines with mutant ABL kinases.8,9,10,11,12 This report summarizes the results of a phase 1 dose-escalation study of nilotinib in patients with CML and Ph-positive ALL whose disease was resistant to imatinib.

資料來源:N Engl J Med 354:2542, June 15, 2006 Original Article

60_Nilotinib monohydrochloride, monohydrate.jpg

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機轉圖解說:

圖解藥理學 13 化療藥物機轉-10

 

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