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A highly selective BCR-ABL tyrosine kinase inhibitor
selleckchem
Posted: Tuesday, April 07, 2015 7:32 PM
Joined: 4/7/2015
Posts: 1


Nilotinib, an orally bioavailable, selective Bcr-Abl tyrosine kinase inhibitor, is 30-fold far more potent than imatinib in pre-clinical models, and overcomes most imatinib resistant BCR-ABL mutations. Within this phase two open-label study, 400 mg nilotinib was administered orally twice day-to-day to 280 individuals with Philadelphia chromosome�Cpositive (Ph+) chronic myeloid leukemia in chronic phase (CML-CP) right after imatinib failure or intolerance. Patients had at the least 6 months of follow-up and had been evaluated for hematologic and cytogenetic responses, and also for safety and general survival. At 6 months, the rate of important cytogenetic response (Ph < 35%) was 48%: full (Ph = 0%) in 31%, and partial (Ph = 1%-35%) in 16%. The estimated survival at 12 months was 95%. Nilotinib was powerful in individuals harboring BCR-ABL mutations linked to imatinib resistance (except T315I), as well as in patients having a resistance mechanism independent of BCR-ABL mutations. Adverse events were mostly mild to moderate, and there was minimal cross- intolerance with imatinib. Grades 3 to 4 neutropenia and thrombocytopenia had been observed in 29% of sufferers; pleural or pericardial effusions were observed in 1% (none were serious). In summary, nilotinib is very active and secure in patients with CML-CP following imatinib failure or intolerance. This clinical trial is registered at http://www.selleckchem.com/products/Nilotinib.html
inhibitor expert
 

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