Nilotinib - CAS 641571-10-0
Catalog number: 641571-10-0
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
Nilotinib is a Bcr-Abl inhibitor with IC50 less than 30 nM.
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1.Peripheral arterial occlusive disease during ponatinib therapy after failure of imatinib: a case report.
Tournaire G1, Despas F2, Huguet F3, Montastruc JL1, Bondon-Guitton E1. J Clin Pharm Ther. 2016 Mar 23. doi: 10.1111/jcpt.12383. [Epub ahead of print]
WHAT IS KNOWN AND OBJECTIVE: Peripheral vascular adverse events have been reported with ponatinib treatment in chronic myeloid leukaemia (CML) after failure of dasatinib or nilotinib. We here report peripheral arterial occlusive disease (PAOD) in a patient who had previously received only imatinib as tyrosine kinase inhibitor.
2.Simplifying procedure for prediction of resistance risk in CML patients - Test of sensitivity to TKI ex vivo.
Žáčková M1, Macháčková-Lopotová T2, Ondráčková Z3, Kuželová K2, Klamová H4, Moravcová J2. Blood Cells Mol Dis. 2016 May;58:67-75. doi: 10.1016/j.bcmd.2016.03.005. Epub 2016 Mar 10.
Tyrosine kinase inhibitors (TKIs) targeting BCR-ABL have dramatically improved chronic myeloid leukemia therapy. While imatinib remains to be the first line therapy, about 30% of patients develop resistance or intolerance to this drug and are recommended to switch to other TKIs. Nilotinib and dasatinib are currently implemented into the first line therapy and other inhibitors have already entered the clinical practice. This opens further questions on how to select the best TKI for each patient not only during the therapy but also at diagnosis. The individualized therapy concept requires a reliable establishment of prognosis and prediction of response to the available TKIs. We tested the ex vivo sensitivity of patient primary leukocytes to imatinib, nilotinib and dasatinib - two concentrations of each inhibitor for 48h incubation - and we evaluated the usefulness of such tests for the clinical practice. Besides reflecting the actual sensitivity to the therapy, our optimized simple tests were able to predict the outcome in 90/87% of patients, for the next 12/24months, respectively.
3.Update on the management of Philadelphia chromosome positive chronic myelogenous leukemia: role of nilotinib.
Emole J1, Talabi T2, Pinilla-Ibarz J1. Biologics. 2016 Feb 26;10:23-31. doi: 10.2147/BTT.S67844. eCollection 2016.
Chronic myelogenous leukemia (CML) is a pluripotent stem cell disease characterized by the presence of the Philadelphia chromosome and the bcr-abl gene. The discovery of tyrosine kinase inhibitors (TKIs) revolutionized therapy for CML, such that durable response, increased overall survival, and increased progression-free survival of patients in chronic phase CML is now possible. Due to resistance and intolerance to imatinib, there was need for development of second- and third-generation TKIs for the treatment of CML. This review examines the role of nilotinib, an oral second-generation TKI, in the treatment of Philadelphia positive CML. The pharmacology, efficacy, and safety of nilotinib are critically evaluated. Patient-related issues, including tolerance, drug interactions, and quality of life issues are also examined.
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