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Nilotinib: Wikis


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Systematic (IUPAC) name
4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)- 5-(trifluoromethyl)phenyl]-3- [(4-pyridin-3-ylpyrimidin-2-yl) amino]benzamide
CAS number 641571-10-0(base)
ATC code L01XE08
PubChem 644241
Chemical data
Formula C28H22F3N7O 
Mol. mass 529.516 g/mol
Pharmacokinetic data
Bioavailability 30%
Protein binding 98%
Metabolism hepatic
Half life 17 h
Excretion biliary
Therapeutic considerations
Licence data

EU EMEA:linkUS FDA:link

Pregnancy cat. D(US)
Legal status POM (UK) -only (US)
Routes Oral

Nilotinib, in the form of the hydrochloride monohydrate salt, is a tyrosine kinase inhibitor.

It inhibits BCR-ABL.[1]


It was approved as Tasigna in the USA and the EU for drug-resistant chronic myelogenous leukemia (CML)[2]. In June 2006, a Phase I clinical trial found nilotinib, also known by its clinical code AMN107, has a relatively favorable safety profile and shows activity in cases of CML resistant to treatment with imatinib (Gleevec), another tyrosine kinase inhibitor currently used as a first-line treatment.[3] In that study 92% of patients (already resistant or unresponsive to Gleevec) achieved a normal white blood cell counts after five months of treatment.[4] The drug carries a black box warning for possible heart complications.[5][6]


  1. ^ Weisberg E, Manley P, Mestan J, Cowan-Jacob S, Ray A, Griffin JD (June 2006). "AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL". Br. J. Cancer 94 (12): 1765–9. doi:10.1038/sj.bjc.6603170. PMID 16721371. 
  2. ^ Novartis 29/10/2007 Press Release.
  3. ^ Kantarjian H et al. (2006). "Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive ALL". N Engl J Med 354 (24): 2542–51. doi:10.1056/NEJMoa055104. PMID 16775235. 
  4. ^ "Patients with treatment-resistant leukemia achieve high responses to Tasigna (nilotinib) in first published clinical trial results". MediaReleases (Novartis). 2006-06-14. Retrieved 2009-08-04. 
  5. ^ "FDA Approves Tasigna for Treatment of Philadelphia Chromosome Positive Chronic Myeloid Leukemia". U.S. Food and Drug Administration. 2007-10-30. Retrieved 2009-08-04. 
  6. ^ "Prescribing information for Tasigna (nilotinib) Capsules" (PDF). NDA 022068. U.S. FDA. 2007-10-29. Retrieved 2009-08-04. 


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