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Nilotinib



Nilotinib
Systematic (IUPAC) name
4-methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)
phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]
benzamide
Identifiers
CAS number 641571-10-0(base)
ATC code  ?
PubChem 644241
Chemical data
Formula C28H22F3N7O 
Mol. mass 529.516 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?

Legal status
Routes Oral

Nilotinib, in the form of the hydrochloride monohydrate salt, is a tyrosine kinase inhibitor approved as Tasigna® in the USA and the EU for drug-resistant chronic myelogenous leukemia (CML)[1]. 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.[2] In that study 92% of patients (already resistant or unresponsive to Gleevec) achieved a normal white blood cell counts after 5 month of treatment. [3]

Additional recommended knowledge

The drug will carry a black box warning for possible heart complications. [4]

References

  1. ^ Novartis 29/10/2007 Press Release.
  2. ^ Kantarjian H et al. (2006). "Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive ALL". N Engl J Med 354 (24): 2542-51. PMID 16775235.
  3. ^ http://cws.huginonline.com/N/134323/PR/200606/1056533_5.html Patients with treatment-resistant leukemia achieve high responses to Tasigna® (nilotinib) in first published clinical trial results - Novartis 14/06/2006 Press Release.
  4. ^ http://www.fda.gov/bbs/topics/NEWS/2007/NEW01734.html FDA Approves Tasigna for Treatment of Philadelphia Chromosome Positive Chronic Myeloid Leukemia - FDA 31/10/2007 Press Release
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Nilotinib". A list of authors is available in Wikipedia.
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