The Full Wiki

More info on Nilotinib

Nilotinib: Wikis

Advertisements
  

Note: Many of our articles have direct quotes from sources you can cite, within the Wikipedia article! This article doesn't yet, but we're working on it! See more info or our list of citable articles.

Encyclopedia

From Wikipedia, the free encyclopedia

Nilotinib
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
Identifiers
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]

Uses

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]

References

  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. http://cws.huginonline.com/N/134323/PR/200606/1056533_5.html. 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. http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/2007/ucm109017.htm. Retrieved 2009-08-04. 
  6. ^ "Prescribing information for Tasigna (nilotinib) Capsules" (PDF). NDA 022068. U.S. FDA. 2007-10-29. http://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022068lbl.pdf. Retrieved 2009-08-04. 
Advertisements

Advertisements






Got something to say? Make a comment.
Your name
Your email address
Message