Nilotinib

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Structural formula
Structural formula of nilotinib
General
Non-proprietary name Nilotinib
other names

4-methyl- N - [3- (4-methylimidazol-1-yl) -5- (trifluoromethyl) phenyl] -3 - [(4-pyridin-3-ylpyrimidin-2-yl) amino] benzamide ( IUPAC )

Molecular formula C 28 H 22 F 3 N 7 O
External identifiers / databases
CAS number 641571-10-0
EC number 700-544-5
ECHA InfoCard 100.166.395
PubChem 644241
ChemSpider 559260
DrugBank DB04868
Wikidata Q412327
Drug information
ATC code

L01 XE08

Drug class

Tyrosine kinase inhibitor

properties
Molar mass 529.52 g · mol -1
safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
GHS hazard labeling
no classification available
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Nilotinib (trade name: Tasigna ® , manufacturer: Novartis ) is a protein kinase inhibitor that was developed under the name AMN107 . It is a specific BCR-ABL tyrosine kinase inhibitor . Tasigna was first approved in Switzerland in mid-2007 for the treatment of chronic myeloid leukemia (CML), and approval in the USA and the EU followed shortly afterwards. The prescription drug for the treatment of CML has been available in Germany since January 1, 2008.

The approval was initially granted to patients who do not tolerate treatment with imatinib or who do not respond to it. Approval for newly diagnosed patients followed at the end of 2010. The approval was based on large phase III therapy studies in which nilotinib had also shown efficacy in imatinib-resistant CML patients.

Currently (as of July 2020) nilotinib is in a phase II study for the treatment of Alzheimer's disease .

Side effects

Like most tyrosine kinase inhibitors, nilotinib can cause a reversible reduction in red blood cells ( anemia ), white blood cells ( leukopenia ) and thrombocytes ( thrombocytopenia ), which is usually only mild to moderate and does not limit the use of the drug. Nilotinib causes an increase in the QT time in the electrocardiogram (ECG) in around 1% of patients . Due to the occurrence of sudden cardiac death in 0.6% of patients in the pivotal phase II study for nilotinib, potassium or magnesium deficiency or long QT syndrome are contraindications to treatment with nilotinib. Since nilotinib can lead to short-term significantly increased plasma levels if taken at the same time as fat, no food should be consumed two hours before and one hour after taking the preparation. ECG checks should also be carried out before the start of therapy and during the course.

Individual evidence

  1. ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
  2. ↑ H. Kantarjian et al .: Nilotinib in Imatinib-Resistant CML and Philadelphia Chromosome – Positive ALL . In: New England Journal of Medicine . tape 354 , no. 24 , June 15, 2006, pp. 2542-2551 , doi : 10.1056 / NEJMoa055104 , PMID 16775235 .
  3. ↑ Sven Siebenand: Dementia research: Nilotinib in Alzheimer's disease in conversation. In: pharmische-zeitung.de. July 20, 2020, accessed July 20, 2020 .
  4. ↑ Clinical study (phase II): Impact of Nilotinib on Safety, Biomarkers and Clinical Outcomes in Mild to Moderate Alzheimer's Disease (AD) at Clinicaltrials.gov of the NIH
  5. ↑ E. Jabbour, M. Deininger, A. Hochhaus: Management of adverse events associated with tyrosine kinase inhibitors in the treatment of chronic myeloid leukemia . In: Leukemia . tape 25 , no. 2 , 2011, p. 201-210 , doi : 10.1038 / leu.2010.215 , PMID 20861918 .

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