Nilotinib

Nilotinib
Clinical data
Trade names	Tasigna, others
Other names	AMN107
AHFS/Drugs.com	Monograph
MedlinePlus	a608002
License data	EU EMA: by INN; US DailyMed: Nilotinib;
Pregnancy; category	AU: D;
Routes of; administration	By mouth
ATC code	L01EA03 (WHO) ;
Legal status
Legal status	AU: S4 (Prescription only); CA: ℞-only; UK: POM (Prescription only); US: WARNINGRx-only; EU: Rx-only;
Pharmacokinetic data
Bioavailability	30%
Protein binding	98%
Metabolism	Liver (mostly CYP3A4-mediated)
Elimination half-life	15-17 hours
Excretion	Faeces (93%)
Identifiers
	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);
PubChem CID	644241;
IUPHAR/BPS	5697;
DrugBank	DB04868 ;
ChemSpider	559260 ;
UNII	F41401512X;
KEGG	D08953 ;
ChEBI	CHEBI:52172 ;
ChEMBL	ChEMBL255863 ;
PDB ligand	NIL (PDBe, RCSB PDB);
CompTox Dashboard (EPA)	DTXSID5042663 ;
ECHA InfoCard	100.166.395
Chemical and physical data
Formula	C28H22F3N7O
Molar mass	529.527 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES Cc1ccc(cc1Nc2nccc(n2)c3cccnc3)C(=O)Nc4cc(cc(c4)n5cc(nc5)C)C(F)(F)F;
	InChI InChI=1S/C28H22F3N7O/c1-17-5-6-19(10-25(17)37-27-33-9-7-24(36-27)20-4-3-8-32-14-20)26(39)35-22-11-21(28(29,30)31)12-23(13-22)38-15-18(2)34-16-38/h3-16H,1-2H3,(H,35,39)(H,33,36,37) ; Key:HHZIURLSWUIHRB-UHFFFAOYSA-N ;
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Nilotinib, sold under the brand name Tasigna marketed worldwide by Novartis, is a medication used to treat chronic myelogenous leukemia (CML) which has the Philadelphia chromosome. It may be used both in initial cases of chronic phase CML as well as in accelerated and chronic phase CML that has not responded to imatinib. It is taken by mouth.

Common side effects may include low platelets, low white blood cells, anemia, rashes, vomiting, diarrhea, and joint pains. Other serious side effects may include QT prolongation, sudden death, pancreatitis, and liver problems. It is not safe for use during pregnancy. Nilotinib is a Bcr-Abl tyrosine kinase inhibitor and works by interfering with signalling within the cancer cell.

Nilotinib was approved for medical use in the United States in 2007. It is on the World Health Organization's List of Essential Medicines.

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