Nilotinib

Nilotinib
Clinical data
Trade namesTasigna, others
Other namesAMN107
AHFS/Drugs.comMonograph
MedlinePlusa608002
License data
Pregnancy
category
  • AU: D
Routes of
administration		By mouth
Drug classAntineoplastic
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability30%[5]
Protein binding98%[5]
MetabolismLiver (mostly CYP3A4-mediated)[5]
Elimination half-life15-17 hours[5]
ExcretionFaeces (93%)[5]
Identifiers
  • 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)- 5-(trifluoromethyl)phenyl]-3- [(4-pyridin-3-ylpyrimidin-2-yl) amino]benzamide
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
CompTox Dashboard (EPA)
ECHA InfoCard100.166.395 Edit this at Wikidata
Chemical and physical data
FormulaC28H22F3N7O
Molar mass529.527 g·mol−1
3D model (JSmol)
  • Cc1ccc(cc1Nc2nccc(n2)c3cccnc3)C(=O)Nc4cc(cc(c4)n5cc(nc5)C)C(F)(F)F
  • 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) checkY
  • Key:HHZIURLSWUIHRB-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Nilotinib, sold under the brand name Tasigna among others, is a anti-cancer medication used to treat chronic myelogenous leukemia (CML) which has the Philadelphia chromosome.[3][6] 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.[3][6][7] It is taken by mouth.[3][7]

Common side effects may include low platelets, low white blood cells, anemia, rashes, vomiting, diarrhea, and joint pains.[7] Other serious side effects may include QT prolongation, sudden death, pancreatitis, and liver problems.[7] It is not safe for use during pregnancy.[7] Nilotinib is a Bcr-Abl tyrosine kinase inhibitor and works by interfering with signalling within the cancer cell.[3][7]

Nilotinib was approved for medical use in the United States in 2007.[3][7] It is on the World Health Organization's List of Essential Medicines.[8] It is approved as a generic medication.[9]

  1. ^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved October 22, 2023.
  2. ^ "Tasigna Summary of Product Characteristics (SmPC)". (emc). October 5, 2023. Archived from the original on March 2, 2024. Retrieved November 13, 2024.
  3. ^ a b c d e f "Tasigna- nilotinib capsule". DailyMed. February 8, 2024. Retrieved March 9, 2024.
  4. ^ "Tasigna EPAR". European Medicines Agency (EMA). May 22, 2006. Retrieved August 27, 2024.
  5. ^ a b c d e Cite error: The named reference MSR was invoked but never defined (see the help page).
  6. ^ a b "Nilotinib". National Cancer Institute. February 1, 2008. Archived from the original on July 14, 2021. Retrieved November 14, 2019.
  7. ^ a b c d e f g "Nilotinib Monograph for Professionals". Drugs.com. Archived from the original on July 14, 2021. Retrieved November 14, 2019.
  8. ^ World Health Organization (2023). The selection and use of essential medicines 2023: web annex A: World Health Organization model list of essential medicines: 23rd list (2023). Geneva: World Health Organization. hdl:10665/371090. WHO/MHP/HPS/EML/2023.02.
  9. ^ "First-Time Generic Drug Approvals 2024". U.S. Food and Drug Administration (FDA). March 8, 2024. Archived from the original on January 26, 2021. Retrieved March 9, 2024.