Axitinib

Axitinib
Clinical data
Trade namesInlyta, Axinix
Other namesAG013736
AHFS/Drugs.comMonograph
MedlinePlusa612017
License data
Pregnancy
category
  • AU: D
Routes of
administration		By mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability58%[3]
Protein binding>99%[3]
MetabolismLiver (mostly CYP3A4/CYP3A5-mediated but with some contributions from CYP1A2, CYP2C19, UGT1A1)[3]
Elimination half-life2.5-6.1 hours[3]
ExcretionFeces (41%; 12% as unchanged drug), urine (23%)[3]
Identifiers
  • N-Methyl-2-[[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]sulfanyl]benzamide
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
CompTox Dashboard (EPA)
ECHA InfoCard100.166.384 Edit this at Wikidata
Chemical and physical data
FormulaC22H18N4OS
Molar mass386.47 g·mol−1
3D model (JSmol)
  • CNC(=O)c1ccccc1Sc4ccc3c(C=Cc2ccccn2)n[nH]c3c4
  • InChI=1S/C22H18N4OS/c1-23-22(27)18-7-2-3-8-21(18)28-16-10-11-17-19(25-26-20(17)14-16)12-9-15-6-4-5-13-24-15/h2-14H,1H3,(H,23,27)(H,25,26)/b12-9+ checkY
  • Key:RITAVMQDGBJQJZ-FMIVXFBMSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Axitinib, sold under the brand name Inlyta, is a small molecule tyrosine kinase inhibitor developed by Pfizer. It has been shown to significantly inhibit growth of breast cancer in animal (xenograft) models[4] and has shown partial responses in clinical trials with renal cell carcinoma (RCC)[5] and several other tumour types.[6]

It was approved to treat renal cell carcinoma by the U.S. Food and Drug Administration after showing a modest increase in progression-free survival,[7] though there have been reports of fatal adverse effects.[8]

  1. ^ Cite error: The named reference Inlyta FDA label was invoked but never defined (see the help page).
  2. ^ "Inlyta EPAR". European Medicines Agency (EMA). 3 September 2012. Retrieved 6 August 2024.
  3. ^ a b c d e "Inlyta (axitinib) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Retrieved 25 January 2014.
  4. ^ Wilmes LJ, Pallavicini MG, Fleming LM, Gibbs J, Wang D, Li KL, et al. (April 2007). "AG-013736, a novel inhibitor of VEGF receptor tyrosine kinases, inhibits breast cancer growth and decreases vascular permeability as detected by dynamic contrast-enhanced magnetic resonance imaging". Magnetic Resonance Imaging. 25 (3): 319–327. doi:10.1016/j.mri.2006.09.041. PMID 17371720.{{cite journal}}: CS1 maint: overridden setting (link)
  5. ^ Rini B, Rixe O, Bukowski R, Michaelson MD, Wilding G, Hudes G, et al. (June 2005). "AG-013736, a multi-target tyrosine kinase receptor inhibitor, demonstrates anti-tumor activity in a Phase 2 study of cytokine-refractory, metastatic renal cell cancer (RCC)". Journal of Clinical Oncology ASCO Annual Meeting Proceedings. 23 (16S): 4509. Archived from the original on 26 January 2014.{{cite journal}}: CS1 maint: overridden setting (link)
  6. ^ Rugo HS, Herbst RS, Liu G, Park JW, Kies MS, Steinfeldt HM, et al. (August 2005). "Phase I trial of the oral antiangiogenesis agent AG-013736 in patients with advanced solid tumors: pharmacokinetic and clinical results". Journal of Clinical Oncology. 23 (24): 5474–5483. doi:10.1200/JCO.2005.04.192. PMID 16027439.{{cite journal}}: CS1 maint: overridden setting (link)
  7. ^ "FDA Approves Inlyta for Advanced Renal Cell Carcinoma". Drugs.com. 27 January 2012.
  8. ^ Fauber J, Chu E (27 October 2014). "The Slippery Slope: Is a Surrogate Endpoint Evidence of Efficacy?". MedPage Today.