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Namespace Prefixes

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Statements

Subject Item
n2:DB06626
rdf:type
n8:Drug
n8:description
Axitinib is an oral, potent, and selective inhibitor of vascular endothelial growth factor receptors (VEGFR) 1, 2, and 3. Axitinib is marketed under the name Inlyta®, and if one previous systemic therapy for kidney cell cancer has failed, axitinib is indicated.
n8:dosage
n14:271B4D9C-363D-11E5-9242-09173F13E4C5 n14:271B4D9D-363D-11E5-9242-09173F13E4C5 n14:271B4D9E-363D-11E5-9242-09173F13E4C5 n14:271B4D9F-363D-11E5-9242-09173F13E4C5
n8:generalReferences
# Cohen EE, Rosen LS, Vokes EE, Kies MS, Forastiere AA, Worden FP, Kane MA, Sherman E, Kim S, Bycott P, Tortorici M, Shalinsky DR, Liau KF, Cohen RB: Axitinib Is an Active Treatment for All Histologic Subtypes of Advanced Thyroid Cancer: Results From a Phase II Study. J Clin Oncol. 2008 Jun 9. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18541897 # Inai T, Mancuso M, Hashizume H, Baffert F, Haskell A, Baluk P, Hu-Lowe DD, Shalinsky DR, Thurston G, Yancopoulos GD, McDonald DM: Inhibition of vascular endothelial growth factor (VEGF) signaling in cancer causes loss of endothelial fenestrations, regression of tumor vessels, and appearance of basement membrane ghosts. Am J Pathol. 2004 Jul;165(1):35-52. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15215160 # Rugo HS, Herbst RS, Liu G, Park JW, Kies MS, Steinfeldt HM, Pithavala YK, Reich SD, Freddo JL, Wilding G: Phase I trial of the oral antiangiogenesis agent AG-013736 in patients with advanced solid tumors: pharmacokinetic and clinical results. J Clin Oncol. 2005 Aug 20;23(24):5474-83. Epub 2005 Jul 18. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16027439 # Rini BI: SU11248 and AG013736: current data and future trials in renal cell carcinoma. Clin Genitourin Cancer. 2005 Dec;4(3):175-80. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16425985 # Gilbert JA, Adhikari LJ, Lloyd RV, Halfdanarson TR, Muders MH, Ames MM: Molecular markers for novel therapeutic strategies in pancreatic endocrine tumors. Pancreas. 2013 Apr;42(3):411-21. doi: 10.1097/MPA.0b013e31826cb243. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23211371 # FDA label.
n8:group
investigational approved
n8:halfLife
Axitinib has a half life of 2.5 to 6.1 hours.
n8:indication
Used in kidney cell cancer and investigated for use/treatment in pancreatic and thyroid cancer.
owl:sameAs
n13:DB06626
dcterms:title
Axitinib
adms:identifier
n4:D03218 n5:0069-0145-01 n6:66910 n7:DB06626 n20:PA164924493 n21:Axitinib
n8:mechanismOfAction
Axitinib selectively blocks the tyrosine kinase receptors VEGFR-1 (vascular endothelial growth factor receptor), VEGFR-2, and VEGFR-3.
n8:routeOfElimination
Axitinib is mainly eliminated unchanged in the feces (41%) with 12% of the original dose as unchanged axitinib. There is also 23% eliminated in the urine, most of which are metabolites.
n8:synonym
SID103905539
n8:toxicity
Some of the more serious toxic effects seen in patients taking axitinib include, but are not limited to, hypertension, thrombotic events, hemorrhage, and GI perforation.
n8:volumeOfDistribution
The volume of distribution is 160 L.
n16:hasAHFSCode
n17:10-00%20
n8:foodInteraction
Avoid combination with strong CYP3A4 inhibitors such as grapefruit juice due to the likely increased levels of axitinib. If the combination cannot be avoided, reduce axitinib dose by 50%. Axitinib can be taken with or without food.
n8:proteinBinding
Plasma protein binding for axitinib is high at over 99% with most protein binding to albumin followed by α1-acid glycoprotein.
n8:synthesisReference
Hu-Lowe D, Hallin M, Feeley R, Zou H, Rewolinski D, Wickman G, Chen E, Kim Y, Riney S, Reed J, Heller D, Simmons B, Kania R, McTigue M, Niesman M, Gregory S, Shalinsky D, Bender S. Characterization of potency and activity of the VEGF/PDGF receptor tyrosine kinase inhibitor AG013736. Proc Am Assoc Cancer Res. 2002;43:A5357.
foaf:page
n11:inlyta-drug.htm n18:axitinib.html
n8:Water-Solubility
n9:271B4DA0-363D-11E5-9242-09173F13E4C5
n8:pKa
n9:271B4DA1-363D-11E5-9242-09173F13E4C5
n16:hasATCCode
n19:L01XE17
n8:absorption
After one 5 mg dose of axitinib, it takes about 2.5 to 4.1 hours to reach maximum plasma concentration.
n8:affectedOrganism
Humans and other mammals
n8:casRegistryNumber
319460-85-0
n8:clearance
The average clearance of axitinib is 38 L/h.