| Attributes | Values |
|---|
| rdf:type
| |
| http://linked.open...gbank/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. (en)
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| http://linked.open...y/drugbank/dosage
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| http://linked.open...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. (en)
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| http://linked.open...gy/drugbank/group
| - approved (en)
- investigational (en)
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| http://linked.open...drugbank/halfLife
| - Axitinib has a half life of 2.5 to 6.1 hours. (en)
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| http://linked.open...ugbank/indication
| - Used in kidney cell cancer and investigated for use/treatment in pancreatic and thyroid cancer. (en)
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| sameAs
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| Title
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| adms:identifier
| |
| http://linked.open...mechanismOfAction
| - Axitinib selectively blocks the tyrosine kinase receptors VEGFR-1 (vascular endothelial growth factor receptor), VEGFR-2, and VEGFR-3. (en)
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| http://linked.open...outeOfElimination
| - 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. (en)
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| http://linked.open.../drugbank/synonym
| |
| http://linked.open...drugbank/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. (en)
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| http://linked.open...umeOfDistribution
| - The volume of distribution is 160 L. (en)
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| http://linked.open.../drug/hasAHFSCode
| |
| http://linked.open...k/foodInteraction
| - Axitinib can be taken with or without food. (en)
- 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%. (en)
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| http://linked.open...nk/proteinBinding
| - Plasma protein binding for axitinib is high at over 99% with most protein binding to albumin followed by α1-acid glycoprotein. (en)
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| http://linked.open...ynthesisReference
| - 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. (en)
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| foaf:page
| |
| http://linked.open.../Water-Solubility
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| http://linked.open...logy/drugbank/pKa
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| http://linked.open...l/drug/hasATCCode
| |
| http://linked.open...ugbank/absorption
| - After one 5 mg dose of axitinib, it takes about 2.5 to 4.1 hours to reach maximum plasma concentration. (en)
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| http://linked.open.../affectedOrganism
| - Humans and other mammals (en)
|
| http://linked.open...casRegistryNumber
| |
| http://linked.open...rugbank/clearance
| - The average clearance of axitinib is 38 L/h. (en)
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