About: Gefitinib

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An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

Attributes	Values
rdf:type	http://linked.opendata.cz/ontology/drugbank/Drug
http://linked.open...gbank/description	Gefitinib (originally coded ZD1839) is a drug used in the treatment of certain types of cancer. Acting in a similar manner to erlotinib (marketed as Tarceva), gefitinib selectively targets the mutant proteins in malignant cells. It is marketed by AstraZeneca under the trade name Iressa. [Wikipedia] (en)
http://linked.open...y/drugbank/dosage	http://linked.opendata.cz/resource/drugbank/dosage/271B5290-363D-11E5-9242-09173F13E4C5
http://linked.open...generalReferences	# Pao W, Miller V, Zakowski M, Doherty J, Politi K, Sarkaria I, Singh B, Heelan R, Rusch V, Fulton L, Mardis E, Kupfer D, Wilson R, Kris M, Varmus H: EGF receptor gene mutations are common in lung cancers from "never smokers" and are associated with sensitivity of tumors to gefitinib and erlotinib. Proc Natl Acad Sci U S A. 2004 Sep 7;101(36):13306-11. Epub 2004 Aug 25. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15329413 # Sordella R, Bell DW, Haber DA, Settleman J: Gefitinib-sensitizing EGFR mutations in lung cancer activate anti-apoptotic pathways. Science. 2004 Aug 20;305(5687):1163-7. Epub 2004 Jul 29. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/ # FDA label (en)
http://linked.open...gy/drugbank/group	approved (en) investigational (en)
http://linked.open...drugbank/halfLife	48 hours [IV administration] (en)
http://linked.open...ugbank/indication	For the continued treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of either platinum-based or docetaxel chemotherapies. (en)
http://linked.open...bank/manufacturer	Astrazeneca uk ltd
sameAs	Gefitinib
Title	Gefitinib (en)
adms:identifier	http://linked.opendata.cz/resource/drugbank/drug/DB00317/identifier/bindingdb/5447 http://linked.opendata.cz/resource/drugbank/drug/DB00317/identifier/chebi/49668 http://linked.opendata.cz/resource/drugbank/drug/DB00317/identifier/chemspider/110217 http://linked.opendata.cz/resource/drugbank/drug/DB00317/identifier/drugbank/DB00317 http://linked.opendata.cz/resource/drugbank/drug/DB00317/identifier/kegg-drug/D01977 http://linked.opendata.cz/resource/drugbank/drug/DB00317/identifier/national-drug-code-directory/0310-0482-30 http://linked.opendata.cz/resource/drugbank/drug/DB00317/identifier/pdb/IRE http://linked.opendata.cz/resource/drugbank/drug/DB00317/identifier/pubchem-compound/123631 http://linked.opendata.cz/resource/drugbank/drug/DB00317/identifier/pubchem-substance/46508649 http://linked.opendata.cz/resource/drugbank/drug/DB00317/identifier/pharmgkb/PA131301952 http://linked.opendata.cz/resource/drugbank/drug/DB00317/identifier/wikipedia/Gefitinib
http://linked.open...mechanismOfAction	Gefitinib inhibits the epidermal growth factor receptor (EGFR) tyrosine kinase by binding to the adenosine triphosphate (ATP)-binding site of the enzyme. Thus the function of the EGFR tyrosine kinase in activating the Ras signal transduction cascade is inhibited; and malignant cells are inhibited. Gefitinib is the first selective inhibitor of the EGFR tyrosine kinase which is also referred to as Her1 or ErbB-1. EGFR is overexpressed in the cells of certain types of human carcinomas - for example in lung and breast cancers. Overexpression leads to inappropriate activation of the apoptotic Ras signal transduction cascade, eventually leading to uncontrolled cell proliferation. (en)
http://linked.open...drugbank/packager	Pfizer Inc. Genentech Inc.
http://linked.open...y/drugbank/patent	http://linked.opendata.cz/resource/drugbank/patent/2086968 http://linked.opendata.cz/resource/drugbank/patent/2215732 http://linked.opendata.cz/resource/drugbank/patent/5457105 http://linked.opendata.cz/resource/drugbank/patent/5770599
http://linked.open...outeOfElimination	Elimination is by metabolism (primarily CYP3A4) and excretion in feces. Excretion is predominantly via the feces (86%), with renal elimination of drug and metabolites accounting for less than 4% of the administered dose. (en)
http://linked.open.../drugbank/synonym	Gefitinib (en) Iressa (en) N-(3-chloro-4-Fluorophenyl)-7-methoxy-6-(3-(4-morpholinyl)propoxy)-4-quinazolinamine (en) ZD 1839 (en) 4-(3'-chloro-4'-Fluoroanilino)-7-methoxy-6-(3-morpholinopropoxy)quinazoline (en)
http://linked.open...drugbank/toxicity	The acute toxicity of gefitinib up to 500 mg in clinical studies has been low. In non-clinical studies, a single dose of 12,000 mg/m<sup>2</sup> (about 80 times the recommended clinical dose on a mg/m<sup>2</sup> basis) was lethal to rats. Half this dose caused no mortality in mice. Symptoms of overdose include diarrhea and skin rash. (en)
http://linked.open...umeOfDistribution	* 1400 L [IV administration] (en)
http://linked.open.../drug/hasAHFSCode	http://linked.opendata.cz/resource/AHFS/10-00-00
http://linked.open...k/foodInteraction	Avoid fresh grapefruit and its juice during therapy as grapefruit may increase serum product levels. (en) Take without regard to meals. (en)
http://linked.open...nk/proteinBinding	90% primarily to serum albumin and alpha 1-acid glycoproteins (independent of drug concentrations). (en)
http://linked.open...ynthesisReference	"DrugSyn.org":http://www.drugsyn.org/Gefitinib.htm (en)
foaf:page	http://www.drugs.com/cdi/gefitinib.html http://www.rxlist.com/cgi/generic3/iressa.htm
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http://linked.open...l/drug/hasATCCode	Gefitinib
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http://linked.open...ugbank/absorption	Absorbed slowly after oral administration with a mean bioavailability of 60%. Peak plasma levels occurs 3-7 hours post-administration. Food does not affect the bioavailability of gefitinib. (en)
http://linked.open.../affectedOrganism	Humans and other mammals (en)
http://linked.open...casRegistryNumber	184475-35-2 (en)
http://linked.open...rugbank/clearance	* 595 mL/min [IV administration] (en)
http://linked.open...gbank/containedIn	Diabeta 2.5 mg tablet Iressa 250 mg tablet Nexium i.v. 40 mg vial Tarceva 150 mg tablet
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http://linked.open...-strongest-basic-	http://linked.opendata.cz/resource/drugbank/property/271B52A4-363D-11E5-9242-09173F13E4C5

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