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Namespace Prefixes

PrefixIRI
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n28http://linked.opendata.cz/resource/drugbank/drug/DB00317/identifier/pharmgkb/
n27http://linked.opendata.cz/resource/drugbank/dosage/
n18http://linked.opendata.cz/resource/drugbank/drug/DB00317/identifier/pdb/
n22http://linked.opendata.cz/resource/drugbank/drug/DB00317/identifier/bindingdb/
n16http://linked.opendata.cz/resource/drugbank/drug/DB00317/identifier/pubchem-compound/
n30http://bio2rdf.org/drugbank:
n15http://linked.opendata.cz/resource/drugbank/drug/DB00317/identifier/pubchem-substance/
n19http://linked.opendata.cz/resource/drugbank/drug/DB00317/identifier/kegg-drug/
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n21http://linked.opendata.cz/resource/drugbank/drug/DB00317/identifier/drugbank/
n9http://linked.opendata.cz/resource/drugbank/patent/
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n17http://linked.opendata.cz/resource/drugbank/drug/DB00317/identifier/national-drug-code-directory/
rdfhttp://www.w3.org/1999/02/22-rdf-syntax-ns#
n8http://linked.opendata.cz/resource/drugbank/medicinal-product/
owlhttp://www.w3.org/2002/07/owl#
n3http://linked.opendata.cz/ontology/drugbank/
n29http://www.drugs.com/cdi/
n4http://linked.opendata.cz/resource/drugbank/property/
n20http://linked.opendata.cz/resource/drugbank/drug/DB00317/identifier/chemspider/
xsdhhttp://www.w3.org/2001/XMLSchema#
n13http://linked.opendata.cz/resource/atc/
n23http://linked.opendata.cz/resource/drugbank/drug/DB00317/identifier/chebi/
n6http://linked.opendata.cz/ontology/sukl/drug/

Statements

Subject Item
n2:DB00317
rdf:type
n3:Drug
n3: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]
n3:dosage
n27:271B5290-363D-11E5-9242-09173F13E4C5
n3: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
n3:group
investigational approved
n3:halfLife
48 hours [IV administration]
n3: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.
n3:manufacturer
n5:271B528B-363D-11E5-9242-09173F13E4C5
owl:sameAs
n11:DB00317 n30:DB00317
dcterms:title
Gefitinib
adms:identifier
n15:46508649 n16:123631 n17:0310-0482-30 n18:IRE n19:D01977 n20:110217 n21:DB00317 n22:5447 n23:49668 n26:Gefitinib n28:PA131301952
n3: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.
n3:packager
n5:271B5289-363D-11E5-9242-09173F13E4C5 n5:271B528A-363D-11E5-9242-09173F13E4C5
n3:patent
n9:2086968 n9:2215732 n9:5457105 n9:5770599
n3:routeOfElimination
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.
n3:synonym
Iressa Gefitinib N-(3-chloro-4-Fluorophenyl)-7-methoxy-6-(3-(4-morpholinyl)propoxy)-4-quinazolinamine ZD 1839 4-(3'-chloro-4'-Fluoroanilino)-7-methoxy-6-(3-morpholinopropoxy)quinazoline
n3: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.
n3:volumeOfDistribution
* 1400 L [IV administration]
n6:hasAHFSCode
n7:10-00-00
n3:foodInteraction
Avoid fresh grapefruit and its juice during therapy as grapefruit may increase serum product levels. Take without regard to meals.
n3:proteinBinding
90% primarily to serum albumin and alpha 1-acid glycoproteins (independent of drug concentrations).
n3:synthesisReference
"DrugSyn.org":http://www.drugsyn.org/Gefitinib.htm
foaf:page
n25:iressa.htm n29:gefitinib.html
n3:IUPAC-Name
n4:271B5295-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B529B-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B529A-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B5297-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B5298-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B5299-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B5293-363D-11E5-9242-09173F13E4C5 n4:271B52AB-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B5291-363D-11E5-9242-09173F13E4C5 n4:271B5294-363D-11E5-9242-09173F13E4C5 n4:271B52AC-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B5292-363D-11E5-9242-09173F13E4C5
n3:pKa
n4:271B52AD-363D-11E5-9242-09173F13E4C5
n6:hasATCCode
n13:L01XE02
n3:H-Bond-Acceptor-Count
n4:271B52A1-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B52A2-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B529C-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B529D-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B529F-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B529E-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B52A0-363D-11E5-9242-09173F13E4C5
n3: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.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
184475-35-2
n3:clearance
* 595 mL/min [IV administration]
n3:containedIn
n8:271B528C-363D-11E5-9242-09173F13E4C5 n8:271B528F-363D-11E5-9242-09173F13E4C5 n8:271B528D-363D-11E5-9242-09173F13E4C5 n8:271B528E-363D-11E5-9242-09173F13E4C5
n3:Bioavailability
n4:271B52A7-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B52A9-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B52AA-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B52A6-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B52A5-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B52A8-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B5296-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n4:271B52A3-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B52A4-363D-11E5-9242-09173F13E4C5