About: Gefitinib     Goto   Sponge   NotDistinct   Permalink

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

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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.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
sameAs
Title
  • Gefitinib (en)
adms:identifier
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
http://linked.open...y/drugbank/patent
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.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://linked.open...ugbank/IUPAC-Name
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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
http://linked.open...k/Bioavailability
http://linked.open...bank/Ghose-Filter
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http://linked.open...strongest-acidic-
http://linked.open...-strongest-basic-
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