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Gefitinib belongs to a class of tyrosine kinase inhibitors (TKI) designed to compete with ATP for binding into the ATP binding pocket of mutated or over-expressed receptor and thus inhibit its tyrosine kinase activity and the signaling events downstream of it. Gefitinib along with erlotinib have been used to target epidermal growth factor receptor, Egfr. Gefitinib, presented here, was among the first and the most widely used TKI for use in the treatment of locally advanced or metastatic non-smal

Pathway Diagram:

Ariadne Genomics Inc. CYP3A4 CYP3A5 ABCG2 ABCB1 CYP2D6 CYP1A1 gefitinib ---> other gefitinib metabolites gefitinib ---> O-desmethyl-gefitinib gefitinib and metabolites elimination O-desmethyl-gefitinib ---> gefitinib and metabolites elimination other gefitinib metabolites ---> gefitinib and metabolites elimination gefitinib other gefitinib metabolites O-desmethyl-gefitinib

Genes in Pathway:

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Additional Elements in Pathway:

(includes Gene Groups, Small Molecules, Other Pathways..etc.)
Object TypePathway ObjectPathway Object Description
Small MoleculegefitinibIressa; ZD1839 (AstraZeneca, Inc.)
Small MoleculeO-desmethyl-gefitinibmain metabolite

Pathway Gene Annotations

References Associated with the gefitinib pharmacokinetics pathway:

Ontology Path Diagram:

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