O-Desmethyl Gefitinib

O-Desmethyl Gefitinib

CAT N°: 22365
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O-Desmethyl gefitinib is the major metabolite of gefitinib (Item No. 13166) in human plasma, formed by the cytochrome P450 isoform CYP2D6.{39029} It is an active metabolite that inhibits EGFR similarly to gefitinib in subcellular assays (IC50s = 36 and 22 nM, respectively) but is less active in whole cell assays (IC50s = 760 and 49 nM, respectively).{39030} In a LoVo tumor mouse xenograft model, the tumor concentration of O-desmethyl gefitinib was 6.8-fold lower than that of gefitinib and did not significantly reduce tumor growth. A high plasma concentration of O-desmethyl gefitinib in patients homozygous for CYP2D6 was not associated with an increase in adverse effects.{39028}

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