The effect of apigenin on pharmacokinetics of imatinib and its metabolite N-desmethyl imatinib in rats.

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Liu XY, Xu T, Li WS, Luo J, Geng PW, Wang L, Xia MM, Chen MC, Yu L, Hu GX

The effect of apigenin on pharmacokinetics of imatinib and its metabolite N-desmethyl imatinib in rats.

Biomed Res Int. 2013;2013:789184. doi: 10.1155/2013/789184. Epub 2013 Nov 28.

PubMed ID

24369535 [ View in PubMed

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Abstract

The purpose of this study was to determine the effect of apigenin on the pharmacokinetics of imatinib and N-desmethyl imatinib in rats. Healthy male SD rats were randomly divided into four groups: A group (the control group), B group (the long-term administration of 165 mg/kg apigenin for 15 days), C group (a single dose of 165 mg/kg apigenin), and D group (a single dose of 252 mg/kg apigenin). The serum concentrations of imatinib and N-desmethyl imatinib were measured by HPLC, and pharmacokinetic parameters were calculated using DAS 3.0 software. The parameters of AUC(0-t), AUC(0-infinity), Tmax, V(z)/F, and CL(z)/F for imatinib in group B were different from those in group A (P < 0.05). Besides, MRT(0-t) and MRT(0-infinity) in groups C and D differed distinctly from those in group A as well. The parameters of AUC(0-t) and Cmax for N-desmethyl imatinib in group C were significantly lower than those in group A (P < 0.05); however, compared with groups B and D, the magnitude of effect was modest. Those results indicated that apigenin in the short-term study inhibited the metabolism of imatinib and its metabolite N-desmethyl imatinib, while in the long-term study the metabolism could be accelerated.

DrugBank Data that Cites this Article

Drug Enzymes

Drug	Enzyme	Kind	Organism	Pharmacological Action	Actions
Imatinib	Cytochrome P450 1A2	Protein	Humans	No	Substrate	Details