Pharmacokinetics Interaction between Imatinib and Genistein in Rats

Abstract EN

The objective of this work was to investigate the effect of orally administered genistein on the pharmacokinetics of imatinib and N-desmethyl imatinib in rats.

Twenty-five healthy male SD (Sprague-Dawley) rats were randomly divided into five groups: A group (control group), B group (multiple dose of 100 mg/kg genistein for consecutive 15 days), C group (multiple dose of 50 mg/kg genistein for consecutive 15 days), D group (a single dose of 100 mg/kg genistein), and E group (a single dose of 50 mg/kg genistein).

A single dose of imatinib is administered orally 30 min after administration of genistein (100 mg/kg or 50 mg/kg).

The pharmacokinetic parameters of imatinib and N-desmethyl imatinib were calculated by DAS 3.0 software.

The multiple dose of 100 mg/kg or 50 mg/kg genistein significantly (P<0.05) decreased the AUC0-t and Cmax of imatinib.

AUC0-t and the Cmax of N-desmethyl imatinib were also increased, but without any significant difference.

However, the single dose of 100 mg/kg or 50 mg/kg genistein has no effect on the pharmacokinetics of imatinib and N-desmethyl imatinib.

Those results indicated that multiple dose of genistein (100 mg/kg or 50 mg/kg) induces the metabolism of imatinib, while single dose of genistein has no effect.