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• W2086013018 abstract "The purpose of this study was to establish a novel in vitro method for screening reversibility of P-glycoprotein (P-gp) inhibitors. Caco-2 cells with 21 days of cultivation were used as an in vitro model. Transport of rhodamine 123 in the presence of various inhibitors and after removing of inhibitors was determined. Transport of rhodamine 123 at 4 °C and in the secretory direction assured that Caco-2 cells exhibited P-gp function at all time of experiment. The apparent permeability coefficient (Papp) of rhodamine 123 in the presence of verapamil, cyclosporin A, ritonavir, quinidine, N-ethylmaleimide, Cremophor® EL, Tween 80 and poly(acrylic acid)-cysteine-2-mercaptonicotinic acid (PAA-cys-2MNA) was 2.3-, 3.8-, 2.3-, 3.1, 7.5-, 2.1-, 2.9- and 2.5-fold higher than Papp of rhodamine 123 alone. After removing of the inhibitors, Papp decreased to the same range of control except in the case of N-ethylmaleimide which was 2.4-fold higher than the control. These results revealed a reversible inhibition of verapamil, cyclosporin A, ritonavir, quinidine, Cremophor® EL, Tween 80 and PAA-cys-2MNA and an irreversible inhibition of N-ethylmaleimide for P-gp. Thus, this novel established that in vitro method might be an effective tool for screening the reversibility of inhibition of P-gp inhibitors." @default.
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• W2086013018 date "2010-11-01" @default.
• W2086013018 modified "2023-09-26" @default.
• W2086013018 title "405 A mass balance study to investigate the metabolism, excretion and pharmacokinetics of [14C]-olaparib (AZD2281) in patients with advanced solid tumours refractory to standard treatments" @default.
• W2086013018 doi "https://doi.org/10.1016/s1359-6349(10)72112-1" @default.
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