A functional model for feline P‐glycoprotein |
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| Authors: | C D van Beusekom R Lange J A Schrickx |
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| Affiliation: | Faculty of Veterinary Medicine, Institute for Risk Assessment Sciences, Veterinary Pharmacology, Pharmacotherapy and Toxicology, Utrecht, The Netherlands |
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| Abstract: | P‐gp (ABCB1) belongs to the group of export transporters that is expressed in various species at biological barriers. Inhibition of P‐gp can lead to changes in pharmacokinetics of drugs (drug–drug interactions), which can lead to toxicity and adverse side effects. This study aimed to establish a functional assay to measure the inhibitory potential of veterinary drugs on feline P‐gp by means of fluorescence‐associated flow cytometry of feline lymphoma cells. In this model, PSC833 and ivermectin potently inhibited P‐gp function; cyclosporine and verapamil moderately inhibited P‐gp function, whereas ketoconazole, itraconazole, diazepam, and its metabolites had no effect on P‐gp function. This model can be used for testing the inhibitory potency of (new) drugs on feline P‐gp. |
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