Interaction of the antiviral drug telaprevir with renal and hepatic drug transporters

Kunze, A. and Huwyler, J. and Camenisch, G. and Gutmann, H.. (2012) Interaction of the antiviral drug telaprevir with renal and hepatic drug transporters. Biochemical pharmacology, Vol. 84, Issue 8. pp. 1096-1102.

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Official URL: http://edoc.unibas.ch/dok/A6043713

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Telaprevir is a new, direct-acting antiviral drug that has been approved for the treatment of chronic hepatitis C viral infection. First data on drug-drug interactions with co-medications such as cyclosporine, tacrolimus and atorvastatin have been reported recently. Drug transporting proteins have been shown to play an important role in clinically observed drug-drug interactions. The aim of this study was therefore to systematically investigate the potential of telaprevir to inhibit drug transporting proteins. The effect of telaprevir on substrate uptake mediated by drug transporters located in human kidney and liver was investigated on a functional level in HEK293 cell lines that over-express single transporter. Telaprevir was shown to exhibit significant inhibition of the human renal drug transporters OCT2 and MATE1 with IC(50) values of 6.4muM and 23.0muM, respectively, whereas no inhibitory effect on OAT1 and OAT3 mediated transport by telaprevir was demonstrated. Liver drug transporters were inhibited with an IC(50) of 2.2muM for OATP1B1, 6.8muM for OATP1B3 and 20.7muM for OCT1. Our data show that telaprevir exhibited significant potential to inhibit human drug transporters. In view of the inhibitory potential of telaprevir, clinical co-administration of telaprevir together with drugs that are substrates of renal or hepatic transporters should be carefully monitored.
Faculties and Departments:05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Pharmazie > Pharmaceutical Technology (Huwyler)
UniBasel Contributors:Huwyler, Jörg
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:Pergamon Press
Note:Publication type according to Uni Basel Research Database: Journal article
Last Modified:04 Jan 2013 08:38
Deposited On:04 Jan 2013 08:35

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