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Telaprevir: pharmacokinetics and drug interactions

Varun Garg, Robert S Kauffman, Maria Beaumont, Rolf PG van Heeswijk

Corresponding author name: Varun Garg
Corresponding author e-mail: varun_garg@vrtx.com

Citation: Antiviral Therapy 2012; 17:1211-1221
doi: 10.3851/IMP2356

Date accepted: 14 March 2012
Date published online: 07 September 2012


Telaprevir is an inhibitor of the HCV NS3/4A protease. When used in combination with pegylated interferon and ribavirin, telaprevir has demonstrated a substantial increase in sustained virological response compared with pegylated interferon and ribavirin used alone. Telaprevir has good oral bioavailability, which is enhanced when administered with food. Telaprevir is extensively metabolized and primarily eliminated via faeces. No dose adjustment of telaprevir is needed in patients with mild to severe renal impairment or mild liver impairment. Telaprevir is a substrate and inhibitor of cytochrome P450 3A and P-glycoprotein and, thus, might interact with coadministered drugs that affect or are affected by these metabolic/transport pathways. This article reviews the pharmacokinetic and drug interaction profile of telaprevir.


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