title: Telaprevir: pharmacokinetics and drug interactions.
abstract: 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.
authors.affiliation: Vertex Pharmaceuticals Incorporated, Cambridge, MA, USA. varun_garg@vrtx.com
authors.forename: Varun
authors.initials: V
authors.lastname: Garg
authors.forename: Robert S
authors.initials: RS
authors.lastname: Kauffman
authors.forename: Maria
authors.initials: M
authors.lastname: Beaumont
authors.forename: Rolf P G
authors.initials: RP
authors.lastname: van Heeswijk
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000008:administration & dosage / Q000378:metabolism / Q000493:pharmacokinetics*; D002986:Clinical Trials as Topic; D051544:Cytochrome P-450 CYP3A / Q000378:metabolism; D065692:Cytochrome P-450 CYP3A Inhibitors; D004347:Drug Interactions; D004359:Drug Therapy, Combination; D016174:Hepacivirus / Q000472:pathogenicity; D019698:Hepatitis C, Chronic / Q000188:drug therapy / Q000378:metabolism / Q000821:virology; D006801:Humans; D016898:Interferon-alpha / Q000008:administration & dosage / Q000494:pharmacology; D007654:Ketoconazole / Q000494:pharmacology; D009842:Oligopeptides / Q000008:administration & dosage / Q000378:metabolism / Q000493:pharmacokinetics*; D011092:Polyethylene Glycols / Q000008:administration & dosage / Q000494:pharmacology; D011480:Protease Inhibitors / Q000378:metabolism / Q000493:pharmacokinetics; D012254:Ribavirin / Q000494:pharmacology; D017361:Viral Nonstructural Proteins / Q000037:antagonists & inhibitors; D012697:Serine Endopeptidases; D043583:Nucleoside-Triphosphatase; D053487:DEAD-box RNA Helicases; D000085242:Viral Proteases
chemical_list: D000998:Antiviral Agents; D051544:Cytochrome P-450 CYP3A; D065692:Cytochrome P-450 CYP3A Inhibitors; D016898:Interferon-alpha; D007654:Ketoconazole; D009842:Oligopeptides; D011092:Polyethylene Glycols; D011480:Protease Inhibitors; D012254:Ribavirin; D017361:Viral Nonstructural Proteins; C084422:NS3 protein, hepatitis C virus; D012697:Serine Endopeptidases; D043583:Nucleoside-Triphosphatase; D053487:DEAD-box RNA Helicases; D000085242:Viral Proteases; C486464:telaprevir; C104464:CYP3A protein, human