Telaprevir: Pharmacokinetics and Drug Interactions
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 bioavail...
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Veröffentlicht in: | Antiviral Therapy 2012-01, Vol.17 (7), p.1211-1221 |
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description | 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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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.</description><identifier>ISSN: 1359-6535</identifier><identifier>EISSN: 2040-2058</identifier><identifier>DOI: 10.3851/IMP2356</identifier><identifier>PMID: 22954756</identifier><language>eng</language><publisher>London, England: SAGE Publications</publisher><subject>Animals ; Antibiotics. Antiinfectious agents. Antiparasitic agents ; Antiviral agents ; Antiviral Agents - administration & dosage ; Antiviral Agents - metabolism ; Antiviral Agents - pharmacokinetics ; Biological and medical sciences ; Clinical Trials as Topic ; Cytochrome P-450 CYP3A - metabolism ; Cytochrome P-450 CYP3A Inhibitors ; Drug Interactions ; Drug Therapy, Combination ; Hepacivirus - pathogenicity ; Hepatitis C, Chronic - drug therapy ; Hepatitis C, Chronic - metabolism ; Hepatitis C, Chronic - virology ; Humans ; Interferon-alpha - administration & dosage ; Interferon-alpha - pharmacology ; Ketoconazole - pharmacology ; Medical sciences ; Oligopeptides - administration & dosage ; Oligopeptides - metabolism ; Oligopeptides - pharmacokinetics ; Pharmacology. Drug treatments ; Polyethylene Glycols - administration & dosage ; Polyethylene Glycols - pharmacology ; Protease Inhibitors - metabolism ; Protease Inhibitors - pharmacokinetics ; Ribavirin - pharmacology ; Viral Nonstructural Proteins - antagonists & inhibitors</subject><ispartof>Antiviral Therapy, 2012-01, Vol.17 (7), p.1211-1221</ispartof><rights>2012 SAGE Publications</rights><rights>2014 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c439t-53d49dbc0143dd9adf9cea7bf1515a084c737ff9256c8092497d7b87ee385aec3</citedby><cites>FETCH-LOGICAL-c439t-53d49dbc0143dd9adf9cea7bf1515a084c737ff9256c8092497d7b87ee385aec3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://journals.sagepub.com/doi/pdf/10.3851/IMP2356$$EPDF$$P50$$Gsage$$H</linktopdf><linktohtml>$$Uhttps://journals.sagepub.com/doi/10.3851/IMP2356$$EHTML$$P50$$Gsage$$H</linktohtml><link.rule.ids>313,314,780,784,792,21966,27853,27922,27924,27925,44945,45333</link.rule.ids><linktorsrc>$$Uhttps://journals.sagepub.com/doi/full/10.3851/IMP2356?utm_source=summon&utm_medium=discovery-provider$$EView_record_in_SAGE_Publications$$FView_record_in_$$GSAGE_Publications</linktorsrc><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=26735932$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/22954756$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Garg, Varun</creatorcontrib><creatorcontrib>Kauffman, Robert S</creatorcontrib><creatorcontrib>Beaumont, Maria</creatorcontrib><creatorcontrib>van Heeswijk, Rolf PG</creatorcontrib><title>Telaprevir: Pharmacokinetics and Drug Interactions</title><title>Antiviral Therapy</title><addtitle>Antivir Ther</addtitle><description>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.</description><subject>Animals</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Antiviral agents</subject><subject>Antiviral Agents - administration & dosage</subject><subject>Antiviral Agents - metabolism</subject><subject>Antiviral Agents - pharmacokinetics</subject><subject>Biological and medical sciences</subject><subject>Clinical Trials as Topic</subject><subject>Cytochrome P-450 CYP3A - metabolism</subject><subject>Cytochrome P-450 CYP3A Inhibitors</subject><subject>Drug Interactions</subject><subject>Drug Therapy, Combination</subject><subject>Hepacivirus - pathogenicity</subject><subject>Hepatitis C, Chronic - drug therapy</subject><subject>Hepatitis C, Chronic - metabolism</subject><subject>Hepatitis C, Chronic - virology</subject><subject>Humans</subject><subject>Interferon-alpha - administration & dosage</subject><subject>Interferon-alpha - pharmacology</subject><subject>Ketoconazole - pharmacology</subject><subject>Medical sciences</subject><subject>Oligopeptides - administration & dosage</subject><subject>Oligopeptides - metabolism</subject><subject>Oligopeptides - pharmacokinetics</subject><subject>Pharmacology. Drug treatments</subject><subject>Polyethylene Glycols - administration & dosage</subject><subject>Polyethylene Glycols - pharmacology</subject><subject>Protease Inhibitors - metabolism</subject><subject>Protease Inhibitors - pharmacokinetics</subject><subject>Ribavirin - pharmacology</subject><subject>Viral Nonstructural Proteins - antagonists & inhibitors</subject><issn>1359-6535</issn><issn>2040-2058</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2012</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpl0DtPwzAQwHELgWgpiG-AMoBgCfgZx2yovCoV0aHM0cV2SkoexU6Q-PYYNcDAdMtPd7o_QscEX7JUkKvZ04IykeygMcUcxxSLdBeNCRMqTgQTI3Tg_RpjmiqM99GIUiW4FMkY0aWtYOPsR-muo8UruBp0-1Y2tiu1j6Ax0a3rV9Gs6awD3ZVt4w_RXgGVt0fDnKCX-7vl9DGePz_MpjfzWHOmulgww5XJNSacGaPAFEpbkHlBBBGAU64lk0WhqEh0ihXlShqZp9La8BFYzSboYrt349r33vouq0uvbVVBY9veZ4RIkibhVR7o-ZZq13rvbJFtXFmD-8wIzr4DZUOgIE-GpX1eW_PrfooEcDYA8BqqwkGjS__nEhmiMhrc6dZ5WNls3fauCTH-3fsC_6p3ew</recordid><startdate>20120101</startdate><enddate>20120101</enddate><creator>Garg, Varun</creator><creator>Kauffman, Robert S</creator><creator>Beaumont, Maria</creator><creator>van Heeswijk, Rolf PG</creator><general>SAGE Publications</general><general>International Medical Press</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>20120101</creationdate><title>Telaprevir: Pharmacokinetics and Drug Interactions</title><author>Garg, Varun ; Kauffman, Robert S ; Beaumont, Maria ; van Heeswijk, Rolf PG</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c439t-53d49dbc0143dd9adf9cea7bf1515a084c737ff9256c8092497d7b87ee385aec3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2012</creationdate><topic>Animals</topic><topic>Antibiotics. Antiinfectious agents. Antiparasitic agents</topic><topic>Antiviral agents</topic><topic>Antiviral Agents - administration & dosage</topic><topic>Antiviral Agents - metabolism</topic><topic>Antiviral Agents - pharmacokinetics</topic><topic>Biological and medical sciences</topic><topic>Clinical Trials as Topic</topic><topic>Cytochrome P-450 CYP3A - metabolism</topic><topic>Cytochrome P-450 CYP3A Inhibitors</topic><topic>Drug Interactions</topic><topic>Drug Therapy, Combination</topic><topic>Hepacivirus - pathogenicity</topic><topic>Hepatitis C, Chronic - drug therapy</topic><topic>Hepatitis C, Chronic - metabolism</topic><topic>Hepatitis C, Chronic - virology</topic><topic>Humans</topic><topic>Interferon-alpha - administration & dosage</topic><topic>Interferon-alpha - pharmacology</topic><topic>Ketoconazole - pharmacology</topic><topic>Medical sciences</topic><topic>Oligopeptides - administration & dosage</topic><topic>Oligopeptides - metabolism</topic><topic>Oligopeptides - pharmacokinetics</topic><topic>Pharmacology. Drug treatments</topic><topic>Polyethylene Glycols - administration & dosage</topic><topic>Polyethylene Glycols - pharmacology</topic><topic>Protease Inhibitors - metabolism</topic><topic>Protease Inhibitors - pharmacokinetics</topic><topic>Ribavirin - pharmacology</topic><topic>Viral Nonstructural Proteins - antagonists & inhibitors</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Garg, Varun</creatorcontrib><creatorcontrib>Kauffman, Robert S</creatorcontrib><creatorcontrib>Beaumont, Maria</creatorcontrib><creatorcontrib>van Heeswijk, Rolf PG</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Antiviral Therapy</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>Garg, Varun</au><au>Kauffman, Robert S</au><au>Beaumont, Maria</au><au>van Heeswijk, Rolf PG</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Telaprevir: Pharmacokinetics and Drug Interactions</atitle><jtitle>Antiviral Therapy</jtitle><addtitle>Antivir Ther</addtitle><date>2012-01-01</date><risdate>2012</risdate><volume>17</volume><issue>7</issue><spage>1211</spage><epage>1221</epage><pages>1211-1221</pages><issn>1359-6535</issn><eissn>2040-2058</eissn><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.</abstract><cop>London, England</cop><pub>SAGE Publications</pub><pmid>22954756</pmid><doi>10.3851/IMP2356</doi><tpages>11</tpages><oa>free_for_read</oa></addata></record> |
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subjects | Animals Antibiotics. Antiinfectious agents. Antiparasitic agents Antiviral agents Antiviral Agents - administration & dosage Antiviral Agents - metabolism Antiviral Agents - pharmacokinetics Biological and medical sciences Clinical Trials as Topic Cytochrome P-450 CYP3A - metabolism Cytochrome P-450 CYP3A Inhibitors Drug Interactions Drug Therapy, Combination Hepacivirus - pathogenicity Hepatitis C, Chronic - drug therapy Hepatitis C, Chronic - metabolism Hepatitis C, Chronic - virology Humans Interferon-alpha - administration & dosage Interferon-alpha - pharmacology Ketoconazole - pharmacology Medical sciences Oligopeptides - administration & dosage Oligopeptides - metabolism Oligopeptides - pharmacokinetics Pharmacology. Drug treatments Polyethylene Glycols - administration & dosage Polyethylene Glycols - pharmacology Protease Inhibitors - metabolism Protease Inhibitors - pharmacokinetics Ribavirin - pharmacology Viral Nonstructural Proteins - antagonists & inhibitors |
title | Telaprevir: Pharmacokinetics and Drug Interactions |
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