| Attributes | Values |
|---|
| rdf:type
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| http://linked.open...gbank/description
| - Telaprevir (VX-950) is a highly selective and potent inhibitor of the HCV NS3-4A serine protease. It is a member of a class of antiviral drugs known as protease inhibitors and is the first hepatitis C drug that has demonstrated activity in patients who have failed prior therapy. On April 28, 2011, the FDA Antiviral Drugs Advisory Committee voted 18-0 to recommend approval telaprevir for people with genotype 1 chronic hepatitis C and was approved in the U.S. in May, 2011. (en)
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| http://linked.open...y/drugbank/dosage
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| http://linked.open...generalReferences
| - # Kim JJ, Culley CM, Mohammad RA: Telaprevir: An oral protease inhibitor for hepatitis C virus infection. Am J Health Syst Pharm. 2012 Jan 1;69(1):19-33. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/22180548 # Liu-Young G, Kozal MJ: Hepatitis C protease and polymerase inhibitors in development. AIDS Patient Care STDS. 2008 Jun;22(6):449-57. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18479202 # Forestier N, Zeuzem S: Telaprevir for the treatment of hepatitis C. Expert Opin Pharmacother. 2012 Mar;13(4):593-606. doi: 10.1517/14656566.2012.660524. Epub 2012 Feb 15. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/22332992 # Garg V, Kauffman RS, Beaumont M, van Heeswijk RP: Telaprevir: pharmacokinetics and drug interactions. Antivir Ther. 2012;17(7):1211-21. doi: 10.3851/IMP2356. Epub 2012 Sep 7. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/22954756 (en)
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| http://linked.open...gy/drugbank/group
| |
| http://linked.open...drugbank/halfLife
| - The mean elimination half-life after single-dose oral administration of telaprevir 750 mg typically ranged from about 4.0 to 4.7 hours. At steady state, the effective half-life is about 9 to 11 hours. (en)
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| http://linked.open...ugbank/indication
| - Treating chronic hepatitis C virus (genotype 1) infection in patients with compensated liver (due to liver diseases like cirrhosis) that are treatment naive or have failed therapy with interferons (either null or partial responders and treatment relapsers). (en)
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| sameAs
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| Title
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| adms:identifier
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| http://linked.open...mechanismOfAction
| - Telaprevir is an inhibitor of the HCV NS3/4A serine protease, necessary for the proteolytic cleavage of the HCV encoded polyprotein into mature forms of the NS4A, NS4B, NS5A and NS5B proteins and essential for viral replication. It belongs to the chemical class of alpha-ketoamids and binds to NS3/4A in a covalent but reversible manner. (en)
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| http://linked.open...y/drugbank/patent
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| http://linked.open...outeOfElimination
| - Following administration of a single oral dose of 750 mg 14C-telaprevir in healthy subjects, 90% of total radioactivity was recovered in feces, urine and expired air within 96 hours post-dose. The median recovery of the administered radioactive dose was approximately 82% in the feces, 9% in exhaled air and 1% in urine. The contribution of unchanged 14C-telaprevir and the R-diastereomer of telaprevir towards total radioactivity recovered in feces was 31.9% and 18.8%, respectively. (en)
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| http://linked.open.../drugbank/synonym
| - Incivek (en)
- MP-424 (en)
- VX-950 (en)
- VX 950 (en)
- (1S,3AR,6as)-(2S)-2-cyclohexyl-N-(pyrazinylcarbonyl)glycyl-3-methyl-L-valyl-N-((1S)-1-((cyclopropylamino)oxoacetyl)butyl)octahydrocyclopenta(c)pyrrole-1-carboxamide (en)
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| http://linked.open...drugbank/toxicity
| - The highest documented dose administered is 1875 mg every 8 hours for 4 days in healthy subjects with telaprevir alone. In that study, the following common adverse events were reported more frequently with the 1875 mg q8h regimen compared to the 750 mg q8h regimen: nausea, headache, diarrhea, decreased appetite, dysgeusia, and vomiting. The two most common adverse events that caused the discontinuation of treatment are anemia and rash. (en)
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| http://linked.open...umeOfDistribution
| - Apparent volume of distribution (Vd/F) = 252 L. This large volume of distribution suggests extensive penetration into tissues. (en)
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| http://linked.open.../drug/hasAHFSCode
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| http://linked.open...k/foodInteraction
| - St. John's wort is a CYP3A4 inducer which will decrease levels of telaprevir. (en)
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| http://linked.open...nk/proteinBinding
| - 59% to 76% and binds to alpha 1-acid glycoprotein and albumin in a concentration dependent manner. (en)
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| http://linked.open...ynthesisReference
| - Znabet A, Polak MM, Janssen E, de Kanter FJ, Turner NJ, Orru RV, Ruijter E. A highly efficient synthesis of telaprevir by strategic use of biocatalysis and multicomponent reactions. Chem Commun (Camb). 2010 Nov 14;46(42):7918-20. Epub 2010 Sep 20. (en)
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| http://linked.open...y/mesh/hasConcept
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| foaf:page
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| http://linked.open...ugbank/IUPAC-Name
| |
| http://linked.open...gy/drugbank/InChI
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| http://linked.open...Molecular-Formula
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| http://linked.open.../Molecular-Weight
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| http://linked.open...noisotopic-Weight
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| http://linked.open...y/drugbank/SMILES
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| http://linked.open.../Water-Solubility
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| http://linked.open...ogy/drugbank/logP
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| http://linked.open...ogy/drugbank/logS
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| http://linked.open...l/drug/hasATCCode
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| http://linked.open...nd-Acceptor-Count
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| http://linked.open...-Bond-Donor-Count
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| http://linked.open...drugbank/InChIKey
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| http://linked.open...urface-Area--PSA-
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| http://linked.open...nk/Polarizability
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| http://linked.open...bank/Refractivity
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| http://linked.open...atable-Bond-Count
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| http://linked.open...ugbank/absorption
| - Telaprevir is orally available, most likely absorbed in the small intestine, with no evidence for absorption in the colon. Maximum plasma concentrations after a single dose of telaprevir are generally achieved after 4 to 5 hours. In vitro studies performed with human Caco-2 cells indicated that telaprevir is a substrate of P-glycoprotein (P-gp). Exposure to telaprevir is higher during co-administration of peginterferon alfa and ribavirin than after administration of telaprevir alone. Dissolution of telaprevir is not dependent by pH. (en)
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| http://linked.open.../affectedOrganism
| - Hepatitis C virus, RSV and other RNA/DNA viruses (en)
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| http://linked.open...casRegistryNumber
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| http://linked.open...rugbank/clearance
| - After oral administration, the apparent total clearance (Cl/F) was estimated to be 32.4 L/h with an inter-individual variability of 27.2%. (en)
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| http://linked.open...k/Bioavailability
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| http://linked.open...bank/Ghose-Filter
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| http://linked.open...nk/MDDR-Like-Rule
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| http://linked.open...k/Number-of-Rings
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| http://linked.open...siological-Charge
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| http://linked.open...bank/Rule-of-Five
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| http://linked.open...tional-IUPAC-Name
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| http://linked.open...strongest-acidic-
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| http://linked.open...-strongest-basic-
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