| Attributes | Values |
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| rdf:type
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| http://linked.open...gbank/description
| - Sofosbuvir is a prodrug nucleotide analog used as part of combination therapy to treat hepatitis C virus (HCV) infection or to treat co-infection of HIV and HCV. After metabolism to the active antiviral agent 2'-deoxy-2'-α-fluoro-β-C-methyluridine-5'-triphosphate (also known as GS-461203), the triphosphate serves as a defective substrate for the NS5B protein, an RNA-dependent RNA polymerase required for replication of viral RNA. Sofosbuvir and other nucleotide inhibitors of the HCV RNA polymerase exhibit a very high barrier to resistance development. This is an important advantage relative to HCV drugs that target other viral enzymes such as the protease, for which rapid resistance development has proved to be an important cause of therapeutic failure. More recently, sofosbuvir has become available as a fixed dose drug combination product with levipasvir (tradename Harvoni) used for the treatment of chronic Hepatitis C, an infectious liver disease caused by infection with Hepatitis C Virus (HCV). Approved in October 2014 by the FDA, ledipasvir and sofosbuvir are direct-acting antiviral agents indicated for the treatment of HCV genotype 1 with or without cirrhosis. HCV is a single-stranded RNA virus that is categorized into nine distinct genotypes, with genotype 1 being the most common in the United States affecting 72% of all chronic HCV patients. Prior to development of this drug, the main treatment available was weekly injections of pegylated interferon with weight-based ribavirin over 48 weeks, which achieved a sustained virological response (SVR) of 45-50% and had multiple unpleasant side effects. When combined together, ledipasvir and sofosbuvir have been shown to have a SVR between 93 and 100% after 12 weeks of treatment. Its use has also proven successful in the treatment of HCV in patients co-infected with HIV. (en)
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| http://linked.open...y/drugbank/dosage
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| http://linked.open...generalReferences
| - # Asselah T: Sofosbuvir for the treatment of hepatitis C virus. Expert Opin Pharmacother. 2014 Jan;15(1):121-30. doi: 10.1517/14656566.2014.857656. Epub 2013 Nov 30. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/24289735 # Fung A, Jin Z, Dyatkina N, Wang G, Beigelman L, Deval J: Efficiency of incorporation and chain termination determines the inhibition potency of 2'-modified nucleotide analogs against hepatitis C virus polymerase. Antimicrob Agents Chemother. 2014 Jul;58(7):3636-45. doi: 10.1128/AAC.02666-14. Epub 2014 Apr 14. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/24733478 # Carey L: What is the role of sofosbuvir in treating hepatitis C infection? JAAPA. 2015 Feb;28(2):16-9. doi: 10.1097/01.JAA.0000459818.09661.c0. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/25621961 # Molina JM, Orkin C, Iser DM, Zamora FX, Nelson M, Stephan C, Massetto B, Gaggar A, Ni L, Svarovskaia E, Brainard D, Subramanian GM, McHutchison JG, Puoti M, Rockstroh JK: Sofosbuvir plus ribavirin for treatment of hepatitis C virus in patients co-infected with HIV (PHOTON-2): a multicentre, open-label, non-randomised, phase 3 study. Lancet. 2015 Mar 21;385(9973):1098-106. doi: 10.1016/S0140-6736(14)62483-1. Epub 2015 Feb 4. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/25659285 (en)
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| http://linked.open...gy/drugbank/group
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| http://linked.open...drugbank/halfLife
| - Sofosbuvir has a terminal half life of 0.4 hours. (en)
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| http://linked.open...ugbank/indication
| - Sofosbuvir is used in combination therapy to treat chronic hepatitis C virus (HCV) infected patients with HCV genoptype 1,2,3, or 4, and to treat HCV and HIV co-infected patients. The combination therapy includes either ribavirin alone or ribavirin and peg-interferon alfa. (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
| - Sofosbuvir is nucleotide analog inhibitor, which specifically inhibits HCV NS5B polymerase. Sofosbuvir prevents HCV viral replication by binding to the two Mg2+ ions present in HCV NS5B polymerase's GDD active site motif. (en)
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| http://linked.open...y/drugbank/patent
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| http://linked.open...outeOfElimination
| - Sofosbuvir is eliminated by three routes: urine ( 80%), feces (14%), and respiration (2.5%); however, elimination through the kidneys is the major route. (en)
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| http://linked.open.../drugbank/synonym
| - S)-Isopropyl 2-((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4- dihydropyrimidin-1(2H)-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-yl)methoxy)- (phenoxy)phosphorylamino)propanoate (en)
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| http://linked.open...drugbank/toxicity
| - Sofosbuvir, as a single agent, has very mild toxicity. The most common adverse reactions are headache and fatigue. (en)
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| http://linked.open...umeOfDistribution
| - The volume of distribution for sofosbuvir has yet to be determined. (en)
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| http://linked.open.../drug/hasAHFSCode
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| http://linked.open...k/foodInteraction
| - Sofosbuvir can be given with or without food. (en)
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| http://linked.open.../drugbank/mixture
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| http://linked.open...nk/proteinBinding
| - Sofosbuvir is approximately 61-65% bound to human plasma proteins. (en)
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| http://linked.open...ynthesisReference
| - Sofia MJ, Bao D, Chang W, Du J, Nagarathnam D, Rachakonda S, Reddy PG, Ross BS, Wang P, Zhang HR, Bansal S, Espiritu C, Keilman M, Lam AM, Steuer HM, Niu C, Otto MJ, Furman PA: Discovery of a beta-d-2'-deoxy-2'-alpha-fluoro-2'-beta-C-methyluridine nucleotide prodrug (PSI-7977) for the treatment of hepatitis C virus. J Med Chem. 2010 Oct 14;53(19):7202-18 (en)
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| foaf:page
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| http://linked.open...ugbank/IUPAC-Name
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| 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...logy/drugbank/pKa
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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
| - When given orally, sofosbuvir reaches its maximum plasma concentration in about 0.5 to 2 hours. (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...drugbank/category
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| http://linked.open...rugbank/clearance
| - The clearance of sofosbuvir has yet to be determined. (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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