About: pradefovir mesylate     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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http://linked.open...gbank/description
  • Pradefovir mesilate (previously known as MB-06886, Hepavir B and remofovir mesylate) is an orally administered small molecule compound that belongs to a novel series of phosphate and phosphonate prodrugs of adefovir. Adefovir (Hepsera) is an acyclic phosphonate analogue of adenine that is used to treat hepatitis B virus. As adefovir is poorly absorbed and associated with a high level of nephrotoxicity, pradefovir mesilate was designed to specifically target the liver and reduce risks to external tissue, especially the kidneys, while improving results of adefovir. Pradefovir is activated through oxidation that is mediated by cytochrome P-450 (CYP) 3A4, which is predominantly expressed in the liver. The novel prodrug is highly stable in both plasma and tissues and demonstrated potent preclinical and clinical anti-HBV activity. Pradefovir is undergoing phase II development for the treatment of chronic hepatitis B. (en)
http://linked.open...generalReferences
  • # Reddy KR, Matelich MC, Ugarkar BG, Gomez-Galeno JE, Dare J, Ollis K, Sun Z, Craigo W, Colby TJ, Fujitaki JM, Boyer SH, van Poelje PD, Erion MD: Pradefovir: A Prodrug That Targets Adefovir to the Liver for the Treatment of Hepatitis B. J Med Chem. 2008 Jan 4;. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18173234 # Tillmann HL: Pradefovir, a liver-targeted prodrug of adefovir against HBV infection. Curr Opin Investig Drugs. 2007 Aug;8(8):682-90. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17668370 # Lin CC, Fang C, Benetton S, Xu GF, Yeh LT: Metabolic activation of pradefovir by CYP3A4 and its potential as an inhibitor or inducer. Antimicrob Agents Chemother. 2006 Sep;50(9):2926-31. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16940083 # Lin CC, Xu C, Teng A, Yeh LT, Peterson J: Pharmacokinetics of pradefovir and PMEA in healthy volunteers after oral dosing of pradefovir. J Clin Pharmacol. 2005 Nov;45(11):1250-8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16239358 (en)
http://linked.open...gy/drugbank/group
  • investigational (en)
http://linked.open...ugbank/indication
  • Investigated for use as a prodrug for Hepsera in treating hepatitis (viral, B). (en)
sameAs
Title
  • pradefovir mesylate (en)
adms:identifier
http://linked.open...mechanismOfAction
  • Pradefovir is activated through oxidation that is mediated by cytochrome P-450 (CYP) 3A4, which is predominantly expressed in the liver. In this way, it allows for increased Hepsera concentrations selectively in the liver. (en)
http://linked.open...drugbank/toxicity
  • Good safety profile. (en)
http://linked.open...ugbank/IUPAC-Name
http://linked.open...gy/drugbank/InChI
http://linked.open...Molecular-Formula
http://linked.open.../Molecular-Weight
http://linked.open...noisotopic-Weight
http://linked.open...y/drugbank/SMILES
http://linked.open...ogy/drugbank/logP
http://linked.open...nd-Acceptor-Count
http://linked.open...-Bond-Donor-Count
http://linked.open...drugbank/InChIKey
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http://linked.open...nk/Polarizability
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http://linked.open...nk/MDDR-Like-Rule
http://linked.open...k/Number-of-Rings
http://linked.open...siological-Charge
http://linked.open...bank/Rule-of-Five
http://linked.open...tional-IUPAC-Name
http://linked.open...strongest-acidic-
http://linked.open...-strongest-basic-
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