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Namespace Prefixes

PrefixIRI
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dctermshttp://purl.org/dc/terms/
n21http://linked.opendata.cz/resource/AHFS/
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n11http://linked.opendata.cz/resource/drugbank/dosage/
n14http://linked.opendata.cz/resource/drugbank/drug/DB06402/identifier/national-drug-code-directory/
n10http://www.rxlist.com/
n9http://bio2rdf.org/drugbank:
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n15http://linked.opendata.cz/resource/drugbank/drug/DB06402/identifier/chebi/
n5http://linked.opendata.cz/resource/drugbank/patent/
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owlhttp://www.w3.org/2002/07/owl#
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n17http://linked.opendata.cz/resource/drugbank/drug/DB06402/identifier/wikipedia/
n7http://www.drugs.com/cdi/
n4http://linked.opendata.cz/resource/drugbank/property/
xsdhhttp://www.w3.org/2001/XMLSchema#
n19http://linked.opendata.cz/resource/atc/
n18http://linked.opendata.cz/ontology/sukl/drug/

Statements

Subject Item
n2:DB06402
rdf:type
n3:Drug
n3:description
Telavancin is a semi-synthetic derivative of vanocymycin that has bactericidal activity against Methicillin-resistant Staphylococcus aureus (MRSA is an important pathogen causing hospital-acquired pneumonia (HAP) worldwide) and other gram-positive bacteria. FDA approved on September 11, 2009.
n3:dosage
n11:271B4C63-363D-11E5-9242-09173F13E4C5 n11:271B4C64-363D-11E5-9242-09173F13E4C5 n11:271B4C65-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Laohavaleeson S, Kuti JL, Nicolau DP: Telavancin: a novel lipoglycopeptide for serious gram-positive infections. Expert Opin Investig Drugs. 2007 Mar;16(3):347-57. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17302529 # Rubinstein E, Corey GR, Stryjewski ME, Kanafani ZA: Telavancin for the treatment of serious gram-positive infections, including hospital acquired pneumonia. Expert Opin Pharmacother. 2011 Dec;12(17):2737-50. doi: 10.1517/14656566.2011.633511. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/22077833 # Zhanel GG, Calic D, Schweizer F, Zelenitsky S, Adam H, Lagace-Wiens PR, Rubinstein E, Gin AS, Hoban DJ, Karlowsky JA: New lipoglycopeptides: a comparative review of dalbavancin, oritavancin and telavancin. Drugs. 2010 May 7;70(7):859-86. doi: 10.2165/11534440-000000000-00000. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/20426497 # Wong SL, Goldberg MR, Ballow CH, Kitt MM, Barriere SL: Effect of Telavancin on the pharmacokinetics of the cytochrome P450 3A probe substrate midazolam: a randomized, double-blind, crossover study in healthy subjects. Pharmacotherapy. 2010 Feb;30(2):136-43. doi: 10.1592/phco.30.2.136. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/20099988
n3:group
approved
n3:halfLife
Terminal elimination half-life = 8 ± 1.5 hours (with normal renal function)
n3:indication
Treatment of complicated skin infections caused by gram-positive bacteria like methicillin-susceptible or -resistant Staphylococcus aureus, vancomycin-susceptible Enterococcus faecalis, and Streptococcus pyogenes, Streptococcus agalactiae, or Streptococcus anginosus group.
owl:sameAs
n9:DB06402
dcterms:title
Telavancin
adms:identifier
n13:D06057 n14:0469-3575-50 n15:71226 n16:DB06402 n17:Telavancin
n3:mechanismOfAction
Telavancin is a bactericidal lipoglycopeptide that is active against a broad range of gram-positive bacteria. Telavancin prevents polymerization of N-acetylmuramic acid (NAM) and N-acetylglucosamine (NAG) and cross-linking of peptidoglycan by binding to D-Ala-D-Ala. As a result, inhibition of bacterial cell wall synthesis occurs. Furthermore, telavancin disrupts membrane potential and cell permeability as a result of the lipophillic side chain moiety. This additional bactericidal mechanism is what sets telavancin apart from vancomycin.
n3:patent
n5:7531623 n5:7208471
n3:routeOfElimination
Urine with >80% as unchanged drug and <20% as hydroxylated metabolites (with dose of 10mg/kg); Feces (<1%)
n3:synonym
TD-6424 Vibativ
n3:volumeOfDistribution
Vss, healthy subjects, 10 mg/kg = 0.14 L/kg
n18:hasAHFSCode
n21:8-12-28-16
n3:proteinBinding
>90% to serum albumin in a concentration independent manner (despite being highly protein bound, antimicrobial activity of telavancin is not affected)
n3:salt
foaf:page
n7:telavancin.html n10:vibativ-drug.htm
n3:IUPAC-Name
n4:271B4C6A-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B4C70-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B4C6F-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B4C6C-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B4C6D-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B4C6E-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B4C68-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B4C66-363D-11E5-9242-09173F13E4C5 n4:271B4C69-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B4C67-363D-11E5-9242-09173F13E4C5
n18:hasATCCode
n19:J01XA03
n3:H-Bond-Acceptor-Count
n4:271B4C76-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B4C77-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B4C71-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B4C72-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B4C74-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B4C73-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B4C75-363D-11E5-9242-09173F13E4C5
n3:absorption
Telavancin demonstrates linear pharmacokinetics at doses between 1 and 12.5 mg/kg. Furthermore, 24 hours post-infusion of a dose of 7.5 to 15 mg/kg, activity against MRSA and penicillin-resistant Streptococcus pneumonia can still be observed. The trough concentration at this point of time is approximately 10 μg/mL. Telavancin also has poor bioavailability and must be administered over 30-120 minutes IV. Cmax, healthy subjects, 10 mg/kg = 93.6 ± 14.2 μg/mL; AUC (0- ∞), healthy subjects, 10 mg/kg = 747 ± 129 μg · h/mL; AUC (0-24h), healthy subjects, 10 mg/kg = 666± 107 μg · h/mL; Time to steady state = 3 days;
n3:affectedOrganism
Gram-positive Bacteria
n3:casRegistryNumber
372151-71-8
n3:category
n3:clearance
Cl, healthy subjects, 10 mg/kg = 13.9 ± 2.9 mL/h/kg
n3:Bioavailability
n4:271B4C7C-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B4C7E-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B4C7F-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B4C7B-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B4C7A-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B4C7D-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B4C6B-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n4:271B4C78-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B4C79-363D-11E5-9242-09173F13E4C5