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Namespace Prefixes

PrefixIRI
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n17http://linked.opendata.cz/resource/drugbank/drug/DB06817/identifier/drugbank/
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Statements

Subject Item
n2:DB06817
rdf:type
n3:Drug
n3:description
Raltegravir is an antiretroviral drug produced by Merck & Co., used to treat HIV infection. It received approval by the U.S. Food and Drug Administration (FDA) on 12 October 2007, the first of a new class of HIV drugs, the integrase inhibitors, to receive such approval. [Wikipedia]
n3:dosage
n7:271B5587-363D-11E5-9242-09173F13E4C5 n7:271B5588-363D-11E5-9242-09173F13E4C5 n7:271B5589-363D-11E5-9242-09173F13E4C5 n7:271B558A-363D-11E5-9242-09173F13E4C5 n7:271B558B-363D-11E5-9242-09173F13E4C5 n7:271B558C-363D-11E5-9242-09173F13E4C5 n7:271B5586-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Nachman S, Zheng N, Acosta E, Teppler H, Homony B, Graham B, Fenton T, Xu X, Wenning L, Spector SA, Frenkel LM, Alvero C, Worrell C, Handelsman E, Wiznia A: Pharmacokinetics, Safety and 48 Week Efficacy of Oral Raltegravir in Human Immunodeficiency Virus type-1 (HIV) infected Children 2 through 18 years of Age. Clin Infect Dis. 2013 Oct 21. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/24145879 # Barau C, Furlan V, Yazdanpanah Y, Fagard C, Molina JM, Taburet AM, Barrail-Tran A: Characterization of binding of raltegravir to plasma proteins. Antimicrob Agents Chemother. 2013 Oct;57(10):5147-50. doi: 10.1128/AAC.00625-13. Epub 2013 Jul 15. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23856784 # Arora R, de Beauchene IC, Polanski J, Laine E, Tchertanov L: Raltegravir flexibility and its impact on recognition by the HIV-1 IN targets. J Mol Recognit. 2013 Sep;26(9):383-401. doi: 10.1002/jmr.2277. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23836466 # Eron JJ, Cooper DA, Steigbigel RT, Clotet B, Gatell JM, Kumar PN, Rockstroh JK, Schechter M, Markowitz M, Yeni P, Loutfy MR, Lazzarin A, Lennox JL, Strohmaier KM, Wan H, Barnard RJ, Nguyen BY, Teppler H: Efficacy and safety of raltegravir for treatment of HIV for 5 years in the BENCHMRK studies: final results of two randomised, placebo-controlled trials. Lancet Infect Dis. 2013 Jul;13(7):587-96. doi: 10.1016/S1473-3099(13)70093-8. Epub 2013 May 7. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23664333 # Winston A, Mallon PW, Boffito M: The clinical pharmacology of antiretrovirals in development. Expert Opin Drug Metab Toxicol. 2006 Jun;2(3):447-58. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16863445 # O'Neal R: MK-0518 and GS-9137: two promising integrase inhibitors in the pipeline. BETA. 2006 Summer;18(4):13-6. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17019786 # James JS: Integrase inhibitor MK-0518: Merck opens expanded-access program. AIDS Treat News. 2006 Jul-Sep;(419):5. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17096488 # Markowitz M, Morales-Ramirez JO, Nguyen BY, Kovacs CM, Steigbigel RT, Cooper DA, Liporace R, Schwartz R, Isaacs R, Gilde LR, Wenning L, Zhao J, Teppler H: Antiretroviral activity, pharmacokinetics, and tolerability of MK-0518, a novel inhibitor of HIV-1 integrase, dosed as monotherapy for 10 days in treatment-naive HIV-1-infected individuals. J Acquir Immune Defic Syndr. 2006 Dec 15;43(5):509-15. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17133211 # Colquitt AR, Pham PA: Expanded access drug profile: raltegravir (RAL, MK-0518). Hopkins HIV Rep. 2007 Jan;19(1):11-2. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17569171 # Raltegravir demonstrates potency. AIDS Patient Care STDS. 2007 Apr;21(4):288. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17506141 # Anti-HIV agents. Raltegravir--other issues. TreatmentUpdate. 2007 Feb;19(2):9-10. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17447317 # Anti-HIV agents. Integrase inhibitor raltegravir makes its mark. TreatmentUpdate. 2007 Feb;19(2):8-9. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17447316 # Cahn P, Sued O: Raltegravir: a new antiretroviral class for salvage therapy. Lancet. 2007 Apr 14;369(9569):1235-6. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17434380
n3:group
approved
n3:halfLife
9 hours
n3:indication
For the treatment of HIV-1 infection in conjunction with other antiretrovirals.
owl:sameAs
n11:DB06817
dcterms:title
Raltegravir
adms:identifier
n15:D06676 n16:Raltegravir n17:DB06817
n3:mechanismOfAction
Raltegravir targets integrase, an HIV enzyme that integrates the viral genetic material into human chromosomes, a critical step in the pathogenesis of HIV. The drug is metabolized away via glucuronidation.
n3:patent
n9:7169780
n3:routeOfElimination
Feces and urine
n3:synonym
MK-0518 RAL
n3:volumeOfDistribution
Approximately 83% bound to human plasma protein and is minimally distributed into red blood cells (blood-to-plasma partitioning ratio of 0.6).
n3:proteinBinding
83%
n3:salt
foaf:page
n13:isentress.html
n3:IUPAC-Name
n4:271B558E-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B5594-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B5593-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B5590-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B5591-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B5592-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B558D-363D-11E5-9242-09173F13E4C5
n5:hasATCCode
n6:J05AX08
n3:H-Bond-Acceptor-Count
n4:271B559A-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B559B-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B5595-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B5596-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B5598-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B5597-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B5599-363D-11E5-9242-09173F13E4C5
n3:absorption
Absorbed from the gastrointestinal tract.
n3:affectedOrganism
Human Immunodeficiency Virus
n3:casRegistryNumber
518048-05-0
n3:category
n3:clearance
The major mechanism of clearance of raltegravir in humans is glucuronidation mediated by UGT1A1, the renal clearance of unchanged drug is a minor pathway of elimination of raltegravir (9% of total dose).
n3:Bioavailability
n4:271B55A0-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B55A2-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B55A3-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B559F-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B559E-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B55A1-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B558F-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n4:271B559C-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B559D-363D-11E5-9242-09173F13E4C5