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Review

Raltegravir: first in class HIV integrase inhibitor

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Pages 493-500 | Published online: 11 Apr 2008

References

  • AndersonMSWenningLMoreauAEffect of raltegravir on the pharmacokinetics of oral contraceptives200747th Interscience Conference on Antimicrobial Agents and ChemotherapySeptember 17-20, 2007Chicago, IL Abstract A-1425
  • CooperDGatellJRockstrohJResults of BENCHMRK-1, a phase III study evaluating the efficacy and safety of MK-0518, a novel HIV-1 integrase inhibitor, in patients with triple-class resistant virus2007Program and abstracts of the 14th Conference on Retroviruses and Opportunistic InfectionsFebruary 25-28, 2007Los Angeles, California Abstracts 105aLB
  • CraigieRHIV integrase, a brief overview from chemistry to therapeuticsJ Biol Chem200127623213611346660
  • DeJesusECohenCElionRFirst report of raltegravir (RAL, MK-0518) use after virologic rebound on elvitegravir (EVT, GS 9137)2007Program and abstracts of the 4th International AIDS Society Conference on HIV Pathogenesis, Treatment and PreventionJuly 22-25, 2007Sydney, Australia Abstract TUPEB032
  • EmbreyMWWaiJSFunkTWA series of 5-(5,6)-dihydrouracil substituted 8-hydroxy-[1,6]naphthyridine-7-carboxylic acid 4-fluorobenzylamide inhibitors of HIV-1 integrase and viral replication in cellsBioorg Med Chem Lett2005154550416102965
  • EspesethASFelockPWolfeAHIV-1 integrase inhibitors that compete with the target DNA substrate define a unique strand transfer conformation for integraseProc Natl Acad Sci USA20009711244911016953
  • GrinsztejnBNguyenBKatlamaCSafety and efficacy of the HIV-1 integrase inhibitor raltegravir (MK-0518) in treatment-experienced patients with multidrug-resistant virus: a phase II randomised controlled trialLancet20073691261917434401
  • HazudaDBlauCUFelockPIsolation and characterization of novel human immunodeficiency virus integrase inhibitors from fungal metabolitesAntivir Chem Chemother199910637010335400
  • HazudaDJAnthonyNJGomezRPA naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integraseProc Natl Acad Sci USA200410111233815277684
  • HazudaDJFelockPWitmerMInhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cellsScience20002876465010649997
  • HazudaDJMillerMDNguyenBYResistance to the HIV-integrase inhibitor raltegravir: analysis of protocol 005, a phase II study in patients with triple-class-resistant HIV-1 infection2007Program and abstracts of the 16th International HIV Drug Resistance WorkshopJune 12-16, 2007Barbados, West Indies Abstract 8
  • Isentress prescribing informationWhitehouse Station, NJ 08889, USAMerck and Co., Iin.
  • ISENTRESS™ (raltegravir) 400 mg for treatment of HIV (NDA 22-145)FDA Briefing Document2007 Accessed October 15, 2007. URL: http://www.fda.gov/OHRMS/DOCKETS/AC/07/briefing/2007-4314b1-01-Merck.pdf
  • IwamotoMWenningLALiouSYRifampin (RIF) modestly reduces plasma levels of MK-051820068th international congress on drug therapy in HIV infectionNov 2006Glasgowp299 Abstract 20061
  • IwamotoMWenningLAPetryASMinimal effect of ritonavir (RTV) and efavirenz (EFV) on the pharmacokinetics (PK) ofMK-0518200646th Annual ICAAC Meeting2006San Francisco, CAA-373 Abstract 2006b
  • KassahunKMcIntoshICuiDMetabolism and disposition in humans of raltegravir (MK-0518), an anti-AIDS drug targeting the HIV-1 integrase enzymeDrug Metab Dispos20073516576317591678
  • KassahunKMcIntoshIHreniukDAbsorption, metabolism and excretion of MK-0518, a potent HIV-1 integrase inhibitor, in healthy male volunteers200646th Annual Interscience Conference on Antimicrobial Agents and ChemotherapySept 27-30, 2006San Francisco, California, USA abstract A-372
  • KumarPCooperDSteigbigelREfficacy of raltegravir, an HIV integrase inhibitor, in combination with regimens containing enfuvirtide, darunavir, or tipranavir in patients with triple-class resistant virus: combined results from Benchmrk-1 and Benchmrk-22007European AIDS ConferenceOctober 24-27, 2007Madrid Abstract P7.2/06
  • LaFeminaRLSchneiderCLRobbinsHORequirement of active human immunodeficiency virus type 1 integrase enzyme for productive infection of human T-lymphoid cellsJ Virol1992667414191433523
  • MarkowitzMMorales-RamirezJONguyenBYAntiretroviral 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 individualsJ Acquir Immune Defic Syndr2006435091517133211
  • MarkowitzMNguyenBYGotuzzoERapid and durable antiretroviral effect of the HIV-1 integrase inhibitor raltegravir as part of combination therapy in treatment-naive patients with HIV-1 infection: results of a 48-week controlled studyJ Acquir Immune Defic Syndr2007461253317721395
  • McCollDJFransenSGuptaSResistance and cross-resistance to first-generation integrase inhibitors: insights from a phase II study of elvitegravir (GS-9137)2007Program and abstracts of the 16th International HIV Drug Resistance WorkshopJune 12-16, 2007Barbados, West Indies Abstract 9
  • MillerMDWitmerMVStillmockKABiochemical and antiviral activity of MK-0518, a potent HIV integrase inhibitor2006program and abstracts of XVI International AIDS Conference2006Toronto
  • MistryGWenningLPetryAAtazanavir modestly increases plasma levels of MK-051820074h International AIDS Society Conference on HIV Pathogenesis, Treatment and Prevention2007Sidney, Australia Abstract number:1985
  • PaisGCGZhangXCMarchandCStructure activity of 3-aryl-1,3-diketo-containing compounds as HIV-1 integrase inhibitorsJ Med Chem20024531849412109903
  • SteigbigelRKumarPEronJResults of BENCHMRK-2, a phase III study evaluating the efficacy and safety of MK-0518, a novel HIV-1 integrase inhibitor, in patients with triple-class resistant virus2007Program and abstracts of the 14th Conference on Retroviruses and Opportunistic InfectionsFebruary 25-28, 2007Los Angeles, California Abstracts 105bLB
  • WenningLAFriedmanEKostJTLack of significant drug interaction between MK-0518 and tenofovir disoproxil fumarate200646th Annual ICAAC Meeting2006San Francisco, CA Abstract 2006b; A-375
  • WenningLAHanleyHStoneJEffect of tipranavir + ritonavir on pharmacokinetics of MK-0518200646th Annual ICAAC Meeting2006San Francisco, CA Abstract 2006a; A-374