Review of the safety, efficacy, and pharmacokinetics of elvitegravir with an emphasis on resource-limited settings

References

• ClaydenPCollinsSHarringtonMHIV, Hepatitis C Virus (HCV), and tuberculosis drugs, diagnostics, vaccines, and preventive technologies in development2011 pipeline reportsecond editioni-Base/Treatment Action GroupNew York2011
   Google Scholar
• Department of Health and Human Services (DHHS) Panel on Antiretroviral Guidelines for Adults and AdolescentsGuidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and AdolescentsRockville, MDDHHS2011 [upated November 29]. Available from: http://aidsinfo.nih.gov/Guidelines/HTML/1/adult-and-adolescent-treatment-guidelines/1/panel-roster/Accessed November 30, 2011
   Google Scholar
• Global HIV/AIDS response: epidemic update and health sector progress towards Universal AccessGenevaWHO/UNAIDS2011 Available from: http://www.who.int/hiv/pub/progress_report2011/hiv_full_report_2011.pdfAccessed December 28, 2011
   Google Scholar
• Renaud-ThéryFDuncombeCKerrSThierrySPerriënsJAdult ART in resource-limited settings: a systematic review of first-line treatment failure and attrition rates17th Conference on Retroviruses and Opportunities InfectionsSan FranciscoFebruary 16–20, 2010
   Google Scholar
• El-KhatibZEkstromAMLedwabaJMohapiLLaherFKarstaedtAViremia and drug resistance among HIV-1 patients on antiretroviral treatment: a cross-sectional study in Soweto, South AfricaAIDS201024111679168720453629
   PubMed Web of Science ®Google Scholar
• HosseinipourMCKumwendaJJWeigelRSecond-line treatment in the Malawi antiretroviral programme: high early mortality, but good outcomes in survivors, despite extensive drug resistance at baselineHIV Med201011851051820345885
   PubMed Web of Science ®Google Scholar
• DeJesusEBergerDMarkowitzMAntiviral activity, pharmacokinetics, and dose response of the HIV-1 integrase inhibitor GS-9137 (JTK-303) in treatment-naive and treatment-experienced patientsJ Acquir Immune Defic Syndr20064311516936557
   PubMed Web of Science ®Google Scholar
• JTK 303 Public Chemical DatabasePubChem Compound Summary (CID 5277135) Available from: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5277135Accessed November 30, 2011
   Google Scholar
• Al-MawsawiLQAl-SafiRINeamatiNAnti-infectives: clinical progress of HIV-1 integrase inhibitorsExpert Opin Emerg Drugs200813221322518537517
   PubMed Web of Science ®Google Scholar
• KawaguchiIIshikawaTIshibashiMIrieSKakeeAGilead integrase inhibitor: safety and pharmacokinetics of single oral dose of JTK 303/GS-9137, a novel HIV integrase inhibitor, in healthy volunteers13th Conference on Retroviruses and Opportunistic InfectionsDenver, USAFebruary 5—9, 2006 Available from: http://www.natap.org/2006/CROI/CROI_11.htmAccessed November 30, 2011
   Google Scholar
• RamanathanSWrightMWestSPharmacokinetics, metabolism, and excretion of ritonavir-boosted GS-9137 (Elvitegravir)Presented at: Eighth International Workshop on Clinical Pharmacology of HIV TherapyApril 16–18, 2007Budapest, Hungary Abstract 30
   Google Scholar
• MathiasAAWestSHuiJKearneyBPDose-response of ritonavir on hepatic CYP3A activity and elvitegravir oral exposureClin Pharmacol Ther2009851647018815591
   PubMed Web of Science ®Google Scholar
• ElionRCohenCGatheJPhase 2 study of cobicistat versus ritonavir each with once-daily atazanavir and fixed-dose emtricitabine/tenofovir df in the initial treatment of HIV infectionAIDS201125151881188621811136
   PubMed Web of Science ®Google Scholar
• GermanPWestSHuiJKearneyBPPharmacokinetic interaction between elvitegravir/ritonavir and dose-adjusted rifabutin9th International Workshop on Clinical Pharmacology of HIV TherapyNew Orleans, LAApril 7–9, 2008 Abstract P19. Available from: http://www.hiv-druginteractions.org/data/NewsItem/62_9PK_NewOrleans.pdfAccessed November 30, 2011
   Google Scholar
• MathiasAAHinkleJShenGEffect of ritonavir-boosted tipranavir or darunavir on the steady-state pharmacokinetics of elvitegravirJ Acquir Immune Defic Syndr200849215616218769354
   PubMed Web of Science ®Google Scholar
• RamanathanSMathiasAAShenGHolmesCKearneyBPLack of clinically relevant drug-drug interaction between ritonavir-boosted GS-9137 (elvitegravir) and fosamprenavir/rPoster exhibition: 4th IAS Conference on HIV Pathogenesis, Treatment and PreventionSydney, AustraliaJuly 22–25, 2007 Abstract WEPEB014
   Google Scholar
• MathiasAWestSEnejosaJKearneyBA pharmacokinetic interaction between lopinavir/r and elvitegravir47th Interscience Conference on Antimicrobial Agents and ChemotherapyChicago, USASeptember 17–20, 2007 Abstract A-1418
   Google Scholar
• RamanathanSWestSHuiJClinical pharmacokinetics of once-daily elvitegravir boosted by atazanavir versus ritonavir9th International Workshop on Clinical Pharmacology of HIV TherapyNew Orleans, USAApril 7–9, 2008 Abstract O18
   Google Scholar
• MathiasARamanathanSHinkleJWestSEnejosaJKearneyBEffect of atazanavir/r on the steady-state pharmacokinetics of elvitegravir47th Interscience Conference on Antimicrobial Agents and ChemotherapyChicago, USASeptember 17–20, 2007 Abstract A-1417
   Google Scholar
• RamanathanSAbelSTweedySWestSHuiJKearneyBPPharmacokinetic interaction of ritonavir-boosted elvitegravir and maravirocJ Acquir Immune Defic Syndr201053220921419851115
   PubMed Web of Science ®Google Scholar
• RamanathanSKakudaTNMackRWestSKearneyBPPharmacokinetics of elvitegravir and etravirine following coadministration of ritonavir-boosted elvitegravir and etravirineAntivir Ther20081381011101719195326
   PubMed Web of Science ®Google Scholar
• RamanathanSShenGChengAKearneyBPPharmacokinetics of emtricitabine, tenofovir, and GS-9137 following coadministration of emtricitabine/tenofovir disoproxil fumarate and ritonavir-boosted GS-9137J Acquir Immune Defic Syndr200745327427917414929
   PubMed Web of Science ®Google Scholar
• RamanathanSShenGHinkleJEnejosaJKearneyBPPharmacokinetics of coadministered ritonavir-boosted elvitegravir and zidovudine, didanosine, stavudine or abacavirJ Acquir Immune Defic Syndr200746216016617693892
   PubMed Web of Science ®Google Scholar
• RamanathanSShenGHinkleJEnejosaJKearneyBPPharmacokinetic evaluation of drug interaction with ritonavir-boosted HIV integrase inhibitor GS-9137 and acid reducing agents8th International Workshop on Clinical Pharmacology of HIV TherapyBudapestApril 16–18, 2007 Abstract 69
   Google Scholar
• GermanPMathiasAWestSChuckSKearneyBPEvaluation of ritonavir-boosted elvitegravir PK upon co-administration with a second potent CYP3A inhibitor, ketoconazole11th International Workshop on Clinical Pharmacology of HIV TherapySorrento, ItalyApril 5–7, 2010 Abstract 48
   Google Scholar
• GermanPWangMWarrenDKearneyPBPharmacokinetic interaction between norgestimate/ethinyl estradiol and EVG/COB/FTC/TDF single tablet regimen12th International Workshop on Clinical Pharmacology of HIV TherapyMiami, USAApril 13–15, 2011 Abstract 17
   Google Scholar
• ZolopaARBergerDSLampirisHZhongLChuckSLEnejosaJVActivity of elvitegravir, a once-daily integrase inhibitor, against resistant HIV Type 1: results of a phase 2, randomized, controlled, dose-ranging clinical trialJ Infect Dis2010201681482220146631
   PubMed Web of Science ®Google Scholar
• Gilead SciencesSafety and efficacy of GS-9350-boosted atazanavir compared to ritonavir-boosted atazanavir in combination with emtricitabine/tenofovir disoproxil fumarate in HIV-1 infected, antiretroviral treatment-naive adultsClinicalTrials.gov identifier: NCT00892437. Ongoing study sponsored by Gilead Sciences Trial began April 30, 2009, last updated October 12, 2011. Available from: http://clinicaltrials.gov/ct2/show/NCT00892437?term=GS-9350&rank=1Accessed November 30, 2011
   Google Scholar
• CohenCElionRRuanePRandomized, phase 2 evaluation of two single-tablet regimens elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate versus efavirenz/emtricitabine/tenofovir disoproxil fumarate for the initial treatment of HIV infectionAIDS2011256F7F1221412057
   PubMed Web of Science ®Google Scholar
• Gilead SciencesGilead’s Investigational Antiretroviral Quad Regimen Meets 48-Week Primary Objective in Pivotal Phase 3 Clinical Study 102 Press release August 15, 2011. Available from: http://www.gilead.com/press_archiveAccessed November 30, 2011
   Google Scholar
• MolinaJ-MLaMarcaAAndrade VillanuevaJfor the Study 145 GroupElvitegravir once-daily is non inferior to raltegravir twice-daily in treatment experienced patients: 48 week results from a phase 3 multicenter, randomized, double blind study6th IAS Conference on HIV Pathogenesis, Treatment and PreventionRomeJuly 17–20, 2011 Abstract WELBB05
   Google Scholar
• FordNLeeJAndrieux-MeyerICalmyASafety, efficacy and pharmacokinetics of rilpivirine: a systematic review with an emphasis on resource-limited settingsHIV/AIDS (Auckl)201133544
   PubMedGoogle Scholar
• BlancoJLVargheseVRheeSYGatellJMShaferRWHIV-1 integrase inhibitor resistance and its clinical implicationsJ Infect Dis201120391204121421459813
   PubMed Web of Science ®Google Scholar
• ShimuraKKodamaESakagamiYBroad antiretroviral activity and resistance profile of the novel human immunodeficiency virus integrase inhibitor elvitegravir (JTK-303/GS-9137)J Virol200882276477417977962
   PubMed Web of Science ®Google Scholar
• GoethalsOClaytonRVan GinderenMResistance mutations in human immunodeficiency virus type 1 integrase selected with elvitegravir confer reduced susceptibility to a wide range of integrase inhibitorsJ Virol20088221103661037418715920
   PubMed Web of Science ®Google Scholar
• GarveyEPJohnsBAGartlandMJThe naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviralAntimicrob Agents Chemother200852390190818160521
   PubMed Web of Science ®Google Scholar
• McCollDJFransenSGuptaSResistance and cross-resistance to first generation integrase inhibitors: insights from a phase 2 study of elvitegravir (GS-9137)16th International Drug Resistance Workshop; BarbadosBridgetownJune 12–16, 2007 Abstract 9
   Google Scholar
• MétifiotMMarchandCMaddaliKPommierYResistance to integrase inhibitorsViruses2010271347136620706558
   PubMed Web of Science ®Google Scholar
• GoethalsOClaytonRVan GinderenMResistance mutations in human immunodeficiency virus type 1 integrase selected with elvitegravir confer reduced susceptibility to a wide range of integrase inhibitorsJ Virol20088221103661037418715920
   PubMed Web of Science ®Google Scholar
• MétifiotMVandegraaffNMaddaliKElvitegravir overcomes resistance to raltegravir induced by integrase mutation Y143AIDS20112591175117821505303
   PubMed Web of Science ®Google Scholar
• DaviesMAMoultrieHEleyBVirologic failure and second-line antiretroviral therapy in children in South Africa – the leDEA Southern Africa collaborationJ Acquir Immune Defic Syndr201156327027821107266
   PubMed Web of Science ®Google Scholar
• Médecins Sans FrontièresUntangling the web of antiretroviral price reductions14th edGeneva2011
   Google Scholar
• Department of Health and Human Services Panel on Antiretroviral Guidelines for Adults and AdolescentsWorking Group of the Office of AIDS Research Advisory Council (OARAC): guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents10142011 Available at: http://aidsinfo.nih.gov/contentfiles/AdultandAdolescentGLAccessed November 30, 2011
   Google Scholar
• SatoAKobayashiMYoshinagaTS/GSK1349572 is a potent next generation HIV integrase inhibitor5th IAS Conference on HIV Pathogenesis, Treatment and PreventionCape Town, South AfricaJuly 19–22, 2009 Abstract WEPEA097
   Google Scholar
• UnderwoodMJohnsBSatoAFujiwaraTSpreenWS/GSK1349572: a next generation integrase inhibitor with activity against integrase inhibitor resistant clinical isolates from patients experiencing virologic failure while on raltegravir therapy5th IAS Conference on HIV Pathogenesis, Treatment and PreventionCape Town, South AfricaJuly 19–22, 2009 Abstract WEPEA098
   Google Scholar
• MinSSongIBorlandJPharmacokinetics (PK) and safety in healthy subjects of S/GSK1349572, a next generation, once-daily HIV integrase inhibitor (INI)5th IAS Conference on HIV Pathogenesis, Treatment and PreventionCape Town, South AfricaJuly 19–22, 2009 Abstract WEPEA099
   Google Scholar
• MinSSongIBorlandJChenSLouYFujiwaraTPharmacokinetics and safety of S/GSK1349572, a next-generation HIV integrase inhibitor, in healthy volunteersAntimicrob Agents Chemother201054125425819884365
   PubMed Web of Science ®Google Scholar
• LalezariJSloanLDeJesusEPotent antiviral activity of S/GSK1349572, a next generation integrase inhibitor (INI), in INI-Naive HIV-1-infected patients: ING111521 protocol5th IAS Conference on HIV Pathogenesis, treatment and preventionCape Town, South AfricaJuly 19–22, 2009 Abstract TUAB105
   Google Scholar
• SongIChenSLouYPharmacokinetic (PK) and pharmacodynamic (PD) relationship of S/GSK1349572, a next generation integrase inhibitor (INI), in HIV-1 infected patients5th IAS Conference on HIV Pathogenesis, Treatment and PreventionCape Town, South AfricaJuly 19–22, 2009 Abstract WePeB250
   Google Scholar
• MinSDeJesusEMcCurdyLPharmacokinetics (PK) and safety in healthy and HIV-infected subjects and short-term antiviral efficacy of S/GSK1265744, a next generation once daily HIV integrase inhibitorThe Interscience Conference on Antimicrobial Agents and ChemotherapySan FranciscoSeptember 12–15, 2009 Abstract H-1228
   Google Scholar
• GlaxoSmithKlineA single dose escalation study to investigate the safety, tolerability and pharmacokinetics of intramuscular and subcutaneous long acting GSK1265744 in healthy subjectsClinicalTrials.gov identifier: NCT01215006. Sponsored by Gilead Sciences2010 [updated June 9, 2011.]. Available from: http://clinicaltrials.gov/ct2/show/NCT01215006Accessed November 30, 2011
   Google Scholar