331
Views
16
CrossRef citations to date
0
Altmetric
Drug Evaluation

Elvitegravir for the treatment of HIV

, , , &
Pages 2359-2370 | Received 28 Aug 2016, Accepted 17 Oct 2016, Published online: 31 Oct 2016

References

  • World Health Organization. Global Health Sector Strategy on HIV. 2016-2021. [cited 2016 Jul 30]. Available from: http://apps.who.int/iris/bitstream/10665/246178/1/WHO-HIV-2016.05-eng.pdf
  • Panel on Antiretroviral Guidelines for Adults and Adolescents. Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents. Department of Health and Human Services. [ cited 2016 Aug 13]. Available from: http://aidsinfo.nih.gov/contentfiles/lvguidelines/AdultandAdolescentGL.pdf
  • Vitekta (R) package insert. Foster city. CA: Gilead Sciences, Inc; 2015 Jul.
  • Stribild (R) package insert. Foster city. CA: Gilead Sciences, Inc; 2016 Feb.
  • Genvoya (R) package insert. Foster city. CA: Gilead Sciences, Inc; 2016 Mar.
  • DeJesus E, Berger D, Markowitz M, et al. Antiviral activity, pharmacokinetics, and dose response of the HIV-1 integrase inhibitor GS-9137 (JTK-303) in treatment-naive and treatment-experienced patients. J Acquir Immune Defic Syndr. 2006;43:1–5.
  • Craigie R. HIV integrase, a brief overview from chemistry to therapeutics. J Biol Chem. 2001;276:23213–23216.
  • Shimura K, Kodama E, Sakagami Y, et al. Broad antiretroviral activity and resistance profile of the novel human immunodeficiency virus integrase inhibitor elvitegravir (JTK-303/GS-9137). J Virol. 2008;82:764–774.
  • Roquebert B, Damond F, Collin G, et al. HIV-2 integrase gene polymorphism and phenotypic susceptibility of HIV-2 clinical isolates to the integrase inhibitors raltegravir and elvitegravir in vitro. J Antimicrob Chemother. 2008;62:914–920.
  • Andreatta K, Miller MD, White KL. HIV-2 antiviral potency and selection of drug resistance mutations by the integrase strand transfer inhibitor elvitegravir and NRTIs emtricitabine and tenofovir in vitro. J Acquir Immune Defic Syndr. 2013;62:367–374.
  • Kulkarni R, Abram ME, McColl DJ, et al. Week 144 resistance analysis of elvitegravir/cobicistat/emtricitabine/tenofovir DF versus atazanavir+ritonavir+emtricitabine/tenofovir DF in antiretroviral-naive patients. HIV Clin Trials. 2014;15:218–230.
  • White KL, Kulkarni R, McColl DJ, et al. Week 144 resistance analysis of elvitegravir/cobicistat/emtricitabine/tenofovir DF versus efavirenz/emtricitabine/tenofovir DF in antiretroviral-naive patients. Antivir Ther. 2015;20:317–327.
  • White K, Kulkarni R, Miller MD. Analysis of early resistance development at the first failure timepoint in elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate-treated patients. J Antimicrob Chemother. 2015;70:2632–2638.
  • Fourati S, Charpentier C, Amiel C, et al. Cross-resistance to elvitegravir and dolutegravir in 502 patients failing on raltegravir: a French national study of raltegravir-experienced HIV-1-infected patients. J Antimicrob Chemother. 2015;70:1507–1512.
  • You J, Wang H, Huang X, et al. Therapy-emergent drug resistance to integrase strand transfer inhibitors in HIV-1 Patients: a subgroup meta-analysis of clinical trials. Plos One. 2016;11:e0160087.
  • Deeks ED. Elvitegravir: a review of its use in adults with HIV-1 infection. Drugs. 2014;74:687–697.
  • Ramanathan S, Mathias AA, German P, et al. Clinical pharmacokinetic and pharmacodynamic profile of the HIV integrase inhibitor elvitegravir. Clin Pharmacokinet. 2011;50:229–244.
  • Vitekta (R) product information. Cambridge, United Kingdom: Gilead Sciences International Limited; Mar 2016.
  • Shiomi M, Matsuki S, Ikeda A, et al. Effects of a protein-rich drink or a standard meal on the pharmacokinetics of elvitegravir, cobicistat, emtricitabine and tenofovir in healthy Japanese male subjects: a randomized, three-way crossover study. J Clin Pharmacol. 2014;54:640–648.
  • German P, Warren D, Wei L, et al. Effect of food on pharmacokinetics of elvitegravir, emtricitabine, tenofovir DF and the pharmacoenhancer GS-9350 as a fixed-dose combination tablet. 49th interscience conference on antimicrobial agents and chemotherapy. San Francisco, CA; 2009.
  • Calcagno A, Simiele M, Motta I, et al. Elvitegravir/Cobicistat/Tenofovir/Emtricitabine Penetration in the Cerebrospinal Fluid of Three HIV-Positive Patients. AIDS Res Hum Retroviruses. 2016;32:409–411.
  • Imaz A, Niubo J, Kashuba AD, et al. Elvitegravir concentrations in seminal plasma in HIV-1-infected men. HIV Med. 2016 Aug;1. DOI:10.1111/hiv.12417
  • Massud I, Martin A, Dinh C, et al. Pharmacokinetic profile of raltegravir, elvitegravir and dolutegravir in plasma and mucosal secretions in rhesus macaques. J Antimicrob Chemother. 2015;70:1473–1481.
  • Custodio JM, Rhee M, Shen G, et al. Pharmacokinetics and safety of boosted elvitegravir in subjects with hepatic impairment. Antimicrob Agents Chemother. 2014;58:2564–2569.
  • German P, Wei L, Mizuno V, et al. Pharmacokinetics of elvitegravir and cobicistat in subjects with severe renal impairment. 13th international workshop on clinical pharmacology of HIV therapy. Barcelona, Spain; 2012.
  • German P, Warren D, West S, et al. Pharmacokinetics and bioavailability of an integrase and novel pharmacoenhancer-containing single-tablet fixed-dose combination regimen for the treatment of HIV. J Acquir Immune Defic Syndr. 2010;55:323–329.
  • Tivicay (R) package insert. Research triangle park. NC: ViiV Healthcare; 2016 Jun.
  • Daklinza (R) package insert. Princeton, NJ: Bristol-Myers Squibb Company; Apr 2016.
  • Epclusa (R) package insert. Foster city. CA: Gilead Sciences, Inc; 2016 Jun.
  • Harvoni (R) package insert. Foster city. CA: Gilead Sciences, Inc; 2016 Jun.
  • Olysio (R) package insert. Titusville, NJ: Janssen Therapeutics; May 2016.
  • Sovaldi (R) package insert. Foster city. CA: Gilead Sciences, Inc; 2015 Aug.
  • Technivie (R) package insert. North Chicago, IL: AbbVie Inc; Jun 2016.
  • Viekira Pak (R) package insert. North Chicago, IL: AbbVie Inc; Jun 2016.
  • Zepatier (R) package insert. Whitehouse Station. NJ: Merck and Co, Inc; 2016 Jan.
  • Cohen C, Elion R, Ruane P, et al. Randomized, 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 infection. Aids. 2011;25:F7- F12.
  • Zolopa AR, Berger DS, Lampiris H, et al. Activity of elvitegravir, a once-daily integrase inhibitor, against resistant HIV type 1: results of a phase 2, randomized, controlled, dose-ranging clinical trial. J Infect Dis. 2010;201:814–822.
  • Sax PE, DeJesus E, Mills A, et al. Co-formulated elvitegravir, cobicistat, emtricitabine, and tenofovir versus co-formulated efavirenz, emtricitabine, and tenofovir for initial treatment of HIV-1 infection: a randomised, double-blind, phase 3 trial, analysis of results after 48 weeks. Lancet. 2012;379:2439–2448.
  • DeJesus E, Rockstroh JK, Henry K, et al. Co-formulated elvitegravir, cobicistat, emtricitabine, and tenofovir disoproxil fumarate versus ritonavir-boosted atazanavir plus co-formulated emtricitabine and tenofovir disoproxil fumarate for initial treatment of HIV-1 infection: a randomised, double-blind, phase 3, non-inferiority trial. Lancet. 2012;379:2429–2438.
  • Zolopa A, Sax PE, DeJesus E, et al. A randomized double-blind comparison of coformulated elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate versus efavirenz/emtricitabine/tenofovir disoproxil fumarate for initial treatment of HIV-1 infection: analysis of week 96 results. J Acquir Immune Defic Syndr. 2013;63:96–100.
  • Wohl DA, Cohen C, Gallant JE, et al. A randomized, double-blind comparison of single-tablet regimen elvitegravir/cobicistat/emtricitabine/tenofovir DF versus single-tablet regimen efavirenz/emtricitabine/tenofovir DF for initial treatment of HIV-1 infection: analysis of week 144 results. J Acquir Immune Defic Syndr. 2014;65:e118- e20.
  • Rockstroh JK, DeJesus E, Henry K, et al. A randomized, double-blind comparison of coformulated elvitegravir/cobicistat/emtricitabine/tenofovir DF vs ritonavir-boosted atazanavir plus coformulated emtricitabine and tenofovir DF for initial treatment of HIV-1 infection: analysis of week 96 results. J Acquir Immune Defic Syndr. 2013;62:483–486.
  • Clumeck N, Molina JM, Henry K, et al. A randomized, double-blind comparison of single-tablet regimen elvitegravir/cobicistat/emtricitabine/tenofovir DF vs ritonavir-boosted atazanavir plus emtricitabine/tenofovir DF for initial treatment of HIV-1 infection: analysis of week 144 results. J Acquir Immune Defic Syndr. 2014;65:e121- e4.
  • Sax PE, Wohl D, Yin MT, et al. Tenofovir alafenamide versus tenofovir disoproxil fumarate, coformulated with elvitegravir, cobicistat, and emtricitabine, for initial treatment of HIV-1 infection: two randomised, double-blind, phase 3, non-inferiority trials. Lancet. 2015;385:2606–2615.
  • Squires K, Kityo C, Hodder S, et al. Integrase inhibitor versus protease inhibitor based regimen for HIV-1 infected women (WAVES): a randomised, controlled, double-blind, phase 3 study. Lancet HIV. 2016;3:e410- e20.
  • Molina JM, Lamarca A, Andrade-Villanueva J, et al. Efficacy and safety of once daily elvitegravir versus twice daily raltegravir in treatment-experienced patients with HIV-1 receiving a ritonavir-boosted protease inhibitor: randomised, double-blind, phase 3, non-inferiority study. Lancet Infect Dis. 2012;12:27–35.
  • Elion R, Molina JM, Ramon Arribas Lopez J, et al. A randomized phase 3 study comparing once-daily elvitegravir with twice-daily raltegravir in treatment-experienced subjects with HIV-1 infection: 96-week results. J Acquir Immune Defic Syndr. 2013;63:494–497.
  • Pozniak A, Markowitz M, Mills A, et al. Switching to coformulated elvitegravir, cobicistat, emtricitabine, and tenofovir versus continuation of non-nucleoside reverse transcriptase inhibitor with emtricitabine and tenofovir in virologically suppressed adults with HIV (STRATEGY-NNRTI): 48 week results of a randomised, open-label, phase 3b non-inferiority trial. Lancet Infect Dis. 2014;14:590–599.
  • Arribas JR, Pialoux G, Gathe J, et al. Simplification to coformulated elvitegravir, cobicistat, emtricitabine, and tenofovir versus continuation of ritonavir-boosted protease inhibitor with emtricitabine and tenofovir in adults with virologically suppressed HIV (STRATEGY-PI): 48 week results of a randomised, open-label, phase 3b, non-inferiority trial. Lancet Infect Dis. 2014;14:581–589.
  • Mills A, Crofoot G, Ortiz R, et al. Switching from twice-daily raltegravir plus tenofovir disoproxil fumarate/emtricitabine to once-daily elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate in virologically suppressed, HIV-1-infected subjects: 48 weeks data. HIV Clin Trials. 2014;15:51–56.
  • Mills A, Arribas JR, Andrade-Villanueva J, et al. Switching from tenofovir disoproxil fumarate to tenofovir alafenamide in antiretroviral regimens for virologically suppressed adults with HIV-1 infection: a randomised, active-controlled, multicentre, open-label, phase 3, non-inferiority study. Lancet Infect Dis. 2016;16:43–52.
  • Pozniak A, Arribas JR, Gathe J, et al. Switching to tenofovir alafenamide, coformulated with elvitegravir, cobicistat, and emtricitabine, in HIV-infected patients with renal impairment: 48-week results from a single-arm, multicenter, Open-label phase 3 study. J Acquir Immune Defic Syndr. 2016;71:530–537.
  • Sherman EM, Worley MV, Unger NR, et al. Cobicistat: review of a pharmacokinetic enhancer for HIV infection. Clin Ther. 2015;37:1876–1893.
  • Mills A, Garner W, Pozniak A, et al. Patient-reported symptoms over 48 weeks in a randomized, open-label, phase iiib non-inferiority trial of adults with HIV switching to co-formulated elvitegravir, cobicistat, emtricitabine, and tenofovir DF versus continuation of non-nucleoside reverse transcriptase inhibitor with emtricitabine and tenofovir DF. Patient. 2015;8:359–371.
  • Gathe J, Arribas JR, Van Lunzen J, et al. Patient-reported symptoms over 48 weeks in a randomized, open-label, phase 3b non-inferiority trial of adults with HIV switching to coformulated elvitegravir, cobicistat, emtricitabine, and tenofovir DF versus continuation of ritonavir-boosted protease inhibitor with emtricitabine and tenofovir DF. Patient. 2015;8:445–454.
  • Lepik KJ, Nohpal A, Yip B, et al. Adverse drug reactions associated with integrase strand transfer inhibitors in clinical practice: post-marketing experience with raltegravir, elvitegravir-cobicistat and dolutegravir. Canada: Vancouver; 2015.
  • Padilla M, Rojas J, Gonzalez-Cordon A, et al. Tolerability of integrase inhibitors in a real-life setting. 2016; New York, New York.
  • Stribild (R) product information. Cambridge, United Kingdom: Gilead Sciences International Limited; May 2016.
  • Genvoya (R) product information. Cambridge, United Kingdom: Gilead Sciences International Limited; Jul 2016.
  • Gilead Sciences, Inc. Important information regarding the voluntary withdrawal of Vitekta (elvitegravir) tablets. [ cited 2016 Jul 8]. Available from https://www.gilead.com/~/media/files/pdfs/other/vitekta_withdrawal_letter.pdf?la=en
  • Lee FJ, Carr A. Tolerability of HIV integrase inhibitors. Curr Opin HIV AIDS. 2012;7:422–428.
  • Cahn P, Kaplan R, Sax P, et al. Raltegravir (RAL) 1200 mg once daily is non-inferior to RAL 400 mg twice daily, in combination with tenofovir/emtricitabine, in treatment-naïve HIV-1 infected subjects: week 48 results. 21st international AIDS conference. Durban, South Africa; 2016.
  • Panel on Antiretroviral Therapy and Medical Management of HIV-Infected Children. Guidelines for the Use of Antiretroviral Agents in Pediatric HIV Infection. [ cited 2016 Aug 7]. Available from: http://aidsinfo.nih.gov/contentfiles/lvguidelines/pediatricguidelines.pdf
  • Panel on Treatment of HIV-Infected Pregnant Women and Prevention of Perinatal Transmission. Recommendations for Use of Antiretroviral Drugs in Pregnant HIV-1-Infected Women for Maternal Health and Interventions to Reduce Perinatal HIV Transmission in the United States. [ cited 2016 Aug 7]. Available from: http://aidsinfo.nih.gov/contentfiles/lvguidelines/PerinatalGL.pdf

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.