Skip to main content
Erschienen in: Drugs 17/2010

01.12.2010 | Adis Drug Evaluation

Efavirenz/Emtricitabine/Tenofovir Disoproxil Fumarate Single-Tablet Regimen (Atripla®)

A Review of its Use in the Management of HIV Infection

verfasst von: Emma D. Deeks, Caroline M. Perry

Erschienen in: Drugs | Ausgabe 17/2010

Einloggen, um Zugang zu erhalten

Abstract

The non-nucleoside reverse transcriptase inhibitor, efavirenz, and the two nucleoside reverse transcriptase inhibitors, emtricitabine and tenofovir disoproxil fumarate (tenofovir DF) are now available as a single-tablet regimen (efavirenz/emtricitabine/tenofovir DF 600 mg/200 mg/300 mg; Atripla®). The efavirenz/emtricitabine/tenofovir DF single-tablet regimen is the first once-daily, single-tablet, triple antiretroviral therapy (ART) formulation available for the treatment of HIV infection and, in the EU, is indicated for use in adults infected with HIV-1 who have been virologically suppressed for >3 months on their current ART regimen.
In treatment-experienced adults with HIV-1 infection already virologically suppressed with ART, switching to once-daily triple combination therapy with efavirenz, emtricitabine and tenofovir DF (including the single-tablet regimen) is effective in maintaining virological suppression and is generally well tolerated, according to several randomized, open-label or noncomparative multicentre trials and an open-label extension study of up to 96 weeks’ duration. Moreover, additional data from some of these studies indicate that adherence to treatment was maintained or improved after switching to the once-daily triple combination, with patients generally preferring the efavirenz/emtricitabine/tenofovir DF single-tablet regimen over their previous more complex regimen and (in one of two trials) finding it easier to follow. Thus, the efavirenz/emtricitabine/tenofovir DF single-tablet regimen provides a convenient once-daily regimen for use in treatment-experienced adults that may confer an advantage over more complex or frequently administered regimens for which adherence to treatment is an issue.
Literatur
1.
Zurück zum Zitat Simon V, Ho DD. HIV/AIDS epidemiology, pathogenesis, prevention, and treatment. Lancet 2006 Aug 5; 368(9534): 489–504PubMedCrossRef Simon V, Ho DD. HIV/AIDS epidemiology, pathogenesis, prevention, and treatment. Lancet 2006 Aug 5; 368(9534): 489–504PubMedCrossRef
2.
Zurück zum Zitat Molina JM. Efficacy and safety of once-daily regimens in the treatment of HIV infection. Drugs 2008; 68(5): 567–78PubMedCrossRef Molina JM. Efficacy and safety of once-daily regimens in the treatment of HIV infection. Drugs 2008; 68(5): 567–78PubMedCrossRef
3.
Zurück zum Zitat Satyanarayana K, Srivastava S. Universal access to HIV/AIDS treatment: challenges ahead. Indian J Med Res 2009 Dec; 130(6): 671–4PubMed Satyanarayana K, Srivastava S. Universal access to HIV/AIDS treatment: challenges ahead. Indian J Med Res 2009 Dec; 130(6): 671–4PubMed
6.
Zurück zum Zitat Gazzard BG. British HIV Association guidelines for the treatment of HIV-1-infected adults with antiretroviral therapy 2008. HIV Med 2008 Oct; 9(8): 563–608PubMedCrossRef Gazzard BG. British HIV Association guidelines for the treatment of HIV-1-infected adults with antiretroviral therapy 2008. HIV Med 2008 Oct; 9(8): 563–608PubMedCrossRef
7.
Zurück zum Zitat Thompson MA, Aberg JA, Cahn P, et al. Antiretroviral treatment of adult HIV infection: 2010 recommendations of the International AIDS Society-USA Panel. JAMA 2010 Jul 21; 304(3): 321–33PubMedCrossRef Thompson MA, Aberg JA, Cahn P, et al. Antiretroviral treatment of adult HIV infection: 2010 recommendations of the International AIDS Society-USA Panel. JAMA 2010 Jul 21; 304(3): 321–33PubMedCrossRef
8.
Zurück zum Zitat Stone VE, Jordan J, Tolson J, et al. Perspectives on adherence and simplicity for HIV-infected patients on antiretroviral therapy. Self-report of the relative importance of multiple attributes of highly active antiretroviral therapy (HAART) regimens in predicting adherence. J Acquir Immune Defic Syndr 2004 Jul 1; 36(3): 808–16 Stone VE, Jordan J, Tolson J, et al. Perspectives on adherence and simplicity for HIV-infected patients on antiretroviral therapy. Self-report of the relative importance of multiple attributes of highly active antiretroviral therapy (HAART) regimens in predicting adherence. J Acquir Immune Defic Syndr 2004 Jul 1; 36(3): 808–16
12.
Zurück zum Zitat Lyseng-Williamson KA, Reynolds NA, Plosker GL. Tenofovir disoproxil fumarate: a review of its use in the management of HIV infection. Drugs 2005; 65(3): 413–32PubMedCrossRef Lyseng-Williamson KA, Reynolds NA, Plosker GL. Tenofovir disoproxil fumarate: a review of its use in the management of HIV infection. Drugs 2005; 65(3): 413–32PubMedCrossRef
13.
Zurück zum Zitat Dando TM, Wagstaff AJ. Emtricitabine/tenofovir disoproxil fumarate. Drugs 2004; 64(18): 2075–82PubMedCrossRef Dando TM, Wagstaff AJ. Emtricitabine/tenofovir disoproxil fumarate. Drugs 2004; 64(18): 2075–82PubMedCrossRef
14.
Zurück zum Zitat Frampton JE, Perry CM. Emtricitabine: a review of its use in the management of HIV infection. Drugs 2005; 65(10): 1427–48PubMedCrossRef Frampton JE, Perry CM. Emtricitabine: a review of its use in the management of HIV infection. Drugs 2005; 65(10): 1427–48PubMedCrossRef
15.
17.
Zurück zum Zitat DeJesus E, Young B, Morales-Ramirez JO, et al. Simplification of antiretroviral therapy to a single-tablet regimen consisting of efavirenz, emtricitabine, and tenofovir disoproxil fumarate versus unmodified antiretroviral therapy in virologically suppressed HIV-1-infected patients. J Acquir Immune Defic Syndr 2009 Jun 1; 51(2): 163–74PubMedCrossRef DeJesus E, Young B, Morales-Ramirez JO, et al. Simplification of antiretroviral therapy to a single-tablet regimen consisting of efavirenz, emtricitabine, and tenofovir disoproxil fumarate versus unmodified antiretroviral therapy in virologically suppressed HIV-1-infected patients. J Acquir Immune Defic Syndr 2009 Jun 1; 51(2): 163–74PubMedCrossRef
18.
Zurück zum Zitat Fisher M, Moyle GJ, Shahmanesh M, et al. A randomized comparative trial of continued zidovudine/lamivudine or replacement with tenofovir disoproxil fumarate/emtricitabine in efavirenz-treated HIV-1-infected individuals. J Acquir Immune Defic Syndr 2009 Aug 15; 51(5): 562–8PubMedCrossRef Fisher M, Moyle GJ, Shahmanesh M, et al. A randomized comparative trial of continued zidovudine/lamivudine or replacement with tenofovir disoproxil fumarate/emtricitabine in efavirenz-treated HIV-1-infected individuals. J Acquir Immune Defic Syndr 2009 Aug 15; 51(5): 562–8PubMedCrossRef
19.
Zurück zum Zitat DeJesus E, Ruane P, McDonald C, et al. Impact of switching virologically suppressed, HIV-1-infected patients from twice-daily fixed-dose zidovudine/lamivudine to once-daily fixed-dose tenofovir disoproxil fumarate/emtricitabine. HIV Clin Trials 2008 Mar–Apr; 9(2): 103–14PubMedCrossRef DeJesus E, Ruane P, McDonald C, et al. Impact of switching virologically suppressed, HIV-1-infected patients from twice-daily fixed-dose zidovudine/lamivudine to once-daily fixed-dose tenofovir disoproxil fumarate/emtricitabine. HIV Clin Trials 2008 Mar–Apr; 9(2): 103–14PubMedCrossRef
20.
Zurück zum Zitat Moyle G, Orkin C, Fisher M, et al. Switching to Atripla® (EFV/FTC/TDF) from ABC/3TC FDC (Kivexa®/Epzicom®) + efavirenz (EFV) improves lipid levels towards NCEP recommendations: primary endpoint results of a 24-week randomised study [poster no. THPE0133]. 18th International AIDS Conference; 2010 Jul 18–23; Vienna Moyle G, Orkin C, Fisher M, et al. Switching to Atripla® (EFV/FTC/TDF) from ABC/3TC FDC (Kivexa®/Epzicom®) + efavirenz (EFV) improves lipid levels towards NCEP recommendations: primary endpoint results of a 24-week randomised study [poster no. THPE0133]. 18th International AIDS Conference; 2010 Jul 18–23; Vienna
21.
Zurück zum Zitat Moyle G, Orkin C, Fisher M, et al. Switching from ABC/3TC + efavirenz [EFV] to TDF/FTC/EFV [atripla, ATR] reduces cholesterol in hypercholesterolemic subjects: 24-week final results of a randomised study [presentation no. H-1809]. Interscience Conference on Antimicrobial Agents and Chemotherapy; 2010 Sep 12–15; Boston (MA) Moyle G, Orkin C, Fisher M, et al. Switching from ABC/3TC + efavirenz [EFV] to TDF/FTC/EFV [atripla, ATR] reduces cholesterol in hypercholesterolemic subjects: 24-week final results of a randomised study [presentation no. H-1809]. Interscience Conference on Antimicrobial Agents and Chemotherapy; 2010 Sep 12–15; Boston (MA)
22.
Zurück zum Zitat DeJesus E, Pozniak A, Gallant J, et al. Improvement in fasting lipids but minimal recovery of limb fat were seen 96 weeks after switching from lamivudine/zidovudine plus efavirenz to fixed-dose efavirenz/emtricitabine/tenofovir DF in HIV-infected patients [abstract and poster no. H-1572]. 49th Interscience Conference on Antimicrobial Agents and Chemotherapy; 2009 Sep 12–15; San Francisco (CA) DeJesus E, Pozniak A, Gallant J, et al. Improvement in fasting lipids but minimal recovery of limb fat were seen 96 weeks after switching from lamivudine/zidovudine plus efavirenz to fixed-dose efavirenz/emtricitabine/tenofovir DF in HIV-infected patients [abstract and poster no. H-1572]. 49th Interscience Conference on Antimicrobial Agents and Chemotherapy; 2009 Sep 12–15; San Francisco (CA)
23.
Zurück zum Zitat Feng JY, Ly JK, Myrick F, et al. The triple combination of tenofovir, emtricitabine and efavirenz shows synergistic anti-HIV-1 activity in vitro: a mechanism of action study. Retrovirology 2009 May 13; 6: 44PubMedCrossRef Feng JY, Ly JK, Myrick F, et al. The triple combination of tenofovir, emtricitabine and efavirenz shows synergistic anti-HIV-1 activity in vitro: a mechanism of action study. Retrovirology 2009 May 13; 6: 44PubMedCrossRef
24.
Zurück zum Zitat Llibre JM, Santos JR, Puig T, et al. Prevalence of etravirine-associated mutations in clinical samples with resistance to nevirapine and efavirenz. J Antimicrob Chemother 2008 Nov; 62(5): 909–13PubMedCrossRef Llibre JM, Santos JR, Puig T, et al. Prevalence of etravirine-associated mutations in clinical samples with resistance to nevirapine and efavirenz. J Antimicrob Chemother 2008 Nov; 62(5): 909–13PubMedCrossRef
25.
Zurück zum Zitat Gallant JE, DeJesus E, Arribas JR, et al. Tenofovir DF, emtricitabine, and efavirenz vs. zidovudine, lamivudine, and efavirenz for HIV. N Engl J Med 2006 Jan 19; 354(3): 251–60 Gallant JE, DeJesus E, Arribas JR, et al. Tenofovir DF, emtricitabine, and efavirenz vs. zidovudine, lamivudine, and efavirenz for HIV. N Engl J Med 2006 Jan 19; 354(3): 251–60
26.
Zurück zum Zitat Pozniak AL, Gallant JE, DeJesus E, et al. Tenofovir disoproxil fumarate, emtricitabine, and efavirenz versus fixed-dose zidovudine/lamivudine and efavirenz in antiretroviral-naive patients: virologic, immunologic, and morphologic changes — a 96-week analysis. J Acquir Immune Defic Syndr 2006 Dec 15; 43(5): 535–40PubMed Pozniak AL, Gallant JE, DeJesus E, et al. Tenofovir disoproxil fumarate, emtricitabine, and efavirenz versus fixed-dose zidovudine/lamivudine and efavirenz in antiretroviral-naive patients: virologic, immunologic, and morphologic changes — a 96-week analysis. J Acquir Immune Defic Syndr 2006 Dec 15; 43(5): 535–40PubMed
27.
Zurück zum Zitat Arribas JR, Pozniak AL, Gallant JE, et al. Tenofovir disoproxil fumarate, emtricitabine, and efavirenz compared with zidovudine/lamivudine and efavirenz in treatment-naive patients: 144-week analysis. J Acquir Immune Defic Syndr 2008 Jan 1; 47(1): 74–8PubMedCrossRef Arribas JR, Pozniak AL, Gallant JE, et al. Tenofovir disoproxil fumarate, emtricitabine, and efavirenz compared with zidovudine/lamivudine and efavirenz in treatment-naive patients: 144-week analysis. J Acquir Immune Defic Syndr 2008 Jan 1; 47(1): 74–8PubMedCrossRef
28.
Zurück zum Zitat Mathias AA, Hinkle J, Menning M, et al. Bioequivalence of efavirenz/emtricitabine/tenofovir disoproxil fumarate single-tablet regimen. J Acquir Immune Defic Syndr 2007 Oct 1; 46(2): 167–73PubMedCrossRef Mathias AA, Hinkle J, Menning M, et al. Bioequivalence of efavirenz/emtricitabine/tenofovir disoproxil fumarate single-tablet regimen. J Acquir Immune Defic Syndr 2007 Oct 1; 46(2): 167–73PubMedCrossRef
30.
Zurück zum Zitat Airoldi M, Zaccarelli M, Bisi L, et al. One-pill once-a-day HAART: a simplification strategy that improves adherence and quality of life of HIV-infected subjects. Patient Prefer Adherence 2010 May 13; 4: 115–25PubMed Airoldi M, Zaccarelli M, Bisi L, et al. One-pill once-a-day HAART: a simplification strategy that improves adherence and quality of life of HIV-infected subjects. Patient Prefer Adherence 2010 May 13; 4: 115–25PubMed
31.
Zurück zum Zitat Gilead Sciences. ROCKET I — randomized open label switch for cholesterol elevation on kivexa evaluation trial [ClinicalTrials.gov identifier NCT00615810]. US National Institutes of Health, ClinicalTrials.gov [online]. Available from URL: http://www.clinicaltrials.gov [Accessed 2010 Aug 16] Gilead Sciences. ROCKET I — randomized open label switch for cholesterol elevation on kivexa evaluation trial [ClinicalTrials.gov identifier NCT00615810]. US National Institutes of Health, ClinicalTrials.gov [online]. Available from URL: http://​www.​clinicaltrials.​gov [Accessed 2010 Aug 16]
33.
Zurück zum Zitat Hodder SL, Mounzer K, DeJesus E, et al. Patient-reported outcomes in virologically suppressed, HIV-1-infected subjects after switching to a simplified, single-tablet regimen of efavirenz, emtricitabine, and tenofovir DF. AIDS Patient Care STDS 2010 Feb; 24(2): 87–96PubMedCrossRef Hodder SL, Mounzer K, DeJesus E, et al. Patient-reported outcomes in virologically suppressed, HIV-1-infected subjects after switching to a simplified, single-tablet regimen of efavirenz, emtricitabine, and tenofovir DF. AIDS Patient Care STDS 2010 Feb; 24(2): 87–96PubMedCrossRef
34.
Zurück zum Zitat Gallant JE, Staszewski S, Pozniak AL, et al. Efficacy and safety of tenofovir DF vs stavudine in combination therapy in antiretroviral-naive patients: a 3-year randomized trial. JAMA 2004 Jul 14; 292(2): 191–201PubMedCrossRef Gallant JE, Staszewski S, Pozniak AL, et al. Efficacy and safety of tenofovir DF vs stavudine in combination therapy in antiretroviral-naive patients: a 3-year randomized trial. JAMA 2004 Jul 14; 292(2): 191–201PubMedCrossRef
35.
Zurück zum Zitat Cassetti I, Valdez J, Madruga R, et al. The safety and efficacy of tenofovir DF in combination with lamivudine and efavirenz through 6 years in antiretroviral-naive HIV-1-infected patients. HIV Clin Trials 2007 May–Jun; 8(3): 164–72PubMedCrossRef Cassetti I, Valdez J, Madruga R, et al. The safety and efficacy of tenofovir DF in combination with lamivudine and efavirenz through 6 years in antiretroviral-naive HIV-1-infected patients. HIV Clin Trials 2007 May–Jun; 8(3): 164–72PubMedCrossRef
36.
Zurück zum Zitat Cassetti I, Madruga JVR, Etzel A, et al. The safety and efficacy of tenofovir DF (TDF) in combination with lamivudine (3TC) and efavirenz (EFV) in antiretroviral-naive patients through seven years [poster no. TUPE0057]. 17th International AIDS Conference; 2008 Aug 3–8; Mexico City Cassetti I, Madruga JVR, Etzel A, et al. The safety and efficacy of tenofovir DF (TDF) in combination with lamivudine (3TC) and efavirenz (EFV) in antiretroviral-naive patients through seven years [poster no. TUPE0057]. 17th International AIDS Conference; 2008 Aug 3–8; Mexico City
37.
Zurück zum Zitat Lagnese M, Daar ES. Antiretroviral regimens for treatment-experienced patients with HIV-1 infection. Expert Opin Pharmacother 2008 Apr; 9(5): 687–700PubMedCrossRef Lagnese M, Daar ES. Antiretroviral regimens for treatment-experienced patients with HIV-1 infection. Expert Opin Pharmacother 2008 Apr; 9(5): 687–700PubMedCrossRef
38.
Zurück zum Zitat Volberding PA, Deeks SG. Antiretroviral therapy and management of HIV infection. Lancet 2010 Jul 3; 376: 49–62PubMedCrossRef Volberding PA, Deeks SG. Antiretroviral therapy and management of HIV infection. Lancet 2010 Jul 3; 376: 49–62PubMedCrossRef
39.
Zurück zum Zitat Powderly WG. Limitations of current HIV therapies: opportunities for improvement. JAIDS 2003 Jun 1; 33 Suppl. 1: S7–16PubMed Powderly WG. Limitations of current HIV therapies: opportunities for improvement. JAIDS 2003 Jun 1; 33 Suppl. 1: S7–16PubMed
40.
Zurück zum Zitat Bangsberg DR, Ragland K, Monk A, et al. A one-pill, once-daily, fixed-dose combination (FDC) of efavirenz, emtricitabine, and tenofovir disoproxil fumarate (EFV/FTC/TDF) regimen is associated with higher unannounced pill count adherence than non-one pill, once-daily [poster no. 510]. 17th Conference on Retroviruses and Opportunistic Infections; 2010 Feb 16–19; San Francisco (CA) Bangsberg DR, Ragland K, Monk A, et al. A one-pill, once-daily, fixed-dose combination (FDC) of efavirenz, emtricitabine, and tenofovir disoproxil fumarate (EFV/FTC/TDF) regimen is associated with higher unannounced pill count adherence than non-one pill, once-daily [poster no. 510]. 17th Conference on Retroviruses and Opportunistic Infections; 2010 Feb 16–19; San Francisco (CA)
42.
Zurück zum Zitat Szczech LA. Renal dysfunction and tenofovir toxicity in HIV-infected patients. Top HIV Med 2008 Oct–Nov; 16(4): 122–6PubMed Szczech LA. Renal dysfunction and tenofovir toxicity in HIV-infected patients. Top HIV Med 2008 Oct–Nov; 16(4): 122–6PubMed
43.
Zurück zum Zitat Izzedine H, Launay-Vacher V, Deray G. Antiviral drug-induced nephrotoxicity. Am J Kidney Dis 2005 May; 45(5): 804–17PubMedCrossRef Izzedine H, Launay-Vacher V, Deray G. Antiviral drug-induced nephrotoxicity. Am J Kidney Dis 2005 May; 45(5): 804–17PubMedCrossRef
Metadaten
Titel
Efavirenz/Emtricitabine/Tenofovir Disoproxil Fumarate Single-Tablet Regimen (Atripla®)
A Review of its Use in the Management of HIV Infection
verfasst von
Emma D. Deeks
Caroline M. Perry
Publikationsdatum
01.12.2010
Verlag
Springer International Publishing
Erschienen in
Drugs / Ausgabe 17/2010
Print ISSN: 0012-6667
Elektronische ISSN: 1179-1950
DOI
https://doi.org/10.2165/11203800-000000000-00000

Weitere Artikel der Ausgabe 17/2010

Drugs 17/2010 Zur Ausgabe

Adis Drug Profile

Fentanyl Sublingual

Adis Drug Profile

Indacaterol

Adis Drug Profile

Trastuzumab