Classes of Antiretroviral Medications

Module 6, Version 4


  • Bourgi K, Jenkins C, Rebeiro PF, et al. Weight gain among treatment-naïve persons with HIV starting integrase inhibitors compared to non-nucleoside reverse transcriptase inhibitors or protease inhibitors in a large observational cohort in the United States and Canada. Conference on Retroviruses and Opportunistic Infections. J Int AIDS Soc. 2020;23(4);e25484. Published online 2020 April 15.
  • Clotet B, Feinberg J, van Lunzen J, et al., and the ING114915 Study Team. Once-daily dolutegravir versus darunavir plus ritonavir in antiretroviral-naïve adults with HIV-1 infection (FLAMINGO): 48-week results from the randomized open-label phase IIIb study. Lancet. 2014;383:2222-2231.
  • Cohen CJ, Molina JM, Cahn P, et al. Efficacy and safety of rilpivirine (TMC278) versus efavirenz at 48 weeks in treatment-naïve HIV-1-infected patients: Pooled results from the phase III double-blind randomized ECHO and THRIVE Trials. J Acquir Immune Defic Syndr. 2012;60:33-42.
  • 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 randomized, double-blind, phase III, noninferiority trial. Lancet. 2012;79:2429-2438. 
  • Gallant J, Lazzarin A, Mills A, et al. Bictegravir, emtricitabine, and tenofovir alafenamide versus dolutegravir, abacavir, and lamivudine for initial treatment of HIV-1 infection (GS-US-380-1489): a double-blind, multicentre, phase 3 randomized controlled non-inferiority trial. Lancet. 2017; 390. 2063-2072.
  • The INSIGHT START Study Group. Initiation of antiretroviral therapy in early asymptomatic HIV infection. N Engl J Med. 2015;373:795-807.
  • Johnson M, Gatey C, Manosuthi W, et al. Efficacy of dolutegravir/abacavir/lamivudine (DTG/ABC/3TC) fixed-dose combination (FDC) compared with ritonavir-boosted atazanavir (ATV/r) plus tenofovir fumarate/emtricitabine (TDF/FTC) in treatment-naïve women with HIV-1 infection (ARIA study): Subgroup analyses. J Intl AIDS Soc. 2016; 19 (8Suppl7); 2148.
  • Lennox JL, DeJesus E, Lazzarin A, et al. Safety and efficacy of raltegravir-based versus efavirenz-based combination therapy in treatment-naïve patients with HIV-1 infection: A multicentre, double blind randomized controlled trial. Lancet. 2009;374:796-806.
  • Lennox JL, Landovitz RJ, Ribaudo HJ, et al. Efficacy and tolerability of 3 nonnucleoside reverse transcriptase inhibitor-sparing antiretroviral regimens for treatment-naïve volunteers infected with HIV-1: A randomized, controlled equivalence trial. Ann Intern Med. 2014;161:461-471.
  • Llibre JM, Hung CC, Brinson C, et al. Efficacy, safety and tolerability of dolutegravir-rilpivirine for the maintenance of virological suppression in adults with HIV-1: phase 3, randomized, non-inferiority SWORD-1 and SWORD-2 studies. Lancet. January 5, 2018.
  • Mallal S, Phillips E, Carosi G, et al. HLA-B*5701 screening for hypersensitivity to abacavir. N Engl J Med. 2008;358:568-579.
  • Molina JM, Clotet B, van Lunzen J, et al. Once-daily dolutegravir is superior to once-daily darunavir/ritonavir in treatment-naïve HIV-1-positive individuals: 96-week results from FLAMINGO. J Int AIDS Soc. 2014;17(4 Suppl 3):19490.
  • Nowcika-Sans B, Protack T, Lin Z, et al. BMS-955176: Identification and Characterization of a Second-Generation HIV-1 Maturation Inhibitor with Improved Potency, Anti-viral Spectrum and Gag Polymorphic Coverage. Antimicrob Agents Chemother. 2016 Apr 18. pii: AAC.02560-15. [Epub ahead of print].
  • Orkin C, DeJesus E, Khanlou H, et al. Final 192-week efficacy and safety of once-daily darunavir/ritonavir compared with lopinavir/ritonavir in HIV-1-infected treatment-naïve patients in the ARTEMIS trial. HIV Med. 2013;14:49-59.
  • Orrell C, Hagins D, Belonosova E, et al. “Fixed-dose combination of dolutegravir, abacavir, lamivudine versus ritonavir boosted atazanavir plus tenofovir disoproxil fumarate and emtricitabine in previously untreated women with HIV-1 Infection (ARIA): week 48 results from a randomized, open-label, non-inferiority, phase 3b study. Lancet HIV. 2017 Dec;4(12):e536-e546.
  • Ortiz R, Dejesus E, Khanlou H, et al. Efficacy and safety of once-daily darunavir/ritonavir versus lopinavir/ritonavir in treatment-naïve HIV-1-infected patients at week 48. AIDS. 2008;22:1389-1397.
  • Pozniak A, Arribas J, Gupta SK, et al. Switching to tenofovir alafenamide, coformulated with elvitegravir, cobicistat, and emtricitabine, in HIV-1 infected patients with renal impairment: 48-week results from a single-arm, multicenter, open-label phase 3 study. J Acquir Immune Defic Syndr. 2016 Apr 16;71(5):530-7.
  • Raffi F, Jaeger H, Quiros-Roldan E, et al. Once-daily dolutegravir versus twice-daily raltegravir in antiretroviral-naïve adults with HIV-1 infection (SPRING-2 study): 96-week results from a randomized, double-blind, non-inferiority trial. Lancet Infect Dis. 2013;13:927-935.
  • Raffi F, Rachlis A, Stellbrink HJ, et al. Once-daily dolutegravir versus raltegravir in antiretroviral-naïve adults with HIV-1 infection: 48-week results from the randomized, double-blind, non-inferiority SPRING-2 study. Lancet. 2013;381:735-743.
  • Rockstroh JK, DeJesus E, Lennox JL, et al. Durable efficacy and safety of raltegravir versus efavirenz when combined with tenofovir/emtricitabine in treatment-naïve HIV-1-infected patients: Final 5-year results from STARTMRK. J Acquir Immune Defic Syndr. 2013;63:77-85.
  • Rotger M, Colombo S, Furrer H, et al. Influence of CYP2B6 polymorphism on plasma and intracellular concentrations and toxicity of efavirenz and nevirapine in HIV-infected patients. Pharmacogenet Genomics. 2005;15:1-5.
  • Rotger M, Taffe P, Bleiber G, et al. Gilbert syndrome and the development of antiretroviral therapy-associated hyperbilirubinemia. J Infect Dis. 2005;192:1381-1386.
  • Saag MS, Gandhi RT, Hoy JF et al. Antiretroviral Drugs for Treatment and Prevention of HIV Infection in Adults: 2018 Recommendations of the International Antiviral Society-USA Panel. JAMA. 2020;324(16):1651-1669.
  • Sax PE, DeJesus E, Mills A, et al. Co-formulated elvitegravir, cobicistat, emtricitabine, and tenofovir versus coformulated efavirenz, emtricitabine, and tenofovir for initial treatment of HIV-1 infection: A randomized, double-blind, phase III trial, analysis of results after 48 weeks. Lancet. 2012;379:2439-2448.
  • Sax PE, Erlandson KM, Lake JE, et al. Weight gain following initiation of antiretroviral therapy: Risk factors in randomized comparative clinical trials. Clin Inf Dis. 2019 Oct 14:ciz999. doi: 10.1093/cid/ciz999. Online ahead of print.
  • Sax P, Pozniak A, Montes, ML, et al. Coformulated bictegravir, emtricitabine, and tenofovir alafenamide versus dolutegravir with emtricitabine and tenofovir alafenamide, for initial treatment of HIV-1 infection (GS-US-380-1490): a randomized, double blind, multicentre, phase 3, non-inferiority trial. Lancet. 2017; 390. 2073-2082.
  • 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 randomized, double-blind, phase III, non-inferiority trials. Lancet. 2015;85:2606-2615.
  • Squires K, Kityo C, Hodder S, et al. Integrase inhibitor versus protease inhibitor based regimen for HIV-1 infected women (WAVES): a randomized, controlled, double-blind, phase 3 study. Lancet HIV. 2016;3(9)e410-e420. Epub 2016 May 27.
  • Teuscher N. Learn PK/ Accessed 6/24/16.
  • Trottier B, Lake J, Logue K, et al. Dolutegravir/abacavir/lamivudine vs current ART in virally suppressed patients : A 48-week, randomized, non-inferiority, open-label, phase IIIb study. Antiviral Therapy. 2017;10.3851MP3166. (STRIIVING).
  • vanWyk, J, Ajana F, Bisshop F, et al. Efficacy and Safety of Switching to Dolutegravir/lamivudine Fixed-Dose Two-Drug Regimen versus Continuing a Tenofovir Alafenamide-Based Three- or Four-Drug Regimen for Maintenance of Virologic Suppression in Adults with HIV-1: Phase 3, Randomized, Non-inferiority TANGO Study. Clin Infect Dis. 2020 6;ciz1243. doi: 10.1093/cid/ciz1243. Online ahead of print.
  • Walmsley SL, Antela A, Clumeck N, et al. Dolutegravir plus abacavir-lamivudine for the treatment of HIV-1 infection. N Engl J Med. 2013;369:1807-1818.
  • Walmsley SL, Baumgarten A, Berenguer J, et al. Brief report: Dolutegravir plus abacavir/lamivudine for the treatment of HIV-1 infection in antiretroviral therapy-naïve patients: Week 96 and week 144 results from the single randomized clinical trial. J Acquir Immune Defic Syndr. 2015;70:515-519.
  • 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(3):e118-120.
  • Zash R, Holmes L, Diseko M, et al. Neural-tube defects and antiretroviral treatment regimens in Botswana. N Engl J Med. 2019;381(9):827-840. Available at:
  • Dunn K, Guillermo Castro J, DeJesus E, et al. High Rates of Virologic Suppression Achieved in MSM or Black/African American Individuals Using a Rapid Initiation Model of Care for Patients Newly Diagnosed with HIV-1 Infection: A Week 24 Interim Analysis of the DIAMOND Study. 2019 African American MSM Leadership Conference on Health Disparities and Social Justice. January 17-20, 2019. Arlington, VA.
  • Mills A, Priest J, Wicks N, et al. Adherence and Persistency with Modern Single vs Multi-Tablet Antiretroviral (ARV) Regimens in 1st Treatment of HIV in Clinical Practice. ID Week 2018. San Francisco, CA October 3-7, 2018.
  • Zash R, et al. Update on neural tube defects with antiretroviral exposure in the Tsepamo study, Botswana. J Int AIDS Soc. 2020;23(suppl 4):183-184. Abstract OAXLB0102.

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