Multiple choices for HIV therapy with integrase strand transfer inhibitors

Retrovirology

Mark A Wainberg¹  Francois Raffi² 

[1] McGill University AIDS Centre, Lady Davis Institute, Jewish General Hospital, 3755 Côte-Sainte-Catherine Rd, Montreal, QC H3T 1E2, Canada;University Hospital of Nantes, EA 4271, 1 Place Ricordeau, Nantes cedex 1 44093, France

关键词: Integrase strand transfer inhibitors;    Dolutegravir;    Elvitegravir;    Raltegravir;   

Others  :  1209214
DOI  :  10.1186/1742-4690-9-110

 received in 2012-11-02, accepted in 2012-12-10,  发布年份 2012

【 摘 要 】

Two integrases inhibitors, raltegravir and elvitegravir, have now been approved by regulatory agencies for use in the treatment of HIV-infected patients; and the approval of a third such drug, dolutegravir, is expected during 2013 on the basis of several phase 3 clinical trials. The advent of this new class of antiretroviral (ARV) medications represents a major advance in the management of HIV infection, and each of these three drugs can be expected to continue to be an important component of ARV combination regimens.

【 授权许可】

   
2012 Raffi and Wainberg; licensee BioMed Central Ltd.

【 参考文献 】

• [1]Malet I, Calvez V, Marcelin AG: The future of integrase inhibitors of HIV-1. Curr Opin Virol 2012, 2:580-587.
• [2]Koh Y, Matreyek KA, Engelman A: Differential sensitivities of retroviruses to integrase strand transfer inhibitors. J Virol 2011, 85:3677-3682.
• [3]Mesplede T, Quashie PK, Wainberg MA: Resistance to HIV integrase inhibitors. Curr Opin HIV AIDS 2012, 7(5):401-408.
• [4]Ni XJ, Delilis O, Charpentier C, Storto A, Collin G, Damond F, Descamps D, Mouscadet JF: G140S/Q148R and N155H mutations render HIV-2 integrase resistant to raltegravir whereas Y143C does not. Retrovirology 2011, 8:68. BioMed Central Full Text
• [5]Sax PE, DeJesus E, Mills A, Zolopa A, Cohen C, Wohl D, Gallant JE, Liu HC, Zhong L, Yale K, 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.
• [6]DeJesus E, Rockstroh JK, Henry K, Molina JM, Gathe J, Ramanathan S, Wei X, Yale K, Szwarcberg J, White 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.
• [7]Molina JM, Lamarca A, Andrade-Villanueva J, Clotet B, Clumeck N, Liu YP, Zhong L, Margot N, Cheng AK, Chuck SL: 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.
• [8]Li JZ, Paredes R, Ribaudo HJ, Svarovskaia ES, Metzner KJ, Kozal MJ, Hullsiek KH, Balduin M, Jakobsen MR, Geretti AM, et al.: Low-frequency HIV-1 drug resistance mutations and risk of NNRTI-based antiretroviral treatment failure: a systematic review and pooled analysis. JAMA 2011, 305:1327-1335.
• [9]Rockstroh J, DeJesus E, Saag M, Yazdanpanah Y, Lennox J, Wan H, Rodgers A, Dinubile MJ, Nguyen BY, Teppler H, Leavitt R, Sklar P, for the STARTMRK Study Team: Long-term safety and efficacy of raltegravir-based versus efavirenz-based combination therapy in treatment-naïve HIV-1 infected patients: final 5-Yr double-blind results from STARTMRK. Washington DC: Abstract LBPE19; 2012. [IAC]
• [10]Lennox JL, DeJesus E, Lazzarin A, Pollard RB, Madruga JV, Berger DS, Zhao J, Xu X, Williams-Diaz A, Rodgers AJ, et al.: Safety and efficacy of raltegravir-based versus efavirenz-based combination therapy in treatment-naive patients with HIV-1 infection: a multicentre, double-blind randomised controlled trial. Lancet 2009, 374:796-806.
• [11]Rizk ML, Hang Y, Luo WL, Su J, Zhao J, Campbell H, Nguyen BY, Sklar P, Eron JJ Jr, Wenning L: Pharmacokinetics and pharmacodynamics of once-daily versus twice-daily raltegravir in treatment-naive HIV-infected patients. Antimicrob Agents Chemother 2012, 56:3101-3106.
• [12]Eron JJ Jr, Rockstroh JK, Reynes J, Andrade-Villanueva J, Ramalho-Madruga JV, Bekker LG, Young B, Katlama C, Gatell-Artigas JM, Arribas JR, et al.: Raltegravir once daily or twice daily in previously untreated patients with HIV-1: a randomised, active-controlled, phase 3 non-inferiority trial. Lancet Infect Dis 2011, 11:907-915.
• [13]Gras G, Schneider MP, Cavassini M, Lucht F, Loilier M, Verdon R, Bernard L, Parienti JJ: Patterns of Adherence to Raltegravir-Based Regimens and the Risk of Virological Failure Among HIV-Infected Patients: The RALTECAPS Cohort Study. J Acquir Immune Defic Syndr 2012, 61:265-269.
• [14]Walmsley S, Antela A, Clumeck N, Duiculescu D, Eberhard A, Gutiérrez F, et al.: Dolutegravir (DTG; S/GSK1349572) + abacavir/lamivudine once daily statistically superior to tenofovir/emtricitabine/efavirenz: 48-week results - SINGLE (ING114467). Abstract H-556b. San Francisco, CA, USA; 2012. [52nd Interscience Conference on Antimicrobial Agents and Chemotherapy; September 9–12, 2012]
• [15]Raffi F, Rachlis A, Stellbrink HJ, Hardy WD, Torti C, Orkin C, et al, on behalf of the SPRING-2 study group, et al.: Once-daily dolutegravirversus raltegravir in antiretroviral naive adults with HIV-1 infection: 48 week results from the randomised, double-blind, non-inferiority SPRING-2 study. Lancet 2012. accepted Oct 25, 2012