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Dolutegravir: A Review of Its Use in the Management of HIV-1 Infection in Adolescents and Adults

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Abstract

Dolutegravir (Tivicay®) is a new-generation HIV-1 integrase strand transfer inhibitor recently approved in the EU and Japan for the treatment of HIV-1 infection in adolescents and adults in combination with other antiretroviral drugs. It is suitable for once-daily administration and achieves therapeutic concentrations without the need for pharmacokinetic boosting. It has a high barrier to resistance and is generally active against viral strains resistant to first-generation integrase inhibitors. In well-designed clinical trials in treatment-naive or treatment-experienced, integrase inhibitor-naive patients, dolutegravir-based combinations were shown to be noninferior or superior to raltegravir-based combinations, an efavirenz-based combination and ritonavir-boosted darunavir-based combinations with respect to virological suppression (plasma HIV-1 RNA <50 copies/mL) at week 48. Dolutegravir was also effective in a high proportion of patients failing on raltegravir- or elvitegravir-based therapy as a result of integrase resistance mutations. Dolutegravir was generally well tolerated, with the vast majority of adverse events being mild or moderate in intensity; serious adverse events were uncommon. Therefore, dolutegravir is an important new addition to the expanding list of antiretroviral drugs for treating HIV-1 infection in adults and adolescents.

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Disclosure

The preparation of this review was not supported by any external funding. During the peer review process, the manufacturer of the agent under review was offered an opportunity to comment on this article. Changes resulting from comments received were made by the author on the basis of scientific and editorial merit. Paul McCormack is a salaried employee of Adis/Springer.

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  1. Adis, Level 1, 5 The Warehouse Way, Northcote 0627; Private Bag 65901, Mairangi Bay 0754, Auckland, New Zealand

    Paul L. McCormack

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Correspondence to Paul L. McCormack.

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The manuscript was reviewed by: J.L. Blanco, Division of Infectious Diseases, Hospital Clinic, University of Barcelona, Barcelona, Spain; P. Domingo, Infectious Diseases Unit, Hospital Santa Creu I Sant Pau, Autonomous University of Barcelona, Barcelona, Spain; S.J. Hurwitz, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Center for AIDS Research, Emory University School of Medicine/VA Medical Center, Atlanta, GA, USA; M.A. Wainberg, McGill University AIDS Centre, Lady Davis Institute for Medical Research, Jewish General Hospital, Montreal, Quebec, Canada.

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McCormack, P.L. Dolutegravir: A Review of Its Use in the Management of HIV-1 Infection in Adolescents and Adults. Drugs 74, 1241–1252 (2014). https://doi.org/10.1007/s40265-014-0256-y

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