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Clinical pharmacokinetics and pharmacodynamics of dolutegravir used as a single tablet regimen for the treatment of HIV-1 infection
Authors:Pauline Bollen  Peter Reiss  Jonathan Schapiro  David Burger
Affiliation:1. Radboud University Medical Center, Department of Pharmacy, Geert Grooteplein-Zuid 10 6525 GA Nijmegen, The Netherlands pauline.bollen@radboudumc.nl;2. Radboud Institute for Health Sciences (RIHS), Nijmegen, The Netherlands;3. Elisabeth TweeSteden Hospital, Hospital Pharmacy Midden-Brabant, Tilburg, The Netherlands;4. University of Amsterdam, Academic Medical Center, Division of Infectious Diseases and Department of Global Health, Amsterdam, The Netherlands;5. National Hemophilia Center, Sheba Medical Center, Ramat Gan, Israel
Abstract:Introduction: With the introduction of the coformulated dolutegravir, abacavir and lamivudine, a new single tablet regimen (STR) is made available for the use in treatment-naive and treatment-experienced HIV-infected patients. This drug combination is the fourth STR that will be positioned next to the STRs with efavirenz, rilpivirine or elvitegravir as third agents, respectively.

Areas covered: The objective of this review is to provide an overview of the efficacy and safety of the combined dolutegravir/abacavir/lamivudine coformulation. The review will focus on dolutegravir and includes both published data as well as data presented at recent major international HIV/AIDS conferences.

Expert opinion: The dolutegravir/abacavir/lamivudine regimen is highly effective in achieving sustained suppression of HIV-1 RNA plasma concentrations. The STR has a favorable safety profile and a low potential for drug interactions, which will contribute to a prominent role in therapy. As this STR contains abacavir as backbone component, the use requires patients to be HLA-B*5701 negative, with good hepatic function. Other first-line treatment combinations are preferred for patients with hepatitis B co-infection or with a high cardiovascular risk.
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