A once-daily tablet formulation (Isentress® HD; Isentress® 600 mg) of the integrase strand transfer inhibitor raltegravir is now available for the treatment of HIV-1 infection. The 600 mg tablet has improved bioavailability versus the existing twice-daily 400 mg tablet (due, at least in part, to differences in tablet dissolution) and the recommended dosage is 1200 mg (i.e. two 600 mg tablets) once daily. In combination with emtricitabine/tenofovir disoproxil fumarate in treatment-naïve adults, once-daily raltegravir 1200 mg provided virological suppression non-inferior to that seen with twice-daily raltegravir 400 mg over 48 and 96 weeks in the phase 3 ONCEMRK trial. The once-daily raltegravir regimen was also generally well tolerated in this study, displaying a tolerability profile similar to that of the twice-daily regimen. The once-daily tablet simplifies and improves the convenience of raltegravir regimens, although its impact on adherence has yet to be determined. Thus, once-daily raltegravir tablets are a convenient alternative to twice-daily raltegravir tablets for the treatment of HIV-1, further expanding the therapeutic options available to meet the diverse needs of this patient population.
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During the peer review process, the manufacturer of once-daily raltegravir was also offered an opportunity to review this article. Changes resulting from comments received were made on the basis of scientific and editorial merit.
The preparation of this review was not supported by any external funding.
Conflict of interest
Emma Deeks is a salaried employee of Adis/Springer, is responsible for the article content and declares no relevant conflicts of interest.
Additional information about this Adis Drug Review can be found at http://www.medengine.com/preview-internal/single/114368.
The manuscript was reviewed by: C. Bernardini, Infectious Disease and Internal Medicine Division, ARUD Zentren für Suchtmedizin, Zürich, Switzerland; D. M. Burger, Radboud University Medical Centre, Nijmegen, The Netherlands; M. Liedtke, College of Pharmacy, University of Oklahoma, Oklahoma City, OK, USA; O. Kirk, CHIP, Department of Infectious Diseases, University of Copenhagen, Copenhagen, Denmark; T. Klimkait, Department of Biomedicine, Institute for Medical Microbiology, University of Basel, Basel, Switzerland; R. L. Murphy, Center for Global Health, Northwestern University, Chicago, IL, USA; M. Nelson, Chelsea & Westminster Hospital, London, UK; R. van der Galien, Radboud University Medical Centre, Nijmegen, The Netherlands.
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Deeks, E.D. Raltegravir Once-Daily Tablet: A Review in HIV-1 Infection. Drugs 77, 1789–1795 (2017). https://doi.org/10.1007/s40265-017-0827-9