Skip to main content
SpringerLink
Log in

Raltegravir Once-Daily Tablet: A Review in HIV-1 Infection

  • Adis Drug Evaluation
  • Published:
Drugs Aims and scope Submit manuscript

Abstract

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.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Fig. 1

Similar content being viewed by others

References

  1. British HIV Association. British HIV Association guidelines for the treatment of HIV-1-positive adults with antiretroviral therapy 2015 (2016 interim update). 2016. http://www.bhiva.org/guidelines.aspx. Accessed 19 Sept 2017.

  2. European AIDS Clinical Society. Guidelines version 8.2. 2017. http://www.eacsociety.org. Accessed 19 Sept 2017.

  3. Department of Health and Human Services USA. Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents. 2016. https://aidsinfo.nih.gov/contentfiles/lvguidelines/adultandadolescentgl.pdf. Accessed 18 Sep 2017.

  4. Gunthard HF, Saag MS, Benson CA, et al. Antiretroviral drugs for treatment and prevention of HIV infection in adults: 2016 recommendations of the International Antiviral Society—USA Panel. JAMA. 2016;316(2):191–210.

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  5. Perry CM. Raltegravir: a review of its use in the management of HIV-1 infection in children and adolescents. Paediatr Drugs. 2014;16(1):91–100.

    Article  PubMed  Google Scholar 

  6. Croxtall JD, Keam SJ. Raltegravir: a review of its use in the management of HIV infection in treatment-experienced patients. Drugs. 2009;69(8):1059–75.

    Article  CAS  PubMed  Google Scholar 

  7. Croxtall JD, Lyseng-Williamson KA, Perry CM. Raltegravir Drugs. 2008;68(1):131–8.

    Article  CAS  PubMed  Google Scholar 

  8. Croxtall JD, Scott LJ. Raltegravir: in treatment-naive patients with HIV-1 infection. Drugs. 2010;70(5):631–42.

    Article  CAS  PubMed  Google Scholar 

  9. Nguyen BY, Isaacs RD, Teppler H, et al. Raltegravir: the first HIV-1 integrase strand transfer inhibitor in the HIV armamentarium. Ann N Y Acad Sci. 2011;1222:83–9.

    Article  CAS  PubMed  Google Scholar 

  10. Liedtke MD, Tomlin CR, Lockhart SM, et al. Long-term efficacy and safety of raltegravir in the management of HIV infection. Infect Drug Resist. 2014;7:73–84.

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  11. Sharma M, Walmsley SL. Raltegravir as antiretroviral therapy in HIV/AIDS. Expert Opin Pharmacother. 2014;15(3):395–405.

    Article  CAS  PubMed  Google Scholar 

  12. Calcagno A, D’Avolio A, Bonora S. Pharmacokinetic and pharmacodynamic evaluation of raltegravir and experience from clinical trials in HIV-positive patients. Expert Opin Drug Metab Toxicol. 2015;11(7):1167–76.

    Article  CAS  PubMed  Google Scholar 

  13. Eron JJ Jr, Rockstroh JK, Reynes J, 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(12):907–15.

    Article  CAS  PubMed  Google Scholar 

  14. Merck Sharp & Dohme Ltd. Isentress 600 mg film-coated tablets: EU summary of product characteristics. 2017. http://www.ema.europa.eu. Accessed 19 Sept 2017.

  15. Merck & Co Inc. Isentress® (raltegravir): US prescribing information. 2017. https://www.fda.gov. Accessed 19 Sept 2017.

  16. Cahn P, Kaplan R, Sax P, et al. Raltegravir 1200 mg once daily versus raltegravir 400 mg twice daily, in combination with tenofovir disoproxil fumarate/emtricitabine, in previously untreated HIV-1 infection through week 96 [Poster]. In: 9th international AIDS society conference; 2017.

  17. Malet I, Thierry E, Wirden M, et al. Combination of two pathways involved in raltegravir resistance confers dolutegravir resistance. J Antimicrob Chemother. 2015;70(10):2870–80.

    Article  CAS  PubMed  Google Scholar 

  18. Krishna R, Rizk ML, Larson P, et al. Single- and multiple-dose pharmacokinetics of once-daily formulations of raltegravir. Clin Pharmacol Drug Dev. 2017. doi:10.1002/cpdd.358.2017.

    PubMed  Google Scholar 

  19. Cahn P, Kaplan R, Sax PE, et al. Raltegravir 1200 mg once daily versus raltegravir 400 mg twice daily, with tenofovir disoproxil fumarate and emtricitabine, for previously untreated HIV-1 infection: a randomised, double-blind, parallel-group, phase 3 non-inferiority trial. Lancet HIV. 2017. doi:10.1016/S2352-3018(17)30128-5.

    PubMed  Google Scholar 

  20. Krishna R, East L, Larson P, et al. Atazanavir increases the plasma concentrations of 1200 mg raltegravir dose. Biopharm Drug Dispos. 2016;37(9):533–41.

    Article  CAS  PubMed  Google Scholar 

  21. Krishna R, East L, Larson P, et al. Efavirenz does not meaningfully affect the single dose pharmacokinetics of 1200 mg raltegravir. Biopharm Drug Dispos. 2016;37(9):542–9.

    Article  CAS  PubMed  Google Scholar 

  22. Krishna R, East L, Larson P, et al. Effect of metal-cation antacids on the pharmacokinetics of 1200 mg raltegravir. J Pharm Pharmacol. 2016;68(11):1359–65.

    Article  CAS  PubMed  Google Scholar 

Download references

Acknowledgements

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.

Author information

Authors and Affiliations

  1. Springer, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand

    Emma D. Deeks

Authors
  1. Emma D. Deeks
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Emma D. Deeks.

Ethics declarations

Funding

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.

Additional information

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.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

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

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s40265-017-0827-9

Search

Navigation