, Volume 78, Issue 5, pp 601–606 | Cite as

Bictegravir: First Global Approval

  • Anthony Markham
AdisInsight Report


Gilead Sciences has developed a single tablet anti-HIV-1 medication (Biktarvy®) combining the novel integrase strand transfer inhibitor (INSTI) bictegravir with the nucleos(t)ide reverse transcriptase inhibitors (NRTIs) emtricitabine and tenofovir alafenamide. This fixed dose combination has demonstrated efficacy as treatment for both anti-retroviral naïve and virologically suppressed HIV-1 infection in patients switching therapy, and was recently approved in the USA. This article summarizes the milestones in the development of bictegravir leading to this first approval of bictegravir/emtricitabine/tenofovir alafenamide as treatment for HIV-1 infection.


Compliance with Ethical Standards


The preparation of this review was not supported by any external funding.

Conflict of interest

During the peer review process the manufacturer of the agent under review was offered an opportunity to comment on the article. Changes resulting from any comments received were made by the author on the basis of scientific completeness and accuracy. A. Markham, a contracted employee of Adis/Springer, is responsible for the article content and declares no relevant conflicts of interest.


  1. 1.
    Hassounah SA, Alikhani A, Oliveira M, et al. Antiviral activity of bictegravir and cabotegravir against integrase inhibitor-resistant SIVmac239 and HIV-1. Antimicrob Agents Chemother. 2017.
  2. 2.
    European AIDS Clinical Society. Guidelines version 9.0. 2017. Accessed 13 Mar 2018.
  3. 3.
    Department of Health and Human Services USA. Guidelines for the use of antiretroviral agents in adults and adolescents living with HIV. 2017. Accessed 13 Mar 2018.
  4. 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.CrossRefPubMedPubMedCentralGoogle Scholar
  5. 5.
    Gilead Sciences Inc. Biktarvy® (bictegravir, emtricitabine, and tenofovir alafenamide) tablets, for oral use: US prescribing information. 2018. Accessed 26 Feb 2018.
  6. 6.
    Gilead Sciences. Gilead announces new license agreement with the medicines patent pool for access to bictegravir [media release]. 4 Oct 2017.
  7. 7.
    Tsiang M, Jones GS, Goldsmith J, et al. Antiviral activity of bictegravir (GS-9883), a novel potent HIV-1 integrase strand transfer inhibitor with an improved resistance profile. Antimicrob Agents Chemother. 2016;60(12):7086–97.PubMedPubMedCentralGoogle Scholar
  8. 8.
    Gallant JE, Thompson M, DeJesus E, et al. Antiviral activity, safety, and pharmacokinetics of bictegravir as 10-day monotherapy in HIV-1-infected adults. J Acquir Immune Defic Syndr. 2017;75(1):61–6.CrossRefPubMedPubMedCentralGoogle Scholar
  9. 9.
    Zhang H, Custodio J, Wei X, et al. Clinical pharmacology of the HIV integrase strand transfer inhibitor bictegravir [abstract no. 02]. HIV Med. 2017;18(Suppl. 1):3.Google Scholar
  10. 10.
    Gallant J, Lazzarin A, Mills A, et al. Bictegravir, emtricitabine, and tenofovir alafenamide versus dolutegravir, abacavir, and lamivudine for initial treatment of HIV-1 infection (GS-US-380-1489): a double-blind, multicentre, phase 3, randomised controlled non-inferiority trial. Lancet. 2017;390(10107):2063–72.CrossRefPubMedGoogle Scholar
  11. 11.
    Sax PE, Pozniak A, Montes ML, et al. Coformulated bictegravir, emtricitabine, and tenofovir alafenamide versus dolutegravir with emtricitabine and tenofovir alafenamide, for initial treatment of HIV-1 infection (GS-US-380-1490): a randomised, double-blind, multicentre, phase 3, non-inferiority trial. Lancet. 2017;390(10107):2073–82.CrossRefPubMedGoogle Scholar
  12. 12.
    Molina J-M, Ward D, Brar I, et al. Switch to bictegravir/F/TAF from DTG and ABC/3TC [abstract no. 22 plus poster]. In: 25th Conference on Retroviruses and Opportunistic Infections. 2018.Google Scholar
  13. 13.
    Daar E, DeJesus E, Ruane P, et al. Phase 3 randomized, controlled trial of switching to fixed-dose bictegravir/emtricitabine/tenofovir alafenamide (B/F/TAF) from boosted protease inhibitor-based regimens in virologically suppressed adults: week 48 results [abstract no. LB-4]. Open Forum Infect Dis Fall. 2017;4(Suppl. 1):S735.CrossRefGoogle Scholar
  14. 14.
    Kityo C, Hagins D, Koenig E, et al. Switching to bictegravir/emtracitabine/tenofovir alafenimide (B/F/TAF) in women [abstract no. 500 plus poster]. In: 25th Conference on Retroviruses and Opportunistic Infections. 2018.Google Scholar
  15. 15.
    Gaur A, Rodriguez C, EJ. M, et al. Bictegravir/FTC/TAF single-tablet-regimen in adolescents: week 24 results [abstract no. 844]. In: 25th Conference on Retrovirals and opportunistic Infections. 2018.Google Scholar

Copyright information

© Springer International Publishing AG, part of Springer Nature 2018

Authors and Affiliations

  1. 1.SpringerAucklandNew Zealand

Personalised recommendations