Bictegravir: First Global Approval
- 220 Downloads
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.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. https://doi.org/10.1128/aac.01695-17.
- 2.European AIDS Clinical Society. Guidelines version 9.0. 2017. http://www.eacsociety.org. Accessed 13 Mar 2018.
- 3.Department of Health and Human Services USA. Guidelines for the use of antiretroviral agents in adults and adolescents living with HIV. 2017. https://aidsinfo.nih.gov/guidelines. Accessed 13 Mar 2018.
- 5.Gilead Sciences Inc. Biktarvy® (bictegravir, emtricitabine, and tenofovir alafenamide) tablets, for oral use: US prescribing information. 2018. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf. Accessed 26 Feb 2018.
- 6.Gilead Sciences. Gilead announces new license agreement with the medicines patent pool for access to bictegravir [media release]. 4 Oct 2017. http://www.gilead.com.
- 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.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.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.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.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.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.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