Chemical compound
Pharmaceutical compound
Bictegravir Clinical data Other names GS-9883 ATC code Identifiers (1S ,11R ,13R )-5-Hydroxy-3,6-dioxo-N -(2,4,6-trifluorobenzyl)-12-oxa-2,9-diazatetracyclo[11.2.1.0~2,11~.0~4,9~]hexadeca-4,7-diene-7-carboxamide
CAS Number PubChem CID DrugBank ChemSpider UNII KEGG ChEBI ChEMBL CompTox Dashboard (EPA) Chemical and physical data Formula C 21 H 18 F 3 N 3 O 5 Molar mass −1 3D model (JSmol ) InChI=1S/C21H18F3N3O5/c22-9-3-14(23)12(15(24)4-9)6-25-20(30)13-7-26-8-16-27(10-1-2-11(5-10)32-16)21(31)17(26)19(29)18(13)28/h3-4,7,10-11,16,29H,1-2,5-6,8H2,(H,25,30)/t10-,11+,16+/m0/s1
Key:SOLUWJRYJLAZCX-LYOVBCGYSA-N
Bictegravir (INN ; BIC, formerly known asGS-9883 )[ 1] [ 2] integrase inhibitor (INSTI) class that was structurally derived from an earlier compounddolutegravir by scientists atGilead Sciences .In vitro and clinical results were presented by Gilead in the summer of 2016.[ 3] [ 4] tenofovir alafenamide (TAF) andemtricitabine (FTC) for the treatment ofHIV-1 infection .[ 5]
Thecombination drug bictegravir/emtricitabine/tenofovir alafenamide (Biktarvy) was approved for use in 2018 in Australia,[ 6] [ 7] [ 8] [ 9] [ 10] Drugs Controller General of India in 2019.[ 11] [update] [ 12] [ 13] [ 14]
Bictegravir is used a in fixed dose combination withtenofovir alafenamide andemtricitabine for the treatment of HIV-1 infection.[ 4] [ 15]
Bictegravir should not be used withdofetilide andrifampin .[ 16] [ 16] [ 16] [ 4]
The most common side effects seen in bictegravir use include diarrhea, nausea, and headache.[ 4]
Society and culture [ edit ] In February 2022, Gilead agreed to payViiV Healthcare over $1 billion to settlepatent infringement cases.[ 17] [ 18]
^ "Recommended INN: List 75" (PDF) .WHO Drug Information .30 (1): 102. 2016.Archived (PDF) from the original on 4 November 2021. Retrieved4 October 2020 .^ "Bictegravir - Gilead Sciences" .Adis Insight . Springer Nature Switzerland AG.Archived from the original on 2 February 2017. Retrieved22 January 2017 .^ Highleyman L (6 July 2016)."New integrase inhibitor bictegravir looks promising in early studies" .NAM aidsmap .Archived from the original on 2 February 2017. Retrieved20 January 2017 . ^a b c d Zeuli J, Rizza S, Bhatia R, Temesgen Z (November 2019)."Bictegravir, a novel integrase inhibitor for the treatment of HIV infection" .Drugs of Today .55 (11):669– 682.doi :10.1358/dot.2019.55.11.3068796 .PMID 31840682 .S2CID 209385285 .Archived from the original on 28 August 2023. Retrieved28 August 2023 . ^ "Gilead Presents Preliminary Data on Bictegravir, an Investigational Integrase Strand Transfer Inhibitor for the Treatment of HIV" (Press release).Gilead Sciences . 20 June 2016.Archived from the original on 2 February 2017. Retrieved20 January 2017 .^ "Australian Public Assessment Report for Bictegravir / Emtricitabine / Tenofovir alafenamide" (PDF) .Therapeutic Goods Administration . 1 August 2019. Retrieved22 February 2024 .^ "Biktarvy" .European Medicines Agency . 21 June 2018. Retrieved22 February 2024 .^ "U.S. Food and Drug Administration Approves Gilead's Biktarvy (Bictegravir, Emtricitabine, Tenofovir Alafenamide) for Treatment of HIV-1 Infection" (Press release).Gilead Sciences . 7 February 2018.^ "BIKTARVY Data Sheet v 8.0" (PDF) .Medsafe . 24 August 2023. Retrieved22 February 2024 .^ "Bictegravir-emtricitabine-tenofovir alafenamide for the treatment of HIV-1 in adults" .NHS England . 17 July 2019. Retrieved22 February 2024 .^ "Hetero launches TAFFIC, the latest 3-in-1 single pill for HIV treatment" (Press release).Hetero Drugs . 17 December 2019. Retrieved22 February 2024 .^ "Initial Regimens: ART-naïve Adults" .European AIDS Clinical Society . October 2023. Retrieved22 February 2024 .^ "BHIVA guidelines on antiretroviral treatment for adults living with HIV-1 2022 (2023 interim update)" (PDF) .British HIV Association . 28 May 2023. p. 16. Retrieved22 February 2024 .^ "Guidelines for the Use of Antiretroviral Agents in Adults and Adolescents with HIV" (PDF) .HIV.gov . 21 September 2022. p. 6. Retrieved22 February 2024 .^ Wohl DA, Yazdanpanah Y, Baumgarten A, Clarke A, Thompson MA, Brinson C, et al. (June 2019)."Bictegravir combined with emtricitabine and tenofovir alafenamide versus dolutegravir, abacavir, and lamivudine for initial treatment of HIV-1 infection: week 96 results from a randomised, double-blind, multicentre, phase 3, non-inferiority trial" .The Lancet. HIV .6 (6):e355 – e363 .doi :10.1016/S2352-3018(19)30077-3 .PMID 31068270 .S2CID 148570850 .Archived from the original on 29 January 2022. Retrieved29 January 2022 . ^a b c "Biktarvy - FDA Prescribing Highlights" (PDF) .Archived (PDF) from the original on 26 July 2021. Retrieved29 January 2022 .^ "GSK announces settlement between ViiV Healthcare and Gilead Sciences, Inc. resolving litigation relating to Biktarvy and ViiV's dolutegravir patents and entry into a patent licence agreement" .ViiV Healthcare (Press release). ViiV Healthcare. Retrieved26 August 2023 .^ "GSK announces settlement between ViiV Healthcare and Gilead Sciences, Inc. resolving litigation relating to Biktarvy and ViiV's dolutegravir patents and entry into a patent licence agreement" .GSK US (Press release). 1 February 2022. Retrieved28 August 2023 .
