Bictegravir Explained

Atc Prefix:None
Index2 Label:as salt
Cas Number:1611493-60-7
Cas Number2:1807988-02-8
Pubchem:90311989
Drugbank:DB11799
Drugbank2:DBSALT002077
Chemspiderid:44208822
Chemspiderid2:48772870
Unii:8GB79LOJ07
Unii2:4L5MP1Y7W7
Kegg:D10909
Kegg2:D10910
Chebi:172943
Chembl:3989866
Chembl2:3989867
Synonyms:GS-9883
Iupac Name:(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
C:21
H:18
F:3
N:3
O:5
Smiles:c1c(cc(c(c1F)CNC(=O)c2cn3c(c(c2=O)O)C(=O)N4[C@H]5CC[C@H](C5)O[C@@H]4C3)F)F
Stdinchi: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
Stdinchikey:SOLUWJRYJLAZCX-LYOVBCGYSA-N

Bictegravir (INN; BIC, formerly known as GS-9883)[1] [2] is a second-generation integrase inhibitor (INSTI) class that was structurally derived from an earlier compound dolutegravir by scientists at Gilead Sciences. In vitro and clinical results were presented by Gilead in the summer of 2016.[3] [4] In 2016, bictegravir was in a Phase 3 trial as part of a single tablet regimen in combination with tenofovir alafenamide (TAF) and emtricitabine (FTC) for the treatment of HIV-1 infection.[5]

The combination drug bictegravir/emtricitabine/tenofovir alafenamide (Biktarvy) was approved for use in 2018 in Australia,[6] the European Union[7] and the United States[8] and in 2019 in New Zealand[9] and the United Kingdom;[10] a generic version was approved by the Drugs Controller General of India in 2019.[11] it is recommended as a first-line choice of antiretroviral therapy in several countries, including the European Union,[12] the United Kingdom[13] and the United States.[14]

Medical use

Bictegravir is used a in fixed dose combination with tenofovir alafenamide and emtricitabine for the treatment of HIV-1 infection.[15]

Contraindication

Bictegravir should not be used with dofetilide and rifampin.[16] Use of dofetilide with bictegravir increases the concentration of dofetilide, which can lead to life-threatening events. Concomitant use of bictegravir and rifampin causes significant interactions because of an effect rifampin has on bictegravir. Bictagravir is metabolized primarily through the liver (CYP3A4), so inducers of CYP3A4 should be avoided.

Adverse effects

The most common side effects seen in bictegravir use include diarrhea, nausea, and headache.

Society and culture

Economics

In February 2022, Gilead agreed to pay ViiV Healthcare over $1 billion to settle patent infringement cases.[17] [18]

Further reading

Notes and References

  1. Recommended INN: List 75 . WHO Drug Information . 2016 . 30 . 1 . 102 . 4 October 2020 . 4 November 2021 . https://web.archive.org/web/20211104134711/https://www.who.int/medicines/publications/druginformation/innlists/RL75.pdf?ua=1 . live .
  2. Web site: Bictegravir - Gilead Sciences . Adis Insight . Springer Nature Switzerland AG . 22 January 2017 . en . 2 February 2017 . https://web.archive.org/web/20170202010400/http://adisinsight.springer.com/drugs/800041516. live.
  3. News: Highleyman L . New integrase inhibitor bictegravir looks promising in early studies . NAM aidsmap . 6 July 2016. 20 January 2017 . 2 February 2017 . https://web.archive.org/web/20170202000610/http://www.aidsmap.com/New-integrase-inhibitor-bictegravir-looks-promising-in-early-studies/page/3069166/ . live .
  4. Zeuli J, Rizza S, Bhatia R, Temesgen Z . Bictegravir, a novel integrase inhibitor for the treatment of HIV infection . Drugs of Today . 55 . 11 . 669–682 . November 2019 . 31840682 . 10.1358/dot.2019.55.11.3068796 . 28 August 2023 . live . 209385285 . https://web.archive.org/web/20230828041350/https://access.portico.org/Portico/auView?auId=ark%3A%2F27927%2Fpjbf7dd1dzx . 28 August 2023 .
  5. Gilead Presents Preliminary Data on Bictegravir, an Investigational Integrase Strand Transfer Inhibitor for the Treatment of HIV . . 20 June 2016 . 20 January 2017 . 2 February 2017 . https://web.archive.org/web/20170202001535/http://www.gilead.com/news/press-releases/2016/6/gilead-presents-preliminary-data-on-bictegravir-an-investigational-integrase-strand-transfer-inhibitor-for-the-treatment-of-hiv/ . live .
  6. Web site: Australian Public Assessment Report for Bictegravir / Emtricitabine / Tenofovir alafenamide . . 1 August 2019 . 22 February 2024 .
  7. Web site: Biktarvy . . 21 June 2018 . 22 February 2024 .
  8. U.S. Food and Drug Administration Approves Gilead's Biktarvy (Bictegravir, Emtricitabine, Tenofovir Alafenamide) for Treatment of HIV-1 Infection . . 7 February 2018 .
  9. Web site: BIKTARVY Data Sheet v 8.0 . . 24 August 2023 . 22 February 2024 .
  10. Web site: Bictegravir-emtricitabine-tenofovir alafenamide for the treatment of HIV-1 in adults . . 17 July 2019 . 22 February 2024 .
  11. Hetero launches TAFFIC, the latest 3-in-1 single pill for HIV treatment . . 17 December 2019 . 22 February 2024 .
  12. Web site: Initial Regimens: ART-naïve Adults . . October 2023 . 22 February 2024 .
  13. Web site: BHIVA guidelines on antiretroviral treatment for adults living with HIV-1 2022 (2023 interim update) . . 16 . 28 May 2023 . 22 February 2024 .
  14. Web site: Guidelines for the Use of Antiretroviral Agents in Adults and Adolescents with HIV . . 6 . 21 September 2022 . 22 February 2024 .
  15. Wohl DA, Yazdanpanah Y, Baumgarten A, Clarke A, Thompson MA, Brinson C, Hagins D, Ramgopal MN, Antinori A, Wei X, Acosta R, Collins SE, Brainard D, Martin H . 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 . June 2019 . 31068270 . 10.1016/S2352-3018(19)30077-3 . 29 January 2022 . live . 148570850 . https://web.archive.org/web/20220129040955/https://pubmed.ncbi.nlm.nih.gov/31068270/ . 29 January 2022 .
  16. Web site: Biktarvy - FDA Prescribing Highlights. 29 January 2022. 26 July 2021. https://web.archive.org/web/20210726012217/https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf. live.
  17. 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 . ViiV Healthcare . 26 August 2023.
  18. 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 . 1 February 2022 . 28 August 2023.

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Bictegravir".

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