Chemistry:Bictegravir
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| Other names | GS-9883 |
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| Formula | C21H18F3N3O5 |
| Molar mass | 449.386 g·mol−1 |
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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] and the combination drug bictegravir/emtricitabine/tenofovir alafenamide (Biktarvy) was approved for use in the United States in 2018.[6]
Medical use
Bictegravir is used a in fixed dose combination with tenofovir alafenamide and emtricitabine for the treatment of HIV-1 infection.[4][7]
Contraindication
Bictegravir should not be used with dofetilide and rifampin.[8] Use of dofetilide with bictegravir increases the concentration of dofetilide, which can lead to life-threatening events.[8] Concomitant use of bictegravir and rifampin causes significant interactions because of an effect rifampin has on bictegravir.[8] Bictagravir is metabolized primarily through the liver (CYP3A4), so inducers of CYP3A4 should be avoided.[4]
Adverse effects
The most common side effects seen in bictegravir use include diarrhea, nausea, and headache.[4]
Society and culture
Economics
In February 2022, Gilead agreed to pay ViiV Healthcare over $1 billion to settle patent infringement cases.[9][10]
References
- ↑ "Recommended INN: List 75". WHO Drug Information 30 (1): 102. 2016. https://www.who.int/medicines/publications/druginformation/innlists/RL75.pdf?ua=1. Retrieved 4 October 2020.
- ↑ "Bictegravir - Gilead Sciences" (in en). Adis Insight. Springer Nature Switzerland AG. http://adisinsight.springer.com/drugs/800041516.
- ↑ "New integrase inhibitor bictegravir looks promising in early studies". NAM aidsmap. 6 July 2016. http://www.aidsmap.com/New-integrase-inhibitor-bictegravir-looks-promising-in-early-studies/page/3069166/.
- ↑ 4.0 4.1 4.2 4.3 "Bictegravir, a novel integrase inhibitor for the treatment of HIV infection". Drugs of Today 55 (11): 669–682. November 2019. doi:10.1358/dot.2019.55.11.3068796. PMID 31840682. https://doi.org/10.1358/dot.2019.55.11.3068796. Retrieved 28 August 2023.
- ↑ "Press Release: Gilead Presents Preliminary Data on Bictegravir, an Investigational Integrase Strand Transfer Inhibitor for the Treatment of HIV | Gilead". Gilead. 20 June 2016. 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/.
- ↑ "U.S. Food and Drug Administration Approves Gilead's Biktarvy (Bictegravir, Emtricitabine, Tenofovir Alafenamide) for Treatment of HIV-1 Infection" (Press release). Gilead. 7 February 2018.
- ↑ "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. doi:10.1016/S2352-3018(19)30077-3. PMID 31068270. https://pubmed.ncbi.nlm.nih.gov/31068270. Retrieved 29 January 2022.
- ↑ 8.0 8.1 8.2 "Biktarvy - FDA Prescribing Highlights". https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf.
- ↑ "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. Retrieved 26 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. Retrieved 28 August 2023.
Further reading
- "Antiviral Activity of Bictegravir (GS-9883), a Novel Potent HIV-1 Integrase Strand Transfer Inhibitor with an Improved Resistance Profile". Antimicrobial Agents and Chemotherapy 60 (12): 7086–7097. December 2016. doi:10.1128/AAC.01474-16. PMID 27645238.
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