Bictegravir
From Proteopedia
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<StructureSection load='' size='340' side='right' caption='Caption for this structure' scene='98/989308/Cv/1'> | <StructureSection load='' size='340' side='right' caption='Caption for this structure' scene='98/989308/Cv/1'> | ||
Bictegravir (INN; BIC, formerly known as GS-9883) is a second-generation integrase inhibitor (INSTI) class that was structurally derived from an earlier compound dolutegravir by scientists at Gilead Sciences. See also [https://en.wikipedia.org/wiki/Bictegravir Bictegravir]. | Bictegravir (INN; BIC, formerly known as GS-9883) is a second-generation integrase inhibitor (INSTI) class that was structurally derived from an earlier compound dolutegravir by scientists at Gilead Sciences. See also [https://en.wikipedia.org/wiki/Bictegravir Bictegravir]. | ||
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| + | 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<ref name="a5">[https://www.gilead.com/news-and-press/press-room/press-releases/2016/6/gilead-presents-preliminary-data-on-bictegravir-an-investigational-integrase-strand-transfer-inhibitor-for-the-treatment-of-hiv "Press Release: Gilead Presents Preliminary Data on Bictegravir, an Investigational Integrase Strand Transfer Inhibitor for the Treatment of HIV | Gilead".] Gilead. 20 June 2016. Archived from the original on 2 February 2017. Retrieved 20 January 2017.</ref> and the combination drug bictegravir/[[emtricitabine]]/tenofovir alafenamide (Biktarvy) was approved for use in the United States in 2018.<ref name="a6">[https://www.businesswire.com/news/home/20180207006071/en/U.S.-Food-Drug-Administration-Approves-Gilead%E2%80%99s-Biktarvy%C2%AE "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.</ref> | ||
<scene name='98/989308/Overall/2'>Structure of the STLV intasome:B56 complex bound to the strand-transfer inhibitor bictegravir</scene> ([[7ouh]]). | <scene name='98/989308/Overall/2'>Structure of the STLV intasome:B56 complex bound to the strand-transfer inhibitor bictegravir</scene> ([[7ouh]]). | ||
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| + | <scene name='98/989308/Overall/4'>Bictegravir inhibits integrase</scene>. | ||
</StructureSection> | </StructureSection> | ||
== References == | == References == | ||
<references/> | <references/> | ||
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References
- ↑ "Press Release: Gilead Presents Preliminary Data on Bictegravir, an Investigational Integrase Strand Transfer Inhibitor for the Treatment of HIV | Gilead". Gilead. 20 June 2016. Archived from the original on 2 February 2017. Retrieved 20 January 2017.
- ↑ "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.
