Bictegravir

Bictegravir
Clinical data
Other names	GS-9883
ATC code	None;
Identifiers
	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;
CAS Number	1611493-60-7; as salt: 1807988-02-8;
PubChem CID	90311989;
DrugBank	DB11799; as salt: DBSALT002077;
ChemSpider	44208822; as salt: 48772870;
UNII	8GB79LOJ07; as salt: 4L5MP1Y7W7;
KEGG	D10909; as salt: D10910;
ChEBI	CHEBI:172943;
ChEMBL	ChEMBL3989866; as salt: ChEMBL3989867;
Chemical and physical data
Formula	C21H18F3N3O5
Molar mass	449.386 g·mol−1
3D model (JSmol)	Interactive image;
	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;
	InChI 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 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. In vitro and clinical results were presented by Gilead in the summer of 2016. 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.

The combination drug bictegravir/emtricitabine/tenofovir alafenamide (Biktarvy) was approved for use in 2018 in Australia, the European Union and the United States and in 2019 in New Zealand and the United Kingdom; a generic version was approved by the Drugs Controller General of India in 2019. As of 2024, it is recommended as a first-line choice of antiretroviral therapy in several countries, including the European Union, the United Kingdom and the United States.

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