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elvitegravir

Structure via PubChem · Public domain (PubChem)

EntityQ2740966· pop 19· linked from 133 articles

elvitegravir

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Also known as JTK-303, 6-(3-chloro-2-fluorobenzyl)-1-[(2S)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid, GS-9137, EVG, GS 9137

Elvitegravir (EVG) is an integrase inhibitor used to treat HIV infection. It was developed by the pharmaceutical company Gilead Sciences, which licensed EVG from Japan Tobacco in March 2008. The drug gained approval by the U.S. Food and Drug Administration on 27 August 2012, for use in adult patients starting HIV treatment for the first time as part of the fixed dose combination known as Stribild. On 24 September 2014, the FDA approved Elvitegravir as a single pill formulation under the trade name Vitekta. On 5 November 2015, the FDA approved the drug for use in patients affected with HIV-1 as

Key facts

Drug.Verifiedfields
changed
Drug.Watchedfields
changed
Drug.verifiedrevid
437144022
Drug.image
Elvitegravir structure.svg
Drug.image_class
skin-invert-image
Drug.caption
Above: molecular structure of elvitegravir Below: 3D representation of an elvitegravir molecule
Drug.image2
Elvitegravir 3D structure.png
Drug.image_class2
bg-transparent
Drug.tradename
Vitekta; Stribild (fixed-dose combination)
Drug.licence_EU
yes
Drug.routes_of_administration
By mouth
Drug.ATC_prefix
J05
Drug.ATC_suffix
AJ02
Drug.protein_bound
98%
Drug.metabolism
liver, via CYP3A
Drug.elimination_half life
12.9 (8.7–13.7) hours
Drug.excretion
liver 93%, renal 7%
Drug.CAS_number
697761-98-1

via Wikipedia infobox

Chemical data

Formula
C23H23ClFNO5
Molecular weight
447.9 g/mol
IUPAC name
6-[(3-chloro-2-fluorophenyl)methyl]-1-[(2S)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxoquinoline-3-carboxylic acid
SMILES
CC(C)[C@@H](CO)N1C=C(C(=O)C2=C1C=C(C(=C2)CC3=C(C(=CC=C3)Cl)F)OC)C(=O)O
InChIKey
JUZYLCPPVHEVSV-LJQANCHMSA-N
XLogP
5.3
Polar surface area
87.1 Ų
H-bond donors
2
H-bond acceptors
7
Formal charge
0

via PubChem

Drug data · ChEMBL

Max clinical phase
Approved
Molecule type
Small molecule
First approval
2012
Admin. routes
oral
Indications
HIV-1 infection, viral disease, HIV infection, AIDS

via ChEMBL · EBI

Wikidata facts

Mass
447.125
Has use
medication
Show 6 more facts
chemical formula
C₂₃H₂₃ClFNO₅
isomeric SMILES
CC(C)[C@@H](CO)N1C=C(C(=O)C2=CC(=C(C=C21)OC)CC3=C(C(=CC=C3)Cl)F)C(=O)O
canonical SMILES
CC(C)C(CO)N1C=C(C(=O)C2=CC(=C(C=C21)OC)CC3=C(C(=CC=C3)Cl)F)C(=O)O
Commons category
Elvitegravir
World Health Organisation international non-proprietary name
elvitegravir
subject has role
antiviral drug
Sources (5)

via Wikidata · CC0

~3 min read

Encyclopedic overview

7 sections
Contents
  • Medical uses
  • Adverse effects
  • Interactions and contraindications
  • Pharmacology
  • Mechanism of action
  • Pharmacokinetics
  • References

Elvitegravir (EVG) is an integrase inhibitor used to treat HIV infection. It was developed by the pharmaceutical company Gilead Sciences, which licensed EVG from Japan Tobacco in March 2008. The drug gained approval by the U.S. Food and Drug Administration on 27 August 2012, for use in adult patients starting HIV treatment for the first time as part of the fixed dose combination known as Stribild. On 24 September 2014, the FDA approved Elvitegravir as a single pill formulation under the trade name Vitekta. On 5 November 2015, the FDA approved the drug for use in patients affected with HIV-1 as a part of a second fixed dose combination pill known as Genvoya.

According to the results of the phase II clinical trial, patients taking once-daily elvitegravir boosted by ritonavir had greater reductions in viral load after 24 weeks compared to individuals randomized to receive a ritonavir-boosted protease inhibitor.

Excerpted from Wikipedia’s “elvitegravir” article, available under the CC BY-SA 4.0 licence.