Drug General Information
Drug ID D0QD1G
Drug Name Elvitegravir
Synonyms EVG
Drug Type Small molecular drug
Structure D0QD1G
Drug Resistance Mutations
Target Name HIV Integrase Target Info
Uniprot ID POL_HV1B1(1160-1447)
Species Human immunodeficiency virus type 1 (HIV-1)
Reference Sequence FLDGIDKAQDEHEKYHSNWRAMASDFNLPPVVAKEIVASCDKCQLKGEAMHGQVDCSPGI
WQLDCTHLEGKVILVAVHVASGYIEAEVIPAETGQETAYFLLKLAGRWPVKTIHTDNGSN
FTSATVKAACWWAGIKQEFGIPYNPQSQGVVESMNKELKKIIGQVRDQAEHLKTAVQMAV
FIHNFKRKGGIGGYSAGERIVDIIATDIQTKELQKQITKIQNFRVYYRDSRNPLWKGPAK
LLWKGEGAVVIQDNSDIKVVPRRKAKIIRDYGKQMAGDDCVASRQDED [Human immu
nodeficiency virus type 1 (HIV-1)]
Targeted Disease HIV infection
Drug Resistance Mutations
Mutation info Missense: N155H [1], [2], [3]
Level of Resistance Reduce EVG susceptibility >30 fold
Mutation info Missense: Q148H [4]
Level of Resistance High-level resistance
Mutation info Missense: Q148K [4]
Level of Resistance High-level resistance
Mutation info Missense: Q148R [4]
Level of Resistance High-level resistance
Mutation info Missense: H51Y [5], [6], [7]
Level of Resistance Reduce EVG susceptibility 2-3 fold
Mutation info Missense: E92Q [1], [2], [3]
Level of Resistance Reduce EVG susceptibility >30 fold
Mutation info Missense: S153Y [5], [7]
Level of Resistance Reduce DTG susceptibility about 2 fold
Mutation info Missense: T66K [7], [1]
Level of Resistance Reduce EVG susceptibility 40-80 fold
Mutation info Missense: S147G [8], [1]
Level of Resistance Reduce EVG susceptibility 5-10 fold
Mutation info Missense: T66A [8], [1]
Level of Resistance Reduce EVG susceptibility 5 fold
Mutation info Missense: E138A/K/T + G140A/C/S [9], [10]
Level of Resistance Low-level resistance
Mutation info Missense: E138A [9], [10]
Level of Resistance Low-level resistance
Mutation info Missense: E138K [9], [10]
Level of Resistance Low-level resistance
Mutation info Missense: E138T [9], [10]
Level of Resistance Low-level resistance
Mutation info Missense: E92V [9], [10]
Level of Resistance High-level resistance
Mutation info Missense: G118R [9], [10]
Level of Resistance Intermediate resistance
Mutation info Missense: G140A [9], [10]
Level of Resistance Intermediate resistance
Mutation info Missense: G140C [9], [10]
Level of Resistance Intermediate resistance
Mutation info Missense: G140S [9], [10]
Level of Resistance Intermediate resistance
Mutation info Missense: G163K [9], [10]
Level of Resistance Low-level resistance
Mutation info Missense: G163R [9], [10]
Level of Resistance Low-level resistance
Mutation info Missense: H51Y + R263K [9], [10]
Level of Resistance Low-level resistance
Mutation info Missense: N155S [9], [10]
Level of Resistance Intermediate resistance
Mutation info Missense: N155T [9], [10]
Level of Resistance Intermediate resistance
Mutation info Missense: P145S [9], [10]
Level of Resistance High-level resistance
Mutation info Missense: Q148N [9], [10]
Level of Resistance Low-level resistance
Mutation info Missense: R263K [9], [10]
Level of Resistance Intermediate resistance
Mutation info Missense: S153F [9], [10]
Level of Resistance Low-level resistance
Mutation info Missense: S230R [9], [10]
Level of Resistance Low-level resistance
Mutation info Missense: T66I [9], [10]
Level of Resistance High-level resistance
Mutation info Missense: V151A [9], [10]
Level of Resistance Intermediate resistance
Mutation info Missense: V151L [9], [10]
Level of Resistance High-level resistance
Mutation info Missense: E157Q [5]
Level of Resistance Reduce EVG susceptibility 2-3 fold
Mutation info Missense: F121Y [5]
Level of Resistance Reduce EVG susceptibility about 30 fold
Mutation info Missense: Q146P [5]
Level of Resistance Reduce EVG susceptibility about 10 fold
Mutation info Missense: E92G [8]
Level of Resistance Reduce EVG susceptibility 10 fold
Mutation info Missense: T97A [8]
Level of Resistance Reduce EVG susceptibility 5-10 fold
References
REF 1 Development of elvitegravir resistance and linkage of integrase inhibitor mutations with protease and reverse transcriptase resistance mutations. PLoS One. 2012;7(7):e40514.
REF 2 Co-formulated elvitegravir, cobicistat, emtricitabine, and tenofovir disoproxil fumarate versus ritonavir-boosted atazanavir plus co-formulated emtricitabine and tenofovir disoproxil fumarate for initial treatment of HIV-1 infection: a randomised, double-blind, phase 3, non-inferiority trial. Lancet. 2012 Jun 30;379(9835):2429-38.
REF 3 Infrequent development of drug resistance in HIV-1-infected treatment-naive subjects after 96 weeks of treatment with elvitegravir/cobicistat/emtri... Antivir Ther. 2017;22(5):443-446.
REF 4 Subgroup and resistance analyses of raltegravir for resistant HIV-1 infection. N Engl J Med. 2008 Jul 24;359(4):355-65.
REF 5 Broad antiretroviral activity and resistance profile of the novel human immunodeficiency virus integrase inhibitor elvitegravir (JTK-303/GS-9137). J Virol. 2008 Jan;82(2):764-74.
REF 6 Strand transfer inhibitors of HIV-1 integrase: bringing IN a new era of antiretroviral therapy. Antiviral Res. 2010 Jan;85(1):101-18.
REF 7 In vitro resistance selections using elvitegravir, raltegravir, and two metabolites of elvitegravir M1 and M4. Antiviral Res. 2012 Feb;93(2):288-96.
REF 8 Efficacy and safety of once daily elvitegravir versus twice daily raltegravir in treatment-experienced patients with HIV-1 receiving a ritonavir-boosted protease inhibitor: randomised, double-blind, phase 3, non-inferiority study. Lancet Infect Dis. 2012 Jan;12(1):27-35.
REF 9 The HIVdb system for HIV-1 genotypic resistance interpretation. Intervirology. 2012;55(2):98-101.
REF 10 Evolutionary consequences of drug resistance: shared principles across diverse targets and organisms. Nat Rev Genet. 2015 Aug;16(8):459-71.

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