Resistance mutation info of drug

Drug General Information
Drug ID D0QD1G
Drug Name Elvitegravir Drug Info
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 [555872], [555877], [556153]
Level of Resistance Reduce EVG susceptibility >30 fold
Mutation info Missense: Q148H [555674]
Level of Resistance High-level resistance
Mutation info Missense: Q148K [555674]
Level of Resistance High-level resistance
Mutation info Missense: Q148R [555674]
Level of Resistance High-level resistance
Mutation info Missense: H51Y [555646], [555736], [555833]
Level of Resistance Reduce EVG susceptibility 2-3 fold
Mutation info Missense: E92Q [555872], [555877], [556153]
Level of Resistance Reduce EVG susceptibility >30 fold
Mutation info Missense: S153Y [555646], [555833]
Level of Resistance Reduce DTG susceptibility about 2 fold
Mutation info Missense: T66K [555833], [555877]
Level of Resistance Reduce EVG susceptibility 40-80 fold
Mutation info Missense: S147G [555823], [555877]
Level of Resistance Reduce EVG susceptibility 5-10 fold
Mutation info Missense: T66A [555823], [555877]
Level of Resistance Reduce EVG susceptibility 5 fold
Mutation info Missense: E138A/K/T + G140A/C/S [556228], [556237]
Level of Resistance Low-level resistance
Mutation info Missense: E138A [556228], [556237]
Level of Resistance Low-level resistance
Mutation info Missense: E138K [556228], [556237]
Level of Resistance Low-level resistance
Mutation info Missense: E138T [556228], [556237]
Level of Resistance Low-level resistance
Mutation info Missense: E92V [556228], [556237]
Level of Resistance High-level resistance
Mutation info Missense: G118R [556228], [556237]
Level of Resistance Intermediate resistance
Mutation info Missense: G140A [556228], [556237]
Level of Resistance Intermediate resistance
Mutation info Missense: G140C [556228], [556237]
Level of Resistance Intermediate resistance
Mutation info Missense: G140S [556228], [556237]
Level of Resistance Intermediate resistance
Mutation info Missense: G163K [556228], [556237]
Level of Resistance Low-level resistance
Mutation info Missense: G163R [556228], [556237]
Level of Resistance Low-level resistance
Mutation info Missense: H51Y + R263K [556228], [556237]
Level of Resistance Low-level resistance
Mutation info Missense: N155S [556228], [556237]
Level of Resistance Intermediate resistance
Mutation info Missense: N155T [556228], [556237]
Level of Resistance Intermediate resistance
Mutation info Missense: P145S [556228], [556237]
Level of Resistance High-level resistance
Mutation info Missense: Q148N [556228], [556237]
Level of Resistance Low-level resistance
Mutation info Missense: R263K [556228], [556237]
Level of Resistance Intermediate resistance
Mutation info Missense: S153F [556228], [556237]
Level of Resistance Low-level resistance
Mutation info Missense: S230R [556228], [556237]
Level of Resistance Low-level resistance
Mutation info Missense: T66I [556228], [556237]
Level of Resistance High-level resistance
Mutation info Missense: V151A [556228], [556237]
Level of Resistance Intermediate resistance
Mutation info Missense: V151L [556228], [556237]
Level of Resistance High-level resistance
Mutation info Missense: E157Q [555646]
Level of Resistance Reduce EVG susceptibility 2-3 fold
Mutation info Missense: F121Y [555646]
Level of Resistance Reduce EVG susceptibility about 30 fold
Mutation info Missense: Q146P [555646]
Level of Resistance Reduce EVG susceptibility about 10 fold
Mutation info Missense: E92G [555823]
Level of Resistance Reduce EVG susceptibility 10 fold
Mutation info Missense: T97A [555823]
Level of Resistance Reduce EVG susceptibility 5-10 fold
References
Ref 5326512013 FDA drug approvals. Nat Rev Drug Discov. 2014 Feb;13(2):85-9.
Ref 555646Broad 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. Epub 2007 Oct 31.
Ref 555674Subgroup and resistance analyses of raltegravir for resistant HIV-1 infection. N Engl J Med. 2008 Jul 24;359(4):355-65. doi: 10.1056/NEJMoa0708978.
Ref 555736Strand transfer inhibitors of HIV-1 integrase: bringing IN a new era of antiretroviral therapy. Antiviral Res. 2010 Jan;85(1):101-18. doi: 10.1016/j.antiviral.2009.11.004. Epub 2009 Nov 17.
Ref 555823Efficacy 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. doi: 10.1016/S1473-3099(11)70249-3. Epub 2011 Oct 18.
Ref 555833In vitro resistance selections using elvitegravir, raltegravir, and two metabolites of elvitegravir M1 and M4. Antiviral Res. 2012 Feb;93(2):288-96. doi: 10.1016/j.antiviral.2011.12.008. Epub 2011 Dec 16.
Ref 556228The HIVdb system for HIV-1 genotypic resistance interpretation. Intervirology. 2012;55(2):98-101. doi: 10.1159/000331998. Epub 2012 Jan 24.
Ref 555872Co-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. doi: 10.1016/S0140-6736(12)60918-0.
Ref 555877Development of elvitegravir resistance and linkage of integrase inhibitor mutations with protease and reverse transcriptase resistance mutations. PLoS One. 2012;7(7):e40514. doi: 10.1371/journal.pone.0040514. Epub 2012 Jul 18.
Ref 556237Evolutionary consequences of drug resistance: shared principles across diverse targets and organisms. Nat Rev Genet. 2015 Aug;16(8):459-71. doi: 10.1038/nrg3922. Epub 2015 Jul 7.
Ref 556153Infrequent development of drug resistance in HIV-1-infected treatment-naive subjects after 96 weeks of treatment with elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide or elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate. Antivir Ther. 2017 Jan 11. doi: 10.3851/IMP3125. [Epub ahead of print]

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