Resistance mutation info of target

Target General Information
Target ID T39087
Target Name HIV Integrase Target Info
Species Human immunodeficiency virus type 1 (HIV-1)
Uniprot ID POL_HV1B1(1160-1447)
Sequence FLDGIDKAQDEHEKYHSNWRAMASDFNLPPVVAKEIVASCDKCQLKGEAMHGQVDCSPGI
WQLDCTHLEGKVILVAVHVASGYIEAEVIPAETGQETAYFLLKLAGRWPVKTIHTDNGSN
FTSATVKAACWWAGIKQEFGIPYNPQSQGVVESMNKELKKIIGQVRDQAEHLKTAVQMAV
FIHNFKRKGGIGGYSAGERIVDIIATDIQTKELQKQITKIQNFRVYYRDSRNPLWKGPAK
LLWKGEGAVVIQDNSDIKVVPRRKAKIIRDYGKQMAGDDCVASRQDED [Human immu
nodeficiency virus type 1 (HIV-1)]
Drug Resistance Mutation and Corresponding Drugs
Ref 5292822007 FDA drug approvals: a year of flux. Nat Rev Drug Discov. 2008 Feb;7(2):107-9.
Ref 5326512013 FDA drug approvals. Nat Rev Drug Discov. 2014 Feb;13(2):85-9.
Ref 542387(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7365).
Ref 5326512013 FDA drug approvals. Nat Rev Drug Discov. 2014 Feb;13(2):85-9.
Mutation Info Missense: E138A
Drugs
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Drug Name Elvitegravir Drug Info [556228], [556237]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Drug Name Dolutegravir Drug Info [556227], [556228]
Targeted Disease HIV infection
Mutation Info Missense: E138A/K/T + G140A/C/S
Drugs
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Drug Name Elvitegravir Drug Info [556228], [556237]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Mutation Info Missense: E138K
Drugs
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Drug Name Elvitegravir Drug Info [556228], [556237]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Drug Name Dolutegravir Drug Info [556227], [556228]
Targeted Disease HIV infection
Mutation Info Missense: E138T
Drugs
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Drug Name Elvitegravir Drug Info [556228], [556237]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Drug Name Dolutegravir Drug Info [556227], [556228]
Targeted Disease HIV infection
Mutation Info Missense: E157Q
Drugs
Drug Name Elvitegravir Drug Info [555646]
Targeted Disease HIV infection
Level of Resistance Reduce EVG susceptibility 2-3 fold
Drug Name Raltegravir Drug Info [555652]
Targeted Disease HIV infection
Level of Resistance Reduce RAL susceptibility 2-3 fold
Mutation Info Missense: E92G
Drugs
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Drug Name Elvitegravir Drug Info [555823]
Targeted Disease HIV infection
Level of Resistance Reduce EVG susceptibility 10 fold
Mutation Info Missense: E92Q
Drugs
Drug Name Raltegravir Drug Info [555802], [555823], [556153]
Targeted Disease HIV infection
Level of Resistance Reduce RAL susceptibility >5 fold
Drug Name Elvitegravir Drug Info [555872], [555877], [556153]
Targeted Disease HIV infection
Level of Resistance Reduce EVG susceptibility >30 fold
Drug Name Dolutegravir Drug Info [556227], [556228]
Targeted Disease HIV infection
Mutation Info Missense: E92V
Drugs
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance Intermediate resistance
Drug Name Elvitegravir Drug Info [556228], [556237]
Targeted Disease HIV infection
Level of Resistance High-level resistance
Mutation Info Missense: F121Y
Drugs
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance Reduce RAL susceptibility 10 fold
Drug Name Elvitegravir Drug Info [555646]
Targeted Disease HIV infection
Level of Resistance Reduce EVG susceptibility about 30 fold
Mutation Info Missense: G118R
Drugs
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance Intermediate resistance
Drug Name Elvitegravir Drug Info [556228], [556237]
Targeted Disease HIV infection
Level of Resistance Intermediate resistance
Drug Name Dolutegravir Drug Info [556227], [556228]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Mutation Info Missense: G140A
Drugs
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance Intermediate resistance
Drug Name Elvitegravir Drug Info [556228], [556237]
Targeted Disease HIV infection
Level of Resistance Intermediate resistance
Drug Name Dolutegravir Drug Info [556227], [556228]
Targeted Disease HIV infection
Mutation Info Missense: G140C
Drugs
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance Intermediate resistance
Drug Name Elvitegravir Drug Info [556228], [556237]
Targeted Disease HIV infection
Level of Resistance Intermediate resistance
Drug Name Dolutegravir Drug Info [556227], [556228]
Targeted Disease HIV infection
Mutation Info Missense: G140S
Drugs
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance Intermediate resistance
Drug Name Elvitegravir Drug Info [556228], [556237]
Targeted Disease HIV infection
Level of Resistance Intermediate resistance
Drug Name Dolutegravir Drug Info [556227], [556228]
Targeted Disease HIV infection
Mutation Info Missense: G163K
Drugs
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Drug Name Elvitegravir Drug Info [556228], [556237]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Mutation Info Missense: G163R
Drugs
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Drug Name Elvitegravir Drug Info [556228], [556237]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Mutation Info Missense: H51Y
Drugs
Drug Name Elvitegravir Drug Info [555646], [555736], [555833]
Targeted Disease HIV infection
Level of Resistance Reduce EVG susceptibility 2-3 fold
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Mutation Info Missense: H51Y + R263K
Drugs
Drug Name Elvitegravir Drug Info [556228], [556237]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Mutation Info Missense: N155H
Drugs
Drug Name Raltegravir Drug Info [555674]
Targeted Disease HIV infection
Level of Resistance Reduce RAL susceptibility >10 fold
Drug Name Elvitegravir Drug Info [555872], [555877], [556153]
Targeted Disease HIV infection
Level of Resistance Reduce EVG susceptibility >30 fold
Drug Name Dolutegravir Drug Info [556227], [556228]
Targeted Disease HIV infection
Mutation Info Missense: N155S
Drugs
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance Intermediate resistance
Drug Name Elvitegravir Drug Info [556228], [556237]
Targeted Disease HIV infection
Level of Resistance Intermediate resistance
Mutation Info Missense: N155T
Drugs
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance Intermediate resistance
Drug Name Elvitegravir Drug Info [556228], [556237]
Targeted Disease HIV infection
Level of Resistance Intermediate resistance
Mutation Info Missense: P145S
Drugs
Drug Name Elvitegravir Drug Info [556228], [556237]
Targeted Disease HIV infection
Level of Resistance High-level resistance
Mutation Info Missense: Q146P
Drugs
Drug Name Elvitegravir Drug Info [555646]
Targeted Disease HIV infection
Level of Resistance Reduce EVG susceptibility about 10 fold
Mutation Info Missense: Q148H
Drugs
Drug Name Raltegravir Drug Info [555674]
Targeted Disease HIV infection
Level of Resistance High-level resistance
Drug Name Elvitegravir Drug Info [555674]
Targeted Disease HIV infection
Level of Resistance High-level resistance
Drug Name Dolutegravir Drug Info [556227], [556228]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Mutation Info Missense: Q148K
Drugs
Drug Name Raltegravir Drug Info [555674]
Targeted Disease HIV infection
Level of Resistance High-level resistance
Drug Name Elvitegravir Drug Info [555674]
Targeted Disease HIV infection
Level of Resistance High-level resistance
Drug Name Dolutegravir Drug Info [556227], [556228]
Targeted Disease HIV infection
Level of Resistance Intermediate resistance
Mutation Info Missense: Q148N
Drugs
Drug Name Elvitegravir Drug Info [556228], [556237]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Mutation Info Missense: Q148R
Drugs
Drug Name Raltegravir Drug Info [555674]
Targeted Disease HIV infection
Level of Resistance High-level resistance
Drug Name Elvitegravir Drug Info [555674]
Targeted Disease HIV infection
Level of Resistance High-level resistance
Drug Name Dolutegravir Drug Info [556227], [556228]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Mutation Info Missense: R263K
Drugs
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Drug Name Elvitegravir Drug Info [556228], [556237]
Targeted Disease HIV infection
Level of Resistance Intermediate resistance
Drug Name Dolutegravir Drug Info [555922], [556030]
Targeted Disease HIV infection
Level of Resistance Reduce DTG susceptibility 6 fold
Mutation Info Missense: S147G
Drugs
Drug Name Elvitegravir Drug Info [555823], [555877]
Targeted Disease HIV infection
Level of Resistance Reduce EVG susceptibility 5-10 fold
Mutation Info Missense: S153F
Drugs
Drug Name Elvitegravir Drug Info [556228], [556237]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Drug Name Dolutegravir Drug Info [556227], [556228]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Mutation Info Missense: S153Y
Drugs
Drug Name Elvitegravir Drug Info [555646], [555833]
Targeted Disease HIV infection
Level of Resistance Reduce DTG susceptibility about 2 fold
Drug Name Dolutegravir Drug Info [555782]
Targeted Disease HIV infection
Level of Resistance Reduce DTG susceptibility about 2 fold
Mutation Info Missense: S230R
Drugs
Drug Name Elvitegravir Drug Info [556228], [556237]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Drug Name Raltegravir Drug Info [555802]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Mutation Info Missense: T66A
Drugs
Drug Name Raltegravir Drug Info [555675], [555752]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Drug Name Elvitegravir Drug Info [555823], [555877]
Targeted Disease HIV infection
Level of Resistance Reduce EVG susceptibility 5 fold
Mutation Info Missense: T66I
Drugs
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Drug Name Elvitegravir Drug Info [556228], [556237]
Targeted Disease HIV infection
Level of Resistance High-level resistance
Mutation Info Missense: T66K
Drugs
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance High-level resistance
Drug Name Elvitegravir Drug Info [555833], [555877]
Targeted Disease HIV infection
Level of Resistance Reduce EVG susceptibility 40-80 fold
Drug Name Dolutegravir Drug Info [556227], [556228]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Mutation Info Missense: T97A
Drugs
Drug Name Raltegravir Drug Info [555652], [555746], [555823]
Targeted Disease HIV infection
Level of Resistance Reduce susceptibility to RAL
Drug Name Elvitegravir Drug Info [555823]
Targeted Disease HIV infection
Level of Resistance Reduce EVG susceptibility 5-10 fold
Mutation Info Missense: V151A
Drugs
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Drug Name Elvitegravir Drug Info [556228], [556237]
Targeted Disease HIV infection
Level of Resistance Intermediate resistance
Mutation Info Missense: V151L
Drugs
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance Intermediate resistance
Drug Name Elvitegravir Drug Info [556228], [556237]
Targeted Disease HIV infection
Level of Resistance High-level resistance
Drug Name Dolutegravir Drug Info [556227], [556228]
Targeted Disease HIV infection
Level of Resistance Low-level resistance
Mutation Info Missense: Y143A
Drugs
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance High-level resistance
Mutation Info Missense: Y143C
Drugs
Drug Name Raltegravir Drug Info [555746], [555802], [555852]
Targeted Disease HIV infection
Level of Resistance Reduce RAL susceptibility 5 fold
Mutation Info Missense: Y143G
Drugs
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance High-level resistance
Mutation Info Missense: Y143H
Drugs
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance High-level resistance
Mutation Info Missense: Y143K
Drugs
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance High-level resistance
Mutation Info Missense: Y143R
Drugs
Drug Name Raltegravir Drug Info [555746], [555802], [555852]
Targeted Disease HIV infection
Level of Resistance Reduce RAL susceptibility 20 fold
Mutation Info Missense: Y143S
Drugs
Drug Name Raltegravir Drug Info [556228], [556239]
Targeted Disease HIV infection
Level of Resistance High-level resistance
Reference
Ref 556227HIV drug development: the next 25 years. Nat Rev Drug Discov. 2007 Dec;6(12):959-66.
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 555652Mutations associated with failure of raltegravir treatment affect integrase sensitivity to the inhibitor in vitro. Antimicrob Agents Chemother. 2008 Apr;52(4):1351-8. doi: 10.1128/AAC.01228-07. Epub 2008 Jan 28.
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 555675Drug resistance profiles for the HIV integrase gene in patients failing raltegravir salvage therapy. HIV Med. 2008 Oct;9(9):765-70. doi: 10.1111/j.1468-1293.2008.00628.x. Epub 2008 Jul 21.
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 555746Genotypic/phenotypic patterns of HIV-1 integrase resistance to raltegravir. J Antimicrob Chemother. 2010 Mar;65(3):425-33. doi: 10.1093/jac/dkp477. Epub 2010 Jan 7.
Ref 555752Long-term efficacy and safety of the HIV integrase inhibitor raltegravir in patients with limited treatment options in a Phase II study. J Acquir Immune Defic Syndr. 2010 Apr 1;53(4):456-63.
Ref 555782In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. Antimicrob Agents Chemother. 2011 Feb;55(2):813-21. doi: 10.1128/AAC.01209-10. Epub 2010 Nov 29.
Ref 555802HIV-1 integrase inhibitor resistance and its clinical implications. J Infect Dis. 2011 May 1;203(9):1204-14. doi: 10.1093/infdis/jir025.
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 555852Broad phenotypic cross-resistance to elvitegravir in HIV-infected patients failing on raltegravir-containing regimens. Antimicrob Agents Chemother. 2012 Jun;56(6):2873-8. doi: 10.1128/AAC.06170-11. Epub 2012 Mar 26.
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 555922Viral fitness cost prevents HIV-1 from evading dolutegravir drug pressure. Retrovirology. 2013 Feb 22;10:22. doi: 10.1186/1742-4690-10-22.
Ref 556030Evolution of a novel pathway leading to dolutegravir resistance in a patient harbouring N155H and multiclass drug resistance. J Antimicrob Chemother. 2015 Feb;70(2):405-11. doi: 10.1093/jac/dku387. Epub 2014 Oct 3.
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 556239Resistance to direct-acting antiviral agents: clinical utility and significance. Curr Opin HIV AIDS. 2015 Sep;10(5):381-9. doi: 10.1097/COH.0000000000000177.
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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