Drug General Information
Drug ID D00YZD
Drug Name Dolutegravir
Synonyms 1051375-16-6; GSK1349572; Tivicay; S/GSK1349572; Dolutegravir (GSK1349572); S-349572; GSK-1349572; GSK 1349572; UNII-DKO1W9H7M1; (4r,12as)-N-(2,4-Difluorobenzyl)-7-Hydroxy-4-Methyl-6,8-Dioxo-3,4,6,8,12,12a-Hexahydro-2h-Pyrido[1',2':4,5]pyrazino[2,1-B][1,3]oxazine-9-Carboxamide; CHEBI:76010; DKO1W9H7M1; Tivicay (TN); (4R,12aS)-N-[(2,4-Difluorophenyl)methyl]-3,4,6,8,12,12a-hexahydro-7-hydroxy-4-methyl-6,8-dioxo-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxamide; Dolutegravir Sodium (
Drug Type Small molecular drug
Company GlaxoSmithKline
Structure D00YZD
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: R263K [1], [2]
Level of Resistance Reduce DTG susceptibility 6 fold
Mutation info Missense: E138A [3], [4]
Mutation info Missense: E138K [3], [4]
Mutation info Missense: E138T [3], [4]
Mutation info Missense: E92Q [3], [4]
Mutation info Missense: G118R [3], [4]
Level of Resistance Low-level resistance
Mutation info Missense: G140A [3], [4]
Mutation info Missense: G140C [3], [4]
Mutation info Missense: G140S [3], [4]
Mutation info Missense: N155H [3], [4]
Mutation info Missense: Q148H [3], [4]
Level of Resistance Low-level resistance
Mutation info Missense: Q148K [3], [4]
Level of Resistance Intermediate resistance
Mutation info Missense: Q148R [3], [4]
Level of Resistance Low-level resistance
Mutation info Missense: S153F [3], [4]
Level of Resistance Low-level resistance
Mutation info Missense: T66K [3], [4]
Level of Resistance Low-level resistance
Mutation info Missense: V151L [3], [4]
Level of Resistance Low-level resistance
Mutation info Missense: S153Y [5]
Level of Resistance Reduce DTG susceptibility about 2 fold
References
REF 1 Viral fitness cost prevents HIV-1 from evading dolutegravir drug pressure. Retrovirology. 2013 Feb 22;10:22.
REF 2 Evolution 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.
REF 3 HIV drug development: the next 25 years. Nat Rev Drug Discov. 2007 Dec;6(12):959-66.
REF 4 The HIVdb system for HIV-1 genotypic resistance interpretation. Intervirology. 2012;55(2):98-101.
REF 5 In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. Antimicrob Agents Chemother. 2011 Feb;55(2):813-21.

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