Drug General Information
Drug ID D07HVY
Drug Name Efavirenz
Synonyms EFV; EFZ; Eravirenz; Stocrin; Sustiva; DMP 266; L 743726; DMP-266; L-741211; L-743725; L-743726; Stocrin (TN); Strocin (TM); Sustiva (TM); Sustiva (TN); Efavirenz (JAN/INN); L-743,726; Zoxazin-2-one; Efavirenz, (S)-isomer; Met-SDF-1.beta. & Efavirenz; Met-Stromal Cell-derived Factor-1.beta. (Human) & Efavirenz; (-)-Efavirenz; (4S)-6-Chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one; (4S)-6-Chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-benzo[d][1,3]oxazin-2-one; (4S)-6-chloro-4-(2-cyclopropylethynyl)-4-(trifluoromethyl)-1H-3,1-benzoxazin-2-one; (4S)-6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-benzoxazin-2-one; (S)-6-Chloro-4-(2-cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-ben; (S)-6-Chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one; (S)-6-Chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-benzo[d][1,3]oxazin-2-one; 2H-3,1-Benzoxazin-2-one, 6-chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-, (4S)-(9; 6-chloro-4-(2-cyclopropyl-1-ethynyl)-4-trifluoromethyl-(4S)-1,4-dihydro-2H-benzo[d][1,3]oxazin-2-one
Drug Type Small molecular drug
Therapeutic Class Anti-HIV Agents
Structure D07HVY
Drug Resistance Mutations
Target Name HIV Non-Nucleoside reverse transcriptase Target Info
Uniprot ID POL_HV1B1(600-1159)
Species Human immunodeficiency virus type 1 (HIV-1)
Reference Sequence PISPIETVPVKLKPGMDGPKVKQWPLTEEKIKALVEICTEMEKEGKISKIGPENPYNTPV
FAIKKKDSTKWRKLVDFRELNKRTQDFWEVQLGIPHPAGLKKKKSVTVLDVGDAYFSVPL
DEDFRKYTAFTIPSINNETPGIRYQYNVLPQGWKGSPAIFQSSMTKILEPFKKQNPDIVI
YQYMDDLYVGSDLEIGQHRTKIEELRQHLLRWGLTTPDKKHQKEPPFLWMGYELHPDKWT
VQPIVLPEKDSWTVNDIQKLVGKLNWASQIYPGIKVRQLCKLLRGTKALTEVIPLTEEAE
LELAENREILKEPVHGVYYDPSKDLIAEIQKQGQGQWTYQIYQEPFKNLKTGKYARMRGA
HTNDVKQLTEAVQKITTESIVIWGKTPKFKLPIQKETWETWWTEYWQATWIPEWEFVNTP
PLVKLWYQLEKEPIVGAETFYVDGAANRETKLGKAGYVTNKGRQKVVPLTNTTNQKTELQ
AIYLALQDSGLEVNIVTDSQYALGIIQAQPDKSESELVNQIIEQLIKKEKVYLAWVPAHK
GIGGNEQVDKLVSAGIRKIL [Human immunodeficiency virus type 1 (H
IV-1)]
Targeted Disease HIV infection
Drug Resistance Mutations
Mutation info Missense: Y188L [1]
Level of Resistance Reduce EFV susceptibility 5 fold
Mutation info Missense: K103N [2]
Level of Resistance Reduce EFV susceptibility about 20 fold
Mutation info Missense: V106A [3]
Level of Resistance Reduce EFV susceptibility 5 fold
Mutation info Missense: K101P [4]
Level of Resistance Reduce EFV susceptibility >50 fold
Mutation info Missense: L100I [2]
Level of Resistance High-level resistance
Mutation info Missense: Y181C [4]
Level of Resistance Reduce EFV susceptibility about 2 fold
Mutation info Missense: V108I [5]
Level of Resistance Reduce EFV susceptibility about 2 fold
Mutation info Missense: A98G [6], [7], [8]
Level of Resistance Reduce EFV susceptibility about 2-3 fold
Mutation info Missense: N348I [9], [10], [11]
Level of Resistance Reduce EFV susceptibility 2 fold
Mutation info Missense: K101E [2], [4], [12]
Level of Resistance Reduce EFV susceptibility 1-5 fold
Mutation info Missense: G190E [8], [13], [14]
Level of Resistance Confer high-level resistance to EFV
Mutation info Missense: V179E [8], [15], [16]
Level of Resistance Confer low-level resistance to EFV
Mutation info Missense: G190A [6], [7], [17]
Level of Resistance Reduce EFV susceptibility 5-10 fold
Mutation info Missense: G190S [6], [7], [17]
Level of Resistance Reduce EFV susceptibility >50 fold
Mutation info Missense: K103S [7], [18], [19]
Level of Resistance Cause high-level resistance to EFV
Mutation info Missense: K238T [8], [15], [20]
Level of Resistance Reduce EFV susceptibility about 5 fold
Mutation info Missense: G190Q [17], [19]
Level of Resistance Confer high-level resistance to EFV
Mutation info Missense: Y188H [7], [19]
Level of Resistance Reduce EFV susceptibility 5 fold
Mutation info Missense: V179D [16], [19]
Level of Resistance Reduce EFV susceptibility 2-5 fold
Mutation info Missense: K238N [21], [8]
Level of Resistance Reduce susceptibility to EFV
Mutation info Missense: L100V [22], [8]
Level of Resistance Reduce EFV susceptibility 10 fold
Mutation info Missense: V106M [8], [19]
Level of Resistance Reduce EFV susceptibility >30 fold
Mutation info Missense: F227L [23], [24]
Level of Resistance Low-level resistance
Mutation info Missense: G190C [23], [24]
Level of Resistance High-level resistance
Mutation info Missense: G190T [23], [24]
Level of Resistance High-level resistance
Mutation info Missense: G190V [23], [24]
Level of Resistance High-level resistance
Mutation info Missense: K103R + V179D [23], [24]
Level of Resistance Low-level resistance
Mutation info Missense: K103T [23], [24]
Level of Resistance Low-level resistance
Mutation info Missense: M230L [23], [24]
Level of Resistance Intermediate resistance
Mutation info Missense: P225H [23], [24]
Level of Resistance Intermediate resistance
Mutation info Missense: V106A + F227L [23], [24]
Level of Resistance Low-level resistance
Mutation info Missense: Y181F [23], [24]
Level of Resistance Low-level resistance
Mutation info Missense: Y181G [23], [24]
Level of Resistance Low-level resistance
Mutation info Missense: Y181I [23], [24]
Level of Resistance Intermediate resistance
Mutation info Missense: Y181S [23], [24]
Level of Resistance Low-level resistance
Mutation info Missense: Y181V [23], [24]
Level of Resistance Intermediate resistance
Mutation info Missense: Y188F [23], [24]
Level of Resistance High-level resistance
Mutation info Missense: K103H [18]
Level of Resistance Reduce EFV susceptibility 20 fold
Mutation info Missense: Y188C [19]
Level of Resistance Reduce EFV susceptibility 20 fold
Mutation info Missense: E138G [25]
Level of Resistance Reduce EFV susceptibility 2 fold
Mutation info Missense: F227C [25]
Level of Resistance Reduce EFV susceptibility 4-5 fold
Mutation info Missense: M230I [25]
Level of Resistance Reduce EFV susceptibility 11 fold
References
REF 1 Genotypic correlates of phenotypic resistance to efavirenz in virus isolates from patients failing nonnucleoside reverse transcriptase inhibitor therapy. J Virol. 2001 Jun;75(11):4999-5008.
REF 2 Human immunodeficiency virus type 1 mutations selected in patients failing efavirenz combination therapy. Antimicrob Agents Chemother. 2000 Sep;44(9):2475-84.
REF 3 Convergent combination therapy can select viable multidrug-resistant HIV-1 in vitro. Nature. 1993 Sep 30;365(6445):451-3.
REF 4 Constrained patterns of covariation and clustering of HIV-1 non-nucleoside reverse transcriptase inhibitor resistance mutations. J Antimicrob Chemother. 2010 Jul;65(7):1477-85.
REF 5 Identification of drug resistant mutations in HIV-1 CRF07_BC variants selected by nevirapine in vitro. PLoS One. 2012;7(9):e44333.
REF 6 Distribution of human immunodeficiency virus type 1 protease and reverse transcriptase mutation patterns in 4,183 persons undergoing genotypic resistance testing. Antimicrob Agents Chemother. 2004 Aug;48(8):3122-6.
REF 7 A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase ... Antimicrob Agents Chemother. 2007 Feb;51(2):429-37.
REF 8 Significantly improved HIV inhibitor efficacy prediction employing proteochemometric models generated from antivirogram data. PLoS Comput Biol. 2013;9(2):e1002899.
REF 9 N348I in the connection domain of HIV-1 reverse transcriptase confers zidovudine and nevirapine resistance. PLoS Med. 2007 Dec;4(12):e335.
REF 10 Amino acid mutation N348I in the connection subdomain of human immunodeficiency virus type 1 reverse transcriptase confers multiclass resistance to nucleoside and nonnucleoside reverse transcriptase inhibitors. J Virol. 2008 Apr;82(7):3261-70.
REF 11 Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. Antimicrob Agents Chemother. 2010 May;54(5):1973-80.
REF 12 Characterization of genotypic and phenotypic changes in HIV-1-infected patients with virologic failure on an etravirine-containing regimen in the DUET-1 and DUET-2 clinical studies. AIDS Res Hum Retroviruses. 2010 Nov;26(11):1197-205.
REF 13 TMC125 displays a high genetic barrier to the development of resistance: evidence from in vitro selection experiments. J Virol. 2005 Oct;79(20):12773-82.
REF 14 TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. Antimicrob Agents Chemother. 2010 Feb;54(2):718-27.
REF 15 Human immunodeficiency virus reverse transcriptase and protease sequence database. Nucleic Acids Res. 2003 Jan 1;31(1):298-303.
REF 16 Compilation and prevalence of mutations associated with resistance to non-nucleoside reverse transcriptase inhibitors. Antivir Ther. 2009;14(1):103-9.
REF 17 Amino acid substitutions at position 190 of human immunodeficiency virus type 1 reverse transcriptase increase susceptibility to delavirdine and impair virus replication. J Virol. 2003 Jan;77(2):1512-23.
REF 18 Rare mutations at codon 103 of HIV-1 reverse transcriptase can confer resistance to non-nucleoside reverse transcriptase inhibitors. AIDS. 2005 Mar 24;19(6):549-54.
REF 19 Non-nucleoside reverse transcriptase inhibitor (NNRTI) cross-resistance: implications for preclinical evaluation of novel NNRTIs and clinical genotypic resistance testing. J Antimicrob Chemother. 2014 Jan;69(1):12-20.
REF 20 The K101P and K103R/V179D mutations in human immunodeficiency virus type 1 reverse transcriptase confer resistance to nonnucleoside reverse transcriptase inhibitors. Antimicrob Agents Chemother. 2006 Jan;50(1):351-4.
REF 21 Nonpolymorphic human immunodeficiency virus type 1 protease and reverse transcriptase treatment-selected mutations. Antimicrob Agents Chemother. 2009 Nov;53(11):4869-78.
REF 22 Quantitative prediction of integrase inhibitor resistance from genotype through consensus linear regression modeling. Virol J. 2013 Jan 3;10:8.
REF 23 The HIVdb system for HIV-1 genotypic resistance interpretation. Intervirology. 2012;55(2):98-101.
REF 24 Development and significance of nucleoside drug resistance in infection caused by the human immunodeficiency virus type 1. Clin Invest Med. 1994 Jun;17(3):226-43.
REF 25 Impact of drug resistance-associated amino acid changes in HIV-1 subtype C on susceptibility to newer nonnucleoside reverse transcriptase inhibitors. Antimicrob Agents Chemother. 2015 Feb;59(2):960-71.

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