Drug General Information
Drug ID D0O2EM
Drug Name Nevirapine
Synonyms NEV; NVP; Viramune; Cahill May Roberts Brand of Nevirapine; Promeco Brand of Nevirapine; BI RG 587; BIRG 0587; BIRG 587; BIRG587; BIRG-0587; BIRG-587; NON-NUCLEOSIDE RT INHIBITOR NEVIRAPINE; Nevirapine & PRO 140; Nevirapine [USAN:INN]; Viramune (TN); Viramune(TM); BI-RG-587; Nevirapine & CD4-IgG; Nevirapine (JAN/USP/INN); Viramune, BI-RG 587, Nevirapine; BI-RG-587 & CD4-IgG; N11-Cyclopropyl-4-methyl-5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e]-[1,4]diazepin-6-one & CD4-immunoadhesin; 11-CYCLOPROPYL-5,11-DIHYDRO-4-METHYL-6H-DIPYRIDO[3,2-B:2',3'-E][1,4]DIAZEPIN-6-ONE; 11-Cyclopropyl-4-methyl-5,11-dihydro-6H-dipyrido[2,3-e:3',2'-b][1,4]diazepin-6-one; 11-Cyclopropyl-4-methyl-5,11-dihydro-6H-dipyrido[2,3-e:3',2'-b][1,4]diazepin-6-one & PRO 140 (Anti-CCR5 monoclonal antibody); 11-Cyclopropyl-4-methyl-5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepin-6-one; 11-Cyclopropyl-5,11-dihydro-4-methyl-6H-dipyrido(3,2-b:2',3'-e)(1,4)diazepin-6-one
Drug Type Small molecular drug
Therapeutic Class Anti-HIV Agents
Company Boehringer Ingelheim
Structure D0O2EM
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], [2]
Level of Resistance Reduce NVP susceptibility >50 fold
Mutation info Missense: K103N [3]
Level of Resistance Reduce NVP susceptibility about 50 fold
Mutation info Missense: V106A [4]
Level of Resistance Reduce NVP susceptibility 50 fold
Mutation info Missense: K101P [5]
Level of Resistance Reduce NVP susceptibility >50 fold
Mutation info Missense: Y181C [5]
Level of Resistance Reduce NVP susceptibility >50 fold
Mutation info Missense: V108I [6]
Level of Resistance Reduce NVP susceptibility about 2 fold
Mutation info Missense: A98G [7], [8], [9]
Level of Resistance Reduce NVP susceptibility about 2-3 fold
Mutation info Missense: K101E [3], [5], [10]
Level of Resistance Reduce NVP susceptibility 3-10 fold
Mutation info Missense: N348I [11], [12], [13]
Level of Resistance Reduce NVP susceptibility 3 fold
Mutation info Missense: K101H [5], [10], [14]
Level of Resistance Low-level resistance
Mutation info Missense: G190E [2], [9], [15]
Level of Resistance Confer high-level resistance to NVP
Mutation info Missense: V179E [9], [16], [17]
Level of Resistance Confer low-level resistance to NVP
Mutation info Missense: G190A [7], [8], [18]
Level of Resistance Reduce NVP susceptibility >50 fold
Mutation info Missense: G190S [7], [8], [18]
Level of Resistance Reduce NVP susceptibility >50 fold
Mutation info Missense: K103T [9], [19], [20]
Level of Resistance Reduce NVP susceptibility 10 fold
Mutation info Missense: K103S [8], [19], [21]
Level of Resistance Cause high-level resistance to NVP
Mutation info Missense: K238T [9], [16], [22]
Level of Resistance Reduce NVP susceptibility about 5 fold
Mutation info Missense: Y318F [1], [2]
Level of Resistance Reduce NVP susceptibility about 5 fold
Mutation info Missense: G190Q [18], [21]
Level of Resistance Confer high-level resistance to NVP
Mutation info Missense: Y188H [8], [21]
Level of Resistance Reduce NVP susceptibility 10 fold
Mutation info Missense: V179D [17], [21]
Level of Resistance Reduce NVP susceptibility 2-5 fold
Mutation info Missense: K238N [14], [9]
Level of Resistance Reduce susceptibility to NVP
Mutation info Missense: L100V [23], [9]
Level of Resistance Reduce NVP susceptibility 5 fold
Mutation info Missense: V106M [9], [21]
Level of Resistance Reduce NVP susceptibility >30 fold
Mutation info Missense: F227L [24], [25]
Level of Resistance Intermediate resistance
Mutation info Missense: G190C [24], [25]
Level of Resistance High-level resistance
Mutation info Missense: G190T [24], [25]
Level of Resistance High-level resistance
Mutation info Missense: G190V [24], [25]
Level of Resistance High-level resistance
Mutation info Missense: H221Y [24], [25]
Level of Resistance Low-level resistance
Mutation info Missense: L100I [24], [25]
Level of Resistance High-level resistance
Mutation info Missense: M230L [24], [25]
Level of Resistance High-level resistance
Mutation info Missense: P225H [24], [25]
Level of Resistance Intermediate resistance
Mutation info Missense: V179F [24], [25]
Level of Resistance Low-level resistance
Mutation info Missense: Y181F [24], [25]
Level of Resistance High-level resistance
Mutation info Missense: Y181G [24], [25]
Level of Resistance High-level resistance
Mutation info Missense: Y181I [24], [25]
Level of Resistance High-level resistance
Mutation info Missense: Y181V [24], [25]
Level of Resistance High-level resistance
Mutation info Missense: Y188F [24], [25]
Level of Resistance High-level resistance
Mutation info Missense: K103R + V179D [24], [26]
Level of Resistance Low-level resistance
Mutation info Missense: K103H [19]
Level of Resistance Reduce NVP susceptibility 20 fold
Mutation info Missense: Y181S [27]
Level of Resistance Reduce NVP susceptibility about 30 fold
Mutation info Missense: Y188C [21]
Level of Resistance Reduce NVP susceptibility >50 fold
Mutation info Missense: E138G [28]
Level of Resistance Reduce NVP susceptibility 2 fold
Mutation info Missense: F227C [28]
Level of Resistance Reduce NVP susceptibility 17 fold
Mutation info Missense: M230I [28]
Level of Resistance Reduce NVP susceptibility 16 fold
References
REF 1 A mutation in the 3' region of the human immunodeficiency virus type 1 reverse transcriptase (Y318F) associated with nonnucleoside reverse transcriptase inhibitor resistance. J Virol. 2002 Jul;76(13):6836-40.
REF 2 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 3 Human immunodeficiency virus type 1 mutations selected in patients failing efavirenz combination therapy. Antimicrob Agents Chemother. 2000 Sep;44(9):2475-84.
REF 4 Convergent combination therapy can select viable multidrug-resistant HIV-1 in vitro. Nature. 1993 Sep 30;365(6445):451-3.
REF 5 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 6 Identification of drug resistant mutations in HIV-1 CRF07_BC variants selected by nevirapine in vitro. PLoS One. 2012;7(9):e44333.
REF 7 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 8 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 9 Significantly improved HIV inhibitor efficacy prediction employing proteochemometric models generated from antivirogram data. PLoS Comput Biol. 2013;9(2):e1002899.
REF 10 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 11 N348I in the connection domain of HIV-1 reverse transcriptase confers zidovudine and nevirapine resistance. PLoS Med. 2007 Dec;4(12):e335.
REF 12 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 13 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 14 Nonpolymorphic human immunodeficiency virus type 1 protease and reverse transcriptase treatment-selected mutations. Antimicrob Agents Chemother. 2009 Nov;53(11):4869-78.
REF 15 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 16 Human immunodeficiency virus reverse transcriptase and protease sequence database. Nucleic Acids Res. 2003 Jan 1;31(1):298-303.
REF 17 Compilation and prevalence of mutations associated with resistance to non-nucleoside reverse transcriptase inhibitors. Antivir Ther. 2009;14(1):103-9.
REF 18 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 19 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 20 In vitro selection of mutations in human immunodeficiency virus type 1 reverse transcriptase that confer resistance to capravirine, a novel nonnucl... Antiviral Res. 2006 Jun;70(2):66-74.
REF 21 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 22 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 23 Quantitative prediction of integrase inhibitor resistance from genotype through consensus linear regression modeling. Virol J. 2013 Jan 3;10:8.
REF 24 The HIVdb system for HIV-1 genotypic resistance interpretation. Intervirology. 2012;55(2):98-101.
REF 25 Evolutionary consequences of drug resistance: shared principles across diverse targets and organisms. Nat Rev Genet. 2015 Aug;16(8):459-71.
REF 26 Resistance to direct-acting antiviral agents: clinical utility and significance. Curr Opin HIV AIDS. 2015 Sep;10(5):381-9.
REF 27 Phenotypic drug resistance patterns in subtype A HIV-1 clones with nonnucleoside reverse transcriptase resistance mutations. AIDS Res Hum Retroviruses. 2006 Mar;22(3):289-93.
REF 28 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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