| Drug General Information |
| Drug ID |
D0L3MP
|
| Drug Name |
VRX496 |
|
| Synonyms |
Nelfinavir; nelfinavir; 159989-64-7; Viracept; Nelfinavir [INN:BAN]; AG1343; UNII-HO3OGH5D7I; AG-1343; C32H45N3O4S; NELFINAVIR MESYLATE AG1343; Viracept (TN); HO3OGH5D7I; CHEBI:7496; AG 1343; NLF; 1UN; 2-[2-HYDROXY-3-(3-HYDROXY-2-METHYL-BENZOYLAMINO)-4-PHENYL SULFANYL-BUTYL]-DECAHYDRO-ISOQUINOLINE-3-CARBOXYLIC ACID TERT-BUTYLAMIDE; (3S-(2(2S*,3S*),3alpha,4abeta,8abeta))-N-(1,1-Dimethylethyl)decahydro-2-(2-hydroxy-3-((3-hydroxy-2-methylbenzoyl)amino)-4-(phenylthio)butyl)-3-isoquinolinecarboxamide; NFV; NFV; Nelfinavir Monomethane Sulfonate; AG1346; Nelfinavir (INN); Nelfinavir [BAN:INN]; AG1343 (*Mesylate salt*); Viracept (TM)(*Mesylate salt*); Met-SDF-1beta & Nelfinavir; Met-Stromal Cell-derived Factor-1beta (Human) & Nelfinavir; (3S,4aS,8aS)-N-tert-butyl-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-phenylsulfanylbutyl]-3,4,4a,5,6,7,8,8a-octahydro-1H-isoquinoline-3-carboxamide |
| Drug Type |
Antisense drug |
| Therapeutic Class |
Antisense |
| Company |
VIRxSYS Corporation |
| Drug Resistance Mutations |
| Target Name |
HIV Protease |
Target Info |
| Uniprot ID |
POL_HV1B1(501-599) |
| Species |
Human immunodeficiency virus type 1 (HIV-1) |
| Reference Sequence |
PQITLWQRPLVTIKIGGQLKEALLDTGADDTVLEEMSLPGRWKPKMIGGIGGFIKVRQYD
QILIEICGHKAIGTVLVGPTPVNIIGRNLLTQIGCTLNF [Human immunodeficie
ncy virus type 1 (HIV-1)]
|
| Targeted Disease |
HIV infection |
| Drug Resistance Mutations |
| Mutation info |
Missense: L90M |
[1] |
| Level of Resistance |
High-level resistance |
|
| Mutation info |
Missense: N88S |
[2] |
| Level of Resistance |
Reduce susceptibility to NFV |
|
| Mutation info |
Missense: D30N |
[3] |
| Level of Resistance |
Confer high-level resistance to NFV |
|
| Mutation info |
Missense: V82A |
[4] |
| Level of Resistance |
Confer reduce susceptibility to NFV |
|
| Mutation info |
Missense: V82F |
[5] |
| Level of Resistance |
Reduce susceptibility to NFV |
|
| Mutation info |
Missense: N88D |
[2] |
| Level of Resistance |
High-level resistance |
|
| Mutation info |
Missense: L24I |
[6] |
| Level of Resistance |
Reduce susceptibility to NFV |
|
| Mutation info |
Missense: G48V |
[5] |
| Level of Resistance |
Confer intermediate-level resistance to NFV |
|
| Mutation info |
Missense: F53L |
[4], [5], [7] |
| Level of Resistance |
Reduce susceptibility to NFV |
|
| Mutation info |
Missense: L10F |
[8], [9], [10] |
| Level of Resistance |
Reduce susceptibility to NFV in vitro |
|
| Mutation info |
Missense: N83D |
[5], [11], [12] |
| Level of Resistance |
Reduce susceptibility to NFV |
|
| Mutation info |
Missense: L89V |
[4], [13], [14] |
| Level of Resistance |
Reduce susceptibility to NFV |
|
| Mutation info |
Missense: G48M |
[7], [15], [16] |
| Level of Resistance |
Intermediate resistance |
|
| Mutation info |
Missense: I54A |
[17], [18], [19] |
| Level of Resistance |
Low-level resistance |
|
| Mutation info |
Missense: L24F |
[20], [5] |
| Level of Resistance |
Reduce susceptibility to NFV |
|
| Mutation info |
Missense: G48A |
[17], [18] |
| Level of Resistance |
Intermediate resistance |
|
| Mutation info |
Missense: G48L |
[17], [18] |
| Level of Resistance |
Intermediate resistance |
|
| Mutation info |
Missense: G48Q |
[17], [18] |
| Level of Resistance |
Intermediate resistance |
|
| Mutation info |
Missense: G48S |
[17], [18] |
| Level of Resistance |
Intermediate resistance |
|
| Mutation info |
Missense: G48T |
[17], [18] |
| Level of Resistance |
Intermediate resistance |
|
| Mutation info |
Missense: G73A |
[17], [18] |
| Level of Resistance |
Low-level resistance |
|
| Mutation info |
Missense: G73C |
[17], [18] |
| Level of Resistance |
Low-level resistance |
|
| Mutation info |
Missense: G73S |
[17], [18] |
| Level of Resistance |
Low-level resistance |
|
| Mutation info |
Missense: G73T |
[17], [18] |
| Level of Resistance |
Low-level resistance |
|
| Mutation info |
Missense: I47A |
[17], [18] |
| Level of Resistance |
Intermediate resistance |
|
| Mutation info |
Missense: I47V |
[17], [18] |
| Level of Resistance |
Low-level resistance |
|
| Mutation info |
Missense: I50V |
[17], [18] |
| Level of Resistance |
Low-level resistance |
|
| Mutation info |
Missense: I54L |
[17], [19] |
| Level of Resistance |
Low-level resistance |
|
| Mutation info |
Missense: I54M |
[17], [19] |
| Level of Resistance |
Low-level resistance |
|
| Mutation info |
Missense: I54S |
[17], [19] |
| Level of Resistance |
Low-level resistance |
|
| Mutation info |
Missense: I54T |
[17], [19] |
| Level of Resistance |
Low-level resistance |
|
| Mutation info |
Missense: I54V |
[17], [19] |
| Level of Resistance |
Low-level resistance |
|
| Mutation info |
Missense: I84A |
[17], [19] |
| Level of Resistance |
High-level resistance |
|
| Mutation info |
Missense: I84C |
[17], [19] |
| Level of Resistance |
High-level resistance |
|
| Mutation info |
Missense: I84V |
[17], [19] |
| Level of Resistance |
High-level resistance |
|
| Mutation info |
Missense: K20T |
[17], [19] |
| Level of Resistance |
Low-level resistance |
|
| Mutation info |
Missense: L33F |
[17], [19] |
|
| Mutation info |
Missense: M46I |
[17], [19] |
| Level of Resistance |
Intermediate resistance |
|
| Mutation info |
Missense: M46L |
[17], [19] |
| Level of Resistance |
Low-level resistance |
|
| Mutation info |
Missense: M46V |
[17], [19] |
| Level of Resistance |
Low-level resistance |
|
| Mutation info |
Missense: N88G |
[17], [19] |
| Level of Resistance |
Intermediate resistance |
|
| Mutation info |
Missense: N88T |
[17], [19] |
| Level of Resistance |
Intermediate resistance |
|
| Mutation info |
Missense: T74P |
[17], [19] |
| Level of Resistance |
Low-level resistance |
|
| Mutation info |
Missense: V32I |
[17], [19] |
| Level of Resistance |
Low-level resistance |
|
| Mutation info |
Missense: V82C |
[17], [19] |
| Level of Resistance |
Intermediate resistance |
|
| Mutation info |
Missense: V82M |
[17], [19] |
| Level of Resistance |
Intermediate resistance |
|
| Mutation info |
Missense: V82S |
[17], [19] |
| Level of Resistance |
Intermediate resistance |
|
| Mutation info |
Missense: V82T |
[17], [19] |
| Level of Resistance |
Intermediate resistance |
|
| Mutation info |
Missense: L23I |
[21] |
| Level of Resistance |
Confer low/intermediate-level resistance to NFV |
|
| Mutation info |
Missense: L90M |
[22] |
| Mutation Frequency |
1 out of 31 samples |
|
| Mutation info |
Missense: K65R |
[23] |
| Mutation Frequency |
7 out of 37 samples |
|
| References |
| REF 1 |
The effect of high-dose saquinavir on viral load and CD4+ T-cell counts in HIV-infected patients. Ann Intern Med. 1996 Jun 15;124(12):1039-50.
|
| REF 2 |
Genotypic and phenotypic characterization of human immunodeficiency virus type 1 variants isolated from patients treated with the protease inhibitor nelfinavir. Antimicrob Agents Chemother. 1998 Oct;42(10):2637-44.
|
| REF 3 |
Postpartum antiretroviral drug resistance in HIV-1-infected women receiving pregnancy-limited antiretroviral therapy. AIDS. 2010 Jan 2;24(1):45-53.
|
| REF 4 |
Human immunodeficiency virus reverse transcriptase and protease sequence database. Nucleic Acids Res. 2003 Jan 1;31(1):298-303.
|
| REF 5 |
HIV-1 protease mutations and protease inhibitor cross-resistance. Antimicrob Agents Chemother. 2010 Oct;54(10):4253-61.
|
| REF 6 |
Genetic correlates of in vivo viral resistance to indinavir, a human immunodeficiency virus type 1 protease inhibitor. J Virol. 1996 Dec;70(12):8270-6.
|
| REF 7 |
Prediction of HIV-1 drug susceptibility phenotype from the viral genotype using linear regression modeling. J Virol Methods. 2007 Oct;145(1):47-55.
|
| REF 8 |
Broad 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.
|
| REF 9 |
Selection of diverse and clinically relevant integrase inhibitor-resistant human immunodeficiency virus type 1 mutants. Antiviral Res. 2008 Nov;80(2):213-22.
|
| REF 10 |
Resistance mutations in human immunodeficiency virus type 1 integrase selected with elvitegravir confer reduced susceptibility to a wide range of integrase inhibitors. J Virol. 2008 Nov;82(21):10366-74.
|
| REF 11 |
Genotypic changes in human immunodeficiency virus type 1 protease associated with reduced susceptibility and virologic response to the protease inh... J Virol. 2006 Nov;80(21):10794-801.
|
| REF 12 |
Improving the prediction of virological response to tipranavir: the development and validation of a tipranavir-weighted mutation score. Antivir Ther. 2010;15(7):1011-9.
|
| REF 13 |
Factors associated with the selection of mutations conferring resistance to protease inhibitors (PIs) in PI-experienced patients displaying treatme... Antimicrob Agents Chemother. 2008 Feb;52(2):491-6.
|
| REF 14 |
Pattern and impact of emerging resistance mutations in treatment experienced patients failing darunavir-containing regimen. AIDS. 2008 Sep 12;22(14):1809-13.
|
| REF 15 |
Improving lopinavir genotype algorithm through phenotype correlations: novel mutation patterns and amprenavir cross-resistance. AIDS. 2003 May 2;17(7):955-61.
|
| REF 16 |
HIV-1 subtype B protease and reverse transcriptase amino acid covariation. PLoS Comput Biol. 2007 May;3(5):e87.
|
| REF 17 |
The HIVdb system for HIV-1 genotypic resistance interpretation. Intervirology. 2012;55(2):98-101.
|
| REF 18 |
Tackling the problem of HIV drug resistance. Postepy Biochem. 2016;62(3):273-279.
|
| REF 19 |
How to win the HIV-1 drug resistance hurdle race: running faster or jumping higher Biochem J. 2017 Apr 26;474(10):1559-1577.
|
| REF 20 |
Nonpolymorphic human immunodeficiency virus type 1 protease and reverse transcriptase treatment-selected mutations. Antimicrob Agents Chemother. 2009 Nov;53(11):4869-78.
|
| REF 21 |
Association of a novel human immunodeficiency virus type 1 protease substrate cleft mutation, L23I, with protease inhibitor therapy and in vitro drug resistance. Antimicrob Agents Chemother. 2004 Dec;48(12):4864-8.
|
| REF 22 |
HIV-1 drug-resistance surveillance among treatment-experienced and -nae patients after the implementation of antiretroviral therapy in Ghana. PLoS One. 2013 Aug 19;8(8):e71972.
|
| REF 23 |
Prevalence and dynamics of the K65R drug resistance mutation in HIV-1-infected infants exposed to maternal therapy with lamivudine, zidovudine and either nevirapine or nelfinavir in breast milk. J Antimicrob Chemother. 2016 Jun;71(6):1619-26.
|
