Compilation and prevalence of mutations associated with resistance to non-nucleoside reverse transcriptase inhibitors

Antiviral Therapy

Volumn 14, Issue 1, 2009, Pages 103-109

  Tambuyzer, Lotke ^a   Azijn, Hilde ^a   Rimsky, Laurence T ^a   Vingerhoets, Johan ^a   Lecocq, Pierre ^b   Kraus, Guenter ^a   Picchio, Gaston ^c   de Béthune, Marie Pierre ^a  

^a TIBOTEC BVBA   (Belgium)

^b Virco BVBA   (Belgium)

^c Tibotec Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

DELAVIRDINE; EFAVIRENZ; ETRAVIRINE; NEVIRAPINE; RNA DIRECTED DNA POLYMERASE INHIBITOR;

ANTIVIRAL RESISTANCE; ARTICLE; CODON; CONTROLLED STUDY; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS 1 INFECTION; IN VITRO STUDY; IN VIVO STUDY; MAJOR CLINICAL STUDY; NUCLEIC ACID BASE SUBSTITUTION; PHENOTYPE; PREVALENCE; PRIORITY JOURNAL; SITE DIRECTED MUTAGENESIS; VIRUS ISOLATION; VIRUS MUTATION;

DRUG RESISTANCE, VIRAL; GENE FREQUENCY; HIV INFECTIONS; HIV REVERSE TRANSCRIPTASE; HIV-1; HUMANS; MUTAGENESIS, SITE-DIRECTED; MUTATION; REVERSE TRANSCRIPTASE INHIBITORS; RNA, VIRAL;

EID: 61849143798     PISSN: 13596535     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (60)

1. Gotte M, Li X, Wainberg MA. HIV-1 reverse transcription: a brief overview focused on structure-function relationships among molecules involved in initiation of the reaction. Arch Biochem Biophys 1999; 365:199-210.
2. Telesnitsky A, Goff SP. Reverse transcriptase and the generation of retroviral DNA. In Coffin JM, Hughes SH, Varmus HE (Editors). Retroviruses. New York: Cold Spring Harbor Laboratory Press 1997. pp.121-160.
3. De Clercq E. Non-nucleoside reverse transcriptase inhibitors (NNRTIs): past, present, and future. Chem Biodivers 2004; 1:44-64.
4. Boone LR. Next-generation HIV-1 non-nucleoside reverse transcriptase inhibitors. Curr Opin Investig Drugs 2006; 7:128-135,
5. US Food and Drug Administration. INTELENCE™. Highlights of prescribing information. (Updated 22 January 2008. Accessed 8 May 2008.) Available from http://www.fda.gov/cder/foi/label/2008/022187lbl.pdf
6. Vingerhoets J, Azijn H, Fransen E, et al. TMC125 displays a high genetic barrier to the development of resistance: evidence from in vitro selection experiments. J Virol 2005; 79:12773-12782.
7. European Medicines Agency (EMEA). Product information for INTELENCE™. 28 August 2008. Available at http://www.emea.europa.eu/ humandocs/Humans/EPAR/intelence/intelence.htm
8. Rinehart AR, Lecocq P, McKenna P, Pattery T, Wasikowski B, Bacheler LT. Predicted phenotypic resistance in routine clinical samples between 1998 and 2003. Antivir Ther 2004; 9:S90.
9. Little SJ, Holte S, Routy JP, et al. Antiretroviral drug resistance among patients recently infected with HIV. N Engl J Med 2002;347:385-394.
10. Wensing AM, Boucher CA. Worldwide transmission of drug-resistant HIV. AIDS Rev 2003; 5:140-155.
11. Johnson VA, Brun-Vézinet F, Clotet B, et al. Update of the drug resistance mutations in HIV-1: 2007. Top HIV Med 2007; 15: 119-125.
12. hnson VA, Brun-Vézinet F, Clotet B, et al. Update of the drug resistance mutations in HIV-1: Spring 2008. Top HIV Med 2008; 16:62-68.
13. Parkin NT, Gupta S, Chappey C, Petropoulos CJ. The K101P and K103R/V179D mutations in human immunodeficiency virus type 1 reverse transcriptase confer resistance to non-nucleoside reverse transcriptase inhibitors. Antimicrob Agents Chemother 2006; 50:351-354.
14. Harrigan PR, Mo T, Wynhoven B, et al. Rare mutations at codon 103 of HIV-1 reverse transcriptase can confer resistance to non-nucleoside reverse transcriptase inhibitors. AIDS 2005; 19:549-554.
15. Pelemans H, Aertsen A, Van Laethem K, et al. Site-directed mutagenesis of human immunodeficiency virus type 1 reverse transcriptase at amino acid position 138. Virology 2001; 280:97-106.
16. The Stanford University HIV Drug Resistance Database. NNRTI resistance notes: NNRTI resistance matrix. (Updated 25 September 2007. Accessed 1 February 2008.) Available from http://hivdb.stanford.edu/cgi-bin/ NNRTIResiNote.cgi
17. Vermeiren H, Van Craenenbroeck E, Alen P, et al. Prediction of HIV-1 drug susceptibility phenotype from the viral genotype using linear regression modeling. J Virol Methods 2007; 145:47-55.
18. Clark S, Calef C, Mellors J. Mutations in retroviral genes associated with drug resistance. In Leitner T, Foley B, Hahn B, et al. (Editors). HIV Sequence Compendium 2006/2007. New Mexico: Theoretical Biology and Biophysics Group 2007. pp. 58-158.
19. Vingerhoets J, Buelens A, Peeters M, et al. Impact of baseline NNRTI mutations on the virological response to TMC125 in the phase III clinical trials DUET-1 and DUET-2. Antivir Ther 2007; 12 Suppl 1:S34.
20. Byrnes VW, Sardana VV, Schleif WA, et al. Comprehensive mutant enzyme and viral variant assessment of human immunodeficiency virus type 1 reverse transcriptase resistance to nonnucleoside inhibitors. Antimicrob Agents Chemother 1993; 37:1576-1579.
21. Bacheler LT, Anton ED, Kudish P, et al. Human immunodeficiency virus type 1 mutations selected in patients failing efavirenz combination therapy. Antimicrob Agents Chemother 2000; 44:2475-2484.
22. Mellors JW, Im GJ, Tramontano E, et al. A single conservative amino acid substitution in the reverse transcriptase of human immunodeficiency virus-1 confers resistance to (+)-(5S)-4,5,6,7-tetrahydro-5-methyl-6-(3-methyl-2-butenyl) imidazo[4,5,1-jk [1,4] benzodiazepin-2(1H)-thione (TIBO R82150). Mol Pharmacol 1993; 43:11-16.
23. Rhee S-Y, Liu T, Ravela J, Gonzales MJ, Shafer, RW. 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; 48:3122-3126.
24. Kleim J-P, Winters M, Dunkler A, et al. Antiviral activity of the human immunodeficiency virus type 1-specific nonnucleoside reverse transcriptase inhibitor HBY 097 alone and in combination with zidovudine in a phase II study. J Infect Dis 1999; 179:709-713.
25. Ceccherini-Silberstein F, Svicher V, Sing T, et al. Characterization and structural analysis of novel mutations in HIV-1 reverse transcriptase involved in the regulation of resistance to nonnucleoside inhibitors. J Virol 2007; 81:11507-11519.
26. Nunberg JH, Schlelf WA, Boots EJ, et al. Viral resistance to human immunodeficiency virus type 1-specific pyridinone reverse transcriptase inhibitors. J Virol 1991; 65:4887-4892.
27. Larder BA. 3′-Azido-3′-deoxythymidine resistance suppressed by a mutation conferring human immunodeficiency virus type 1 resistance to nonnucleoside reverse transcriptase inhibitors. Antimicrob Agents Chemother 1992; 36:2664-2669.
28. Kleim JP, Winkler I, Rösner M, et al. In vitro selection for different mutational patterns in the HIV-1 reverse transcriptase using high and low selective pressure of the nonnucleoside reverse transcriptase inhibitor HBY 097. Virology 1997; 231:112-118.
29. Taylor DL, Ahmed PS, Tyms AS, et al. Drug resistance and drug combination features of the human immunodeficiency virus inhibitor BCH-10652 [(+/-)-2′-deoxy-3′-oxa-4′-thiocytidine, d0TC]. Antivir Chem Chemother 2000; 11:291-301.
30. Loemba H, Brenner B, Parniak MA, et al. Genetic divergence of human immunodeficiency virus type 1 Ethiopian clade C reverse transcriptase (RT) and rapid development of resistance against non-nucleoside inhibitors of RT. Antimicrob Agents Chemother 2002; 46:2087-2094.
31. Balzarini J, Karlsson A, Sardana VV, Emini EA, Camarasa MJ, De Clercq E. Human immunodeficiency virus 1 (HIV-1)-specific reverse transcriptase (RT) inhibitors may suppress the replication of specific drug-resistant (E138K) RT HIV-1 mutants or select for highly resistant (Y181C- >C181I) RT HIV-1 mutants. Proc Natl Acad Sci U S A 1994; 91:6599-6603.
32. McCreedy B, Borroto-Esoda K, Harris J, Klish C, Fang L, Miralles D. Genotypic and phenotypic analysis of HIV-1 from patients receiving combination therapy containing two nucleoside reverse transcriptase inhibitors (NRTIs) and the non-NRTI, emivirine (MKC-442). Antivir Ther 1999; 4 Suppl 1:9.
33. Palmer P, Dam E, Ferchal F, et al. V106M and V179D, a novel HIV-1 reverse transcriptase (RT) combination of mutations conferring high-level resistance to non-nucleoside RT inhibitors. Antivir Ther 2003; 8 Suppl 1:S411-S412.
34. Vingerhoets J, Peeters M, Corbett C, et al. Effect of baseline resistance on the virologic response to a novel NNRTI, TMC125, in patients with extensive NNRTI and PI resistance: analysis of study TMC125-223. 13th Conference on Retroviruses and Opportunistic Infections. 5-8 February 2006, Denver, CO, USA. Abstract 154.
35. Miller MD, Margot NA, McColl DJ, et al. Characterization of resistance mutation patterns emerging over 2 years during first-line antiretroviral treatment with tenofovir DF or stavudine in combination with lamivudine and efavirenz. 12th International Drug Resistance Workshop. 10-14 June 2003, Cabo del Sol, Los Cabos, Mexico. Abstract 135.
36. Turner D, Brenner B, Moisi D, et al. Nucleotide and amino acid polymorphisms at drug resistanz ce sites in non-B-subtype variants of human immunodeficiency virus type 1. Antimicrob Agents Chemother 2004; 48:2993-2998.
37. Shih CK, Rose JM, Hansen GL, et al. Chimeric human immunodeficiency virus type 1/type 2 reverse transcriptases display reversed sensitivity to nonnucleoside analog inhibitors. Proc Natl Acad Sci U S A 1991; 88:9878-9882.
38. Richman DD. Resistance of clinical isolates of human immunodeficiency virus to antiretroviral agents. Antimicrob Agents Chemother 1993; 37:1207-1213.
39. Sardana VV, Emini EA, Gotlib L, et al. Functional analysis of HIV-1 reverse transcriptase amino acids involved in resistance to multiple nonnucleoside inhibitors. J Biol Chem 1992; 267:17526-17530.
40. Kleim JP, Rösner M, Winkler I, et al. Selective pressure of a quinoxaline nonnucleoside inhibitor of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) on HIV-1 replication results in the emergence of nucleoside RT-inhibitor-specific (RT Leu-74->Val or Ile and Val-75->Leu or Ile) HIV-1 mutants. Proc Natl Acad Sci U S A 1996; 93:34-38.
41. Bacolla A, Shih CK, Rose JM, et al. Amino acid substitutions in HIV-1 reverse transcriptase with corresponding residues from HIV-2. Effect on kinetic constants and inhibition by non-nucleoside analogs. J Biol Chem 1993; 268:16571-16577.
42. Huang W, Gamarnik A, Limoli K, Petropoulos CJ, Whitcomb JM. Amino acid substitutions at position 190 of human immunodeficiency virus type 1 reverse transcriptase increase susceptibility to delavirdine and impair virus replication. J Virol2003; 77:1512-1523.
43. Kleim J-P, Bender R, Billhardt U-M, et al. Activity of a novel quinoxaline derivative against human immunodeficiency virus type 1 reverse transcriptase and viral replication. Antimicrob Agents Chemother 1993; 37:1659-1664.
44. Kleim JP, Bender R, Kirsch R, Meichsner C, Paessens A, Rieb G. Mutational analysis of residue 190 of human immunodeficiency virus type 1 reverse transcriptase. Virology 1994; 200:696-701.
45. Gonzales MJ, Wu TD, Taylor J, et al. Extended spectrum of HIV-1 reverse transcriptase mutations in patients receiving multiple nucleoside analog inhibitors. AIDS 2003; 17:791-799.
46. Saracino A, Monno L, Scudeller L, et al. Impact of unreported HIV-1 reverse transcriptase mutations on phenotypic resistance to nucleoside and non-nucleoside inhibitors. J Med Virol 2006; 78:9-17.
47. Perno CF, Svicher V, Ceccherini-Silberstein F. Novel drug resistance mutations in HIV: recognition and clinical relevance. AIDS Rev 2006; 8:179-190.
48. Andries K, Azijn H, Thielemans T, et al. TMC125, a novel next-generation nonnucleoside reverse transcriptase inhibitor active against nonnucleoside reverse transcriptase inhibitor-resistant human immunodeficiency virus type 1. Antimicrob Agents Chemother 2004; 48:4680-4686.
49. Parkin NT, Deeks SG, Wrin MT, et al. Loss of antiretroviral drug susceptibility at low viral load during early virological failure in treatment-experienced patients. AIDS 2000; 14:2877-2887.
50. Dueweke TJ, Pushkarskaya T, Poppe SM, et al. A mutation in reverse transcriptase of bis (heteroaryl) piperazine-resistant human immunodeficiency virus type 1 that confers increased sensitivity to other nonnucleoside inhibitors. Proc Natl Acad Sci U S A 1993; 90:4713-4717.
51. Demeter LM, Meehan PM, Morse G, et al. Phase I study of atevirdine mesylate (U-87201E) monotherapy in HIV-1 -infected patients. J Acquir Immune Defic Syndr Hum Retrovirol 1998; 19:135-144.
52. Pelemans H, Esnouf RM, Jonckheere H, De Clercq E, Balzarini J. Mutational analysis of tyr-318 within the non-nucleoside reverse transcriptase inhibitor binding pocket of human immunodeficiency virus type I reverse transcriptase. J Biol Chem 1998; 273:34234-34239.
53. Harrigan PR, Salim M, Stammers DK, et al. 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; 76:6836-6840.
54. Janssen PAJ, Lewi PJ, Arnold E, et al. In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4- 4-4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2-pyrimidinyl] amino]benzonitrile (R278474, rilpivirine). J Med Chem 2005; 48:1901-1909.
55. Bonneau P, Robinson P, Duan J, et al. Antiviral characterization and human experience with BILR 355 BS, a novel next-generation non-nucleoside reverse transcriptase inhibitor with a broad anti HIV-1 profile. 12th Conference on Retroviruses and Opportunistic Infections. 22-25 February 2005, Boston, MA, USA. Abstract 558.
56. Hamatake R, Zhang Z, Xu W, et al. RDEA806, a potent NNRTI with a high genetic barrier to resistance. 47th Interscience Conference on Antimicrobial Agents and Chemotherapy. 17-20 September 2007, Chicago, IL, USA. Abstract 1662.
57. Gupta S, Fransen S, Paxinos E, et al. Infrequent occurrence of mutations in the C-terminal region of reverse transcriptase modulates susceptibility to RT inhibitors. Antivir Ther 2006; 11 Suppl 1:S143.
58. Yap SH, Sheen CW, Fahey J, et al. N3481 in the connection domain of HIV-1 reverse transcriptase confers zidovudine and nevirapine resistance. PLoS Med 2007; 4:335.
59. Hachiya A, Kodama EN, Sarafianos SG, et al. Amino acid mutation N348I in the connection subdomain of human immunodeficiency virus type 1 reverse transcriptase confers multiclass resistance to nucleoside and non-nucleoside reverse transcriptase inhibitors. J Virol 2008; 82:3261-3270.
60. Kearny M, Palmer S, Maldarelli F, et al. Frequent polymorphism at drug resistance sites in HIV-1 protease and reverse transcriptase. AIDS 2008; 22:497-501.