Patterns of resistance emerging in HIV-1 from antiretroviral-experienced patients undergoing intensification therapy with tenofovir disoproxil fumarate

Journal of Acquired Immune Deficiency Syndromes

Volumn 37, Issue 3, 2004, Pages 1340-1350

  McColl, Damian J ^a   Margot, Nicolas A ^a   Wulfsohn, Michael ^a   Coakley, Dion F ^a   Cheng, Andrew K ^a   Miller, Michael D ^a  

^a GILEAD SCIENCES   (United States)

Author keywords

Drug resistance; Genotype; HIV 1; Mutation; Phenotype; Reverse transcriptase (RT); Tenofovir

Indexed keywords

ABACAVIR; AMPRENAVIR; ANTIRETROVIRUS AGENT; DIDANOSINE; EFAVIRENZ; LAMIVUDINE; NELFINAVIR; NEVIRAPINE; NUCLEOSIDE; PROTEINASE INHIBITOR; RNA DIRECTED DNA POLYMERASE INHIBITOR; STAVUDINE; TENOFOVIR DISOPROXIL; THYMINE DERIVATIVE; ZALCITABINE; ZIDOVUDINE;

ADD ON THERAPY; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DOUBLE BLIND PROCEDURE; DRUG RESPONSE; DRUG SENSITIVITY; GENE MUTATION; GENOTYPE; HIGHLY ACTIVE ANTIRETROVIRAL THERAPY; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS 1; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; INTENSIFICATION THERAPY; MAJOR CLINICAL STUDY; MULTICENTER STUDY; PHASE 3 CLINICAL TRIAL; PHENOTYPE; PHENOTYPIC DRUG SENSITIVITY; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; REBOUND; VIRUS LOAD;

ACQUIRED IMMUNODEFICIENCY SYNDROME; ADENINE; AMINO ACID SUBSTITUTION; DOUBLE-BLIND METHOD; DRUG ADMINISTRATION SCHEDULE; DRUG RESISTANCE, VIRAL; DRUG THERAPY, COMBINATION; GENOTYPE; HIV INFECTIONS; HIV-1; HUMANS; PHENOTYPE; PHOSPHONIC ACIDS; PLACEBOS; POLYMORPHISM, SINGLE NUCLEOTIDE; REVERSE TRANSCRIPTASE INHIBITORS; RNA, VIRAL; RNA-DIRECTED DNA POLYMERASE;

EID: 7244248649     PISSN: 15254135     EISSN: None     Source Type: Journal    
DOI: 10.1097/00126334-200411010-00002     Document Type: Article

References (50)

1. Squires KE. An introduction to nucleoside and nucleotide analogues. Antivir Ther.2001;6:1-14.
2. Volberding PA. HIV therapy in 2003: consensus and controversy. AIDS. 2003;17:S4-S11.
3. Whitcomb JM, Parkin NT, Chappey C, et al. Broad nucleoside reverse-transcriptase inhibitor cross-resistance in human immunodeficiency virus type 1 clinical isolates. J Infect Dis. 2003;188:992-1000.
4. Naesens L, Snoeck R, Andrei G, et al. HPMPC (cidofovir), PMEA (adefovir) and related acyclic nucleoside phosphonate analogues: a review of their pharmacology and clinical potential in the treatment of viral infections. Antivir Chem Chemother. 1997;8:1-23.
5. Mulato AS, Cherrington JM. Anti-HIV activity of adefovir (PMEA) and PMPA in combination with antiretroviral compounds: in vitro analyses. Antiviral Res. 1997;36:91-97.
6. Balzarini J, Aquaro S, Perno CF, et al. Activity of the (R)-enantiomers of 9-(2-phosphonylmethoxypropyl)-adenine and 9-(2-phosphonylmethoxypropyl)-2,6- diaminopurine against human immunodeficiency virus in different human cell systems. Biochem Biophys Res Commun. 1996;219: 337-341.
7. Srinivas RV, Robbins BL, Connelly MC, et al. Metabolism and in vitro antiretroviral activities of bis(pivaloyloxymethyl) prodrugs of acyclic nucleoside phosphonates. Antimicrob Agents Chemother. 1993;37:2247-2250.
8. Balzarini J, Holy A, Jindrich J, et al. Differential antiherpesvirus and antiretrovirus effects of the (S) and (R) enantiomers of acyclic nucleoside phosphonates: potent and selective in vitro and in vivo antiretrovirus activities of (R)-9-(2-phosphonomethoxypropyl)-2, 6-diaminopurine. Antimicrob Agents Chemother. 1993;37:332-338.
9. Ying C, De Clercq E, Nicholson W, et al. Inhibition of the replication of the DNA polymerase M550V mutation variant of human hepatitis B virus by adefovir, tenofovir, L-FMAU, DAPD, penciclovir and lobucavir. J Viral Hepat. 2000;7:161-165.
10. Nelson M, Portsmouth S, Stebbing J, et al. An open-label study of tenofovir in HIV-1 and Hepatitis B virus co-infected individuals. AIDS. 2003; 17:F7-F10.
11. Ristig MB, Crippin J, Aberg JA, et al. Tenofovir disoproxil fumarate therapy for chronic hepatitis B in human immunodeficiency virus/hepatitis B virus-coinfected individuals for whom interferon-alpha and lamivudine therapy have failed. J Infect Dis. 2002;186:1844-1847.
12. Wainberg MA, Miller MD, Quan Y, et al. In vitro selection and characterization of HIV-1 with reduced susceptibility to PMPA. Antivir Ther. 1999;4:87-94.
13. Margot NA, Isaacson E, McGowan I, et al. Extended treatment with tenofovir disoproxil fumarate in treatment-experienced HIV-1 -infected patients: genotypic, phenotypic, and rebound analyses. J Acquir Immune Defic Syndr Hum Retrovirol. 2003;33:15-21.
14. Tisdale M, Alnadaf T, Cousens D. Combination of mutations in human immunodeficiency virus type 1 reverse transcriptase required for resistance to the carbocyclic nucleoside 1592U89. Antimicrob Agents Chemother. 1997;41:1094-1098.
15. Harrigan PR, Stone C, Griffin P, et al. Resistance profile of the human immunodeficiency virus type 1 reverse transcriptase inhibitor abacavir (1592U89) after monotherapy and combination therapy. J Infect Dis. 2000;181:912-920.
16. Winters MA, Shafer RW, Jellinger RA, et al. Human immunodeficiency virus type 1 reverse transcriptase genotype and drug susceptibility changes in infected individuals receiving dideoxyinosine monotherapy for 1 to 2 years. Antimicrob Agents Chemother. 1997;41:757-762.
17. Garcia-Lerma JG, MacInnes H, Bennett D, et al. A novel genetic pathway of human immunodeficiency virus type 1 resistance to stavudine mediated by the K65R mutation. J Virol. 2003;77:5685-5693.
18. Gu Z, Fletcher RS, Arts EJ, et al. The K65R mutant reverse transcriptase of HIV-1 cross-resistant to 2′,3′-dideoxycytidine, 2′,3′-dideoxy-3′-thiacytidine, and 2′,3′- dideoxyinosine shows reduced sensitivity to specific dideoxynucleoside triphosphate inhibitors in vitro. J Biol Chem. 1994;269:28118-28122.
19. Zhang D, Caliendo AM, Eron JJ, et al. Resistance to 2′,3′- dideoxycytidine conferred by a mutation in codon 65 of the human immunodeficiency virus type 1 reverse transcriptase. Antimicrob Agents Chemother. 1994;38:282-287.
20. Bloor S, Kemp SD, Hertogs K, et al. Patterns of HIV drug resistance in routine clinical practice: a survey of almost 12000 samples from the USA in 1999. Antivir Ther. 2000;5:132.
21. Parikh U, Koontz D, Hammond J, et al. K65R: a multi-nucleoside resistance mutation of low but increasing frequency. Antivir Ther. 2003;8: S152.
22. Lanier ER, Scott J, Ait-Khaled M, et al. Prevalence of mutations associated with resistance to antiretroviral therapy from 1999-2002. Paper presented at: 10th Conference on Retroviruses and Opportunistic Infections; February 10-14, 2003; Boston.
23. Miller MD, McCoIl DJ, White KL, et al. Genotypic and phenotypic characterization of patient-derived HIV-1 isolates containing the K65R mutation in reverse transcriptase (RT). Paper presented at: 43rd Annual Interscience Conference on Antimicrobial Agents and Chemotherapy; September 14-17, 2003; Chicago.
24. Schooley RT, Ruane P, Myers RA, et al. Tenofovir DF in antiretroviral-experienced patients: results from a 48-week, randomized, double-blind study. AIDS. 2002;16:1257-1263.
25. Margot NA, Isaacson E, McGowan I, et al. Genotypic and phenotypic analyses of HIV-1 in antiretroviral-experienced patients treated with tenofovir DF. AIDS. 2002;16:1227-1235.
26. Squires K, Pozniak AL, Pierone G Jr, et al. Tenofovir disoproxil fumarate in nucleoside-resistant HIV-1 infection. Ann Intern Med. 2003;139:313-321.
27. White KL, Margot NA, Wrin T, et al. Molecular mechanisms of resistance to human immunodeficiency virus type 1 with reverse transcriptase mutations K65R and K65R + M184V and their effects on enzyme function and viral replication capacity. Antimicrob Agents Chemother. 2002;46: 3437-3446.
28. Miller MD, White KL, Petropoulos CJ, et al. Decreased replication capacity of HIV-1 clinical isolates containing K65R or M184V RT mutations. Paper presented at: 10th Conference on Retroviruses and Opportunistic Infections; February 10-14, 2003; Boston.
29. DeGruttola V, Dix L, D'Aquila R, et al. The relation between baseline HIV drug resistance and response to antiretroviral therapy: re-analysis of retrospective and prospective studies using a standardized data analysis plan. Antivir Ther. 2000;5:41-48.
30. Hertogs K, de Bethune MP, Miller V, et al. A rapid method for simultaneous detection of phenotypic resistance to inhibitors of protease and reverse transcriptase in recombinant human immunodeficiency virus type 1 isolates from patients treated with antiretroviral drugs. Antimicrob Agents Chemother. 1998;42:269-276.
31. Miller MD, Margot N, Lu B, et al. Genotypic and phenotypic predictors of the magnitude of treatment response to tenofovir disoproxil fumarate in antiretroviral-experienced patients. J Infect Dis. 2004;189:837-846.
32. 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.
33. Roge BT, Katzenstein TL, Obel N, et al. K65R with and without S68: a new resistance profile in vivo detected in most patients failing abacavir, didanosine and stavudine. Antivir Ther. 2003;8:173-182.
34. 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. Antivir Ther. 2003;8:S151.
35. Garcia-Lerma JG, Gerrish PJ, Wright AC, et al. Evidence of a role for the Q151L mutation and the viral background in development of multiple dideoxynucleoside- resistant human immunodeficiency virus type 1. J Virol. 2000;74:9339-9346.
36. Miller V, Ait-Khaled M, Stone C, et al. HIV-1 reverse transcriptase (RT) genotype and susceptibility to RT inhibitors during abacavir monotherapy and combination therapy. AIDS. 2000;14:163-171.
37. Larder BA, Bloor S, Kemp SD, et al. A family of insertion mutations between codons 67 and 70 of human immunodeficiency virus type 1 reverse transcriptase confer multinucleoside analog resistance. Antimicrob Agents Chemother. 1999;43:1961-1967.
38. Wolf K, Walter H, Schnell T, et al. The drug resistance profile of tenofovir: a story of resistance and resensitization. Antivir Ther. 2002;7:S22.
39. Louie M, Hogan C, Hurley A, et al. Determining the antiviral activity of tenofovir disoproxil fumarate in treatment-naive chronically HIV-1-infected individuals. AIDS. 2003;17:1151-1156.
40. Miller MD, Margot NA, McColl DJ, et al. Genotypic and phenotypic characterization of virologic failure through 48 weeks among treatment-naive patients taking tenofovir DF or stavudine in combination with lamivudine and efavirenz. Paper presented at: VI International Congress on Drug Therapy in HIV Infection; November 17-21, 2002; Glasgow.
41. Bazmi HZ, Hammond JL, Cavalcanti SCH, et al. In vitro selection of mutations in the human immunodeficiency virus type 1 reverse transcriptase that decrease susceptibility to (-)-beta-D-dioxolane-guanosine and suppress resistance to 3′-azido-3′-deoxythymidine. Antimicrob Agents Chemother, 2000;44:1783-1788.
42. Ait-Khaled M, Lanier R, Richards N, et al. Zidovudine appears to prevent selection of K65R and L74V mutations normally selected by abacavir mono- or combination therapies not containing zidovudine. Antivir Ther. 2002;7:S141.
43. Diallo K, Marchand B, Wei X, et al. Diminished RNA primer usage associated with the L74V and M184V mutations in the reverse transcriptase of human immunodeficiency virus type 1 provides a possible mechanism for diminished viral replication capacity. J Virol. 2003;77:8621-8632.
44. Naeger LK, Margot NA, Miller MD. Increased drug susceptibility of HIV-1 reverse transcriptase mutants containing M184V and zidovudine-associated mutations: analysis of enzyme processivity, chain-terminator removal and viral replication. Antivir Ther. 2001;6:115-126.
45. Wei X, Liang C, Gotte M, et al. Negative effect of the M184V mutation in HIV-1 reverse transcriptase on initiation of viral DNA synthesis. Virology. 2003;311:202-212.
46. Gao H-Q, Boyer PL, Sarafianos SG, et al. The role of steric hindrance in 3TC resistance of human immunodeficiency virus type-1 reverse transcriptase. J Mol Biol. 2000;300:403-408.
47. Farthing C, Khanlou H, Yeh V. Early virologic failure in a pilot study evaluating the efficacy of abacavir, lamivudine and tenofovir in the treatment naive HIV-infected patients. Antivir Ther. 2003;8:S195.
48. Gallant JE, Rodriguez A, Weinberg W, et al. Early non-response to tenofovir DF (TDF) + abacavir (ABC) and lamivudine (3TC) in a randomized trial compared to Efavirenz (EFV) + ABC and 3TC: ESS30009 unplanned interim analysis. Paper presented at: 43rd Interscience Conference on Antimocrobial Agents and Chemotherapy; September 14-17, 2003; Chicago.
49. Gerstoft J, Kirk O, Obel N, et al. Low efficacy and high frequency of adverse events in a randomized trial of the triple nucleoside regimen abacavir, stavudine and didanosine. AIDS. 2003;17:2045-2052.
50. Yeni PG, Hammer SM, Carpenter CCJ, et al. Antiretroviral treatment for adult HIV infection in 2002: updated recommendations of the International AIDS Society-USA Panel. JAMA. 2002;288:222-235.