K65R-associated virologic failure in HIV-infected patients receiving tenofovir-containing triple nucleoside/nucleotide reverse transcriptase inhibitor regimens

MedGenMed Medscape General Medicine

Volumn 6, Issue 2, 2004, Pages

  Ruane, Peter J ^a   Luber, Andrew D ^a  

^a Tower ID Medical Associates ^*  (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ABACAVIR; ABACAVIR PLUS LAMIVUDINE PLUS ZIDOVUDINE; ANTIRETROVIRUS AGENT; DIDANOSINE; EFAVIRENZ; LAMIVUDINE; NEVIRAPINE; NUCLEOSIDE ANALOG; PROTEINASE INHIBITOR; RNA DIRECTED DNA POLYMERASE; RNA DIRECTED DNA POLYMERASE INHIBITOR; STAVUDINE; TENOFOVIR; TENOFOVIR DISOPROXIL; THYMIDINE DERIVATIVE; ZIDOVUDINE; 2',3' DIDEOXYNUCLEOSIDE DERIVATIVE; ADENINE; DRUG DERIVATIVE; PHOSPHONIC ACID DERIVATIVE;

CLINICAL TRIAL; DRUG ANTAGONISM; DRUG EFFICACY; DRUG EXPOSURE; DRUG HALF LIFE; DRUG POTENTIATION; DRUG SAFETY; DRUG TOLERABILITY; DRUG WITHDRAWAL; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; MONOTHERAPY; NONHUMAN; PROSPECTIVE STUDY; RANDOMIZATION; RETROSPECTIVE STUDY; REVIEW; TREATMENT FAILURE; TREATMENT OUTCOME; VIROLOGY; VIRUS LOAD; VIRUS MUTATION; ANTIBIOTIC RESISTANCE; DRUG INTERACTION; GENETICS; MUTATION;

ADENINE; CLINICAL TRIALS; DIDEOXYNUCLEOSIDES; DRUG INTERACTIONS; DRUG RESISTANCE, VIRAL; HIV INFECTIONS; HIV-1 REVERSE TRANSCRIPTASE; HUMANS; MUTATION; PHOSPHONIC ACIDS; PROSPECTIVE STUDIES; RETROSPECTIVE STUDIES; REVERSE TRANSCRIPTASE INHIBITORS; TREATMENT FAILURE;

EID: 23144467839     PISSN: None     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (32)

1. 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.
2. 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.
3. Gu Z, Gao Q, Fang H, et al. Identification of a mutation at codon 65 in the IKKK motif of reverse transcriptase that encodes human immunodeficiency virus resistance to 2′,3′-dideoxycytidine and 2′,3′-dideoxy-3′-thiacytidine. Antimicrob Agents Chemother. 1994;38:275-281.
4. Lanier ER, Irlbeck D, Ross L, et al. Prediction of NRTI options by linking reverse transcriptase genotype to phenotypic breakpoints. Program and abstracts of the 10th Conference on Retroviruses and Opportunistic Infections; February 10-14, 2003; Boston, Massachusetts. Abstract 586.
5. Parikh U, Koontz D, Hammond J, et al. K65R: a multi-nucleoside resistance mutation of low but increasing frequency. Program and abstracts of the 12th International HIV Drug Resistance Workshop; June 10-13, 2003; Los Cabos, Mexico. Abstract 136.
6. Schooley RT, Ruane P, Myers RA, et al; Study 902 Team. Tenofovir DF in antiretroviral-experienced patients: results from a 48-week, randomized, double-blind study. AIDS. 2002;16:1257-1263.
7. Squires K, Pozniak AL, Pierone G Jr, et al; Study 907 Team. Tenofovir disoproxil fumarate in nucleoside-resistant HIV-1 infection: a randomized trial. Ann Intern Med. 2003;139(5 Pt 1):313-320.
8. Miller MD, Margot N, McColl D, Coakley D, Cheng A. Characteristic of virologic failure through 96 weeks among treatment naive patients taking tenofovir DF (tenofovir) or stavudine (stavudine) in combination with lamivudine (lamivudine) and efavirenz (efavirenz). Program and abstracts of the 2nd International AIDS Society Conference on Pathogenesis and Treatment. July 13-16, 2003. Paris, France. Abstract 553.
9. Margot NA, Isaacson E, McGowan I, Cheng AK, Schooley RT, Miller MD. Genotypic and phenotypic analyses of HIV-1 in antiretroviral-experienced patients treated with tenofovir DF. AIDS. 2002;16:1227-1235.
10. Gallant J, Rodriguez A, Weinberg W, et al. Early non-response to tenofovir (tenofovir)+abacavir(abacavir) and lamivudine (lamivudine) in a randomized trial compared to efavirenz (efavirenz)+abacavir and lamivudine: ESS30009 unplanned interim analysis. Program and abstracts of the 43rd Annual ICAAC; September 14-17, 2003; Chicago, Illinois. Abstract H-1722a.
11. Farthing C, Khanlou H, Yeh V.. Early virologic failure in a pilot study evaluating the efficacy of once daily abacavir (abacavir), lamivudine (lamivudine) and tenofovir DF (tenofovir) in treatment naive HIV-infected patients. Program and abstracts of the 2nd International AIDS Society Conference on Pathogenesis and Treatment. July 13-16, 2003. Paris, France. Abstract 43.
12. Winston A, Pozniak A, Gazzard B, and Nelson M. Which nucleoside and nucleotide backbone combinations select for the K65R mutation in HIV-1 reverse transcriptase? Program and abstracts of the 12th International HIV Drug Resistance Workshop; June 10-13, 2003; Los Cabos, Mexico. Abstract 137.
13. Ruane P, Luber A, Akil B, et al. Factors influencing selection of K65R mutation among patients receiving tenofovir (tenofovir) containing regimens. Program and abstracts of the 2nd International AIDS Society Conference on Pathogenesis and Treatment. July 13-16, 2003. Paris, France. Abstract 582
14. MacArthur RD, Crane LR, Alvarez D, Fairfax M, Richmond D, Curtis G. Factors associated with selection of the K65R mutation: A retrospective chart review. Program and abstracts of the 2nd International AIDS Society Conference on Pathogenesis and Treatment. July 13-16, 2003. Paris, France. Abstract 835.
15. Dear Doctor Letter. Gilead Sciences; Foster City, California; October 14, 2003.
16. Kuritzkes DR, Quinn JB, Benoit SL, et al. Drug resistance and virologic response in NUCA 3001, a randomized trial of lamivudine (lamivudine) versus zidovudine (zidovudine) versus zidovudine plus lamivudine in previously untreated patients. AIDS. 1996;10:975-981.
17. Staszewski S, Keiser P, Montaner J, et al; CNAAB3005 International Study Team. Abacavir-lamivudine-zidovudine vs indinavir-lamivudine-zidovudine in antiretroviral-naive HIV-infected adults: A randomized equivalence trial. JAMA. 2001;285:1155-1163.
18. Whitcomb JM, Parkin NT, Chappey C, Hellmann NS, Petropoulos CJ. Broad nucleoside reverse-transcriptase inhibitor cross-resistance in human immunodeficiency virus type 1 clinical isolates. J Infect Dis. 2003;188:992-1000.
19. Mo, H, Lu L, Kempf D, Molla A. The impact of minor populations of wild-type HIV on the replication capacity and phenotype of mutant variants in a single-cycle HIV resistance assay. Program and abstracts of the 12th International HIV Drug Resistance Workshop; June 10-13, 2003; Los Cabos, Mexico. Abstract 85.
20. Rodriguez JF, Rodriguez JL, Santana J, Garcia H, Rosario O. Simultaneous Quantitation of Intracellular Zidovudine and Lamivudine Triphosphates in Human Immunodeficiency Virus-Infected Individuals Antimicrob. Agents Chemother. 2000;44:3097-3100.
21. Yuen G, Lou Y, Bumgarner NT, et al. Equivalence of plasma and intracellular triphosphate lamivudine pharmacokinetics (PK) following lamivudine (lamivudine) 300mg once daily compared to lamivudine 150mg twice a day in healthy volunteers. Program and abstracts of the 5th International Congress on Drug Therapy in HIV Infection. October 22-26, 2001. Glasgow, Scotland. Abstract 269.
22. Moore KHP, Barrett JE, Shaw S, et al. The pharmacokinetics of lamivudine phosphorylation in peripheral blood mononuclear cells from patients infected with HIV-1. AIDS. 1999;13:2239-2250.
23. Piliero P, Shachoy-Clark AD, Para M, et al. A study examining the pharmacokinetics of abacavir and the intracellular carbavir triphosphate (GSK protocol CAN 10905). Program and abstracts of the 43rd ICAAC. September 14-17, 2003. Chicago, Illinois. Abstract A-1797.
24. Harris M, Back D, Kewn S, Jutha S, Marina R, Montaner JS. Intracellular carbovir triphosphate levels in patients taking abacavir once a day. AIDS. 2002;16:1196-1197.
25. DeJesus E, Grinsztejn B, Gough K, et al. Comparable antiviral activity and safety of lamivudine administered 300mg once-daily (QD) versus 150mg BID both in combination with zidovudine (300mg BID) and efavirenz (600mg QD) in HIV-1 infected, antiretroviral naive adults: EPV20001. Program and abstracts of the 42nd ICAAC; September 27-30, 2002. San Diego, California. Abstract H-161.
26. Gazzard BG, DeJesus E, Cahn P, et al. Abacavir (ABC) once daily plus lamivudine (3TC) OAD in combination with efavirenz (EFV) OAD is well tolerated and effective in the treatment of antiretroviral therapy (ART)-naive adults with HIV-1 infection (ZODIAC Study: CNA30021). Program and abstracts of the 43rd ICAAC; September 14-17, 2003; Chicago, Illinois. Abstract H-1722b.
27. Kearney B, Isaacson E, Sayre J, et al. The pharmacokinetics of abacavir, a purine nucleoside analog, are not affected by tenofovir DF. Program and abstracts of the 43rd ICAAC. September 14-17, 2003. Chicago, Illinois. Abstract A-1615.
28. Kaye S, on behalf of the PENTA Virology Committee. Drug resistance in a trial of nucleoside-analog and protease inhibitor therapy in children (PENTA 5). Fifth International Congress on Drug Therapy in HIV Infection. AIDS. 2000;14(suppl 4). Abstract P354.
29. Selmi B, Boretto J, Sarfati SR, Guerreiro C, Canard B. Mechanism-based suppression of dideoxynucleotide resistance by K65R human immunodeficiency virus reverse transcriptase using an alpha-boranophosphate nucleoside analogue. J Biol Chem. 2001;276:48466-48472.
30. Meyer PR, Matsuura SE, Zonarich D, et al. Relationship between 3′-azido-3′-deoxythymidine resistance and primer unblocking activity in foscarnet-resistant mutants of human immunodeficiency virus type 1 reverse transcriptase. J Virol. 2003; 77:6127-6137.
31. Deval J, White KL, Miller MD, et al. Mechanistic basis for reduced viral and enzymatic fitness of HIV-1 reverse transcriptase containing both K65R and M184V mutations. J Biol Chem. 2004;279:509-516.
32. Garcýa-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.