Prevalent polymorphisms in wild-type HIV-1 integrase are unlikely to engender drug resistance to dolutegravir (S/GSK1349572)

Antimicrobial Agents and Chemotherapy

Volumn 57, Issue 3, 2013, Pages 1379-1384

  Vavro, Cindy ^a   Hasan, Samiul ^b   Madsen, Heather ^a   Horton, Joseph ^a   Deanda, Felix ^a   Martin Carpenter, Louise ^c   Sato, Akihiko ^d   Cuffe, Robert ^c   Chen, Shuguang ^a   Underwood, Mark ^a   Nichols, Garrett ^a  

^a GLAXOSMITHKLINE   (United States)

^b GLAXOSMITHKLINE   (United Kingdom)

^c VIIV HEALTHCARE   (United States)

^d SHIONOGI AND CO LTD   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

DOLUTEGRAVIR; INTEGRASE; PLACEBO;

AMINO ACID SUBSTITUTION; ANTIVIRAL ACTIVITY; ARTICLE; CLINICAL ARTICLE; CONTROLLED STUDY; CROSS RESISTANCE; DISEASE PREDISPOSITION; DRUG STRUCTURE; GENETIC POLYMORPHISM; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS 1; HUMAN IMMUNODEFICIENCY VIRUS 1 INFECTION; IN VITRO STUDY; IN VIVO STUDY; MONOTHERAPY; NONHUMAN; PREVALENCE; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; SITE DIRECTED MUTAGENESIS; VIRUS REPLICATION;

AMINO ACID SEQUENCE; CONSERVED SEQUENCE; HETEROCYCLIC COMPOUNDS, 3-RING; HIV INFECTIONS; HIV INTEGRASE; HIV INTEGRASE INHIBITORS; HIV-1; HUMANS; MOLECULAR SEQUENCE DATA; MUTAGENESIS, SITE-DIRECTED; POLYMORPHISM, GENETIC; RANDOMIZED CONTROLLED TRIALS AS TOPIC;

EID: 84874100435     PISSN: 00664804     EISSN: 10986596     Source Type: Journal    
DOI: 10.1128/AAC.01791-12     Document Type: Article

References (26)

1. LaFemina RL, Schneider CL, Robbins HL, Callahan PL, LeGrow K, Roth E, Schleif WA, Emini EA. 1992. Requirement of active human immunodeficiency virus type 1 integrase enzyme for productive infection of human T-lymphoid cells. J. Virol. 66:7414 -7419.
2. Lu W, Salzwedel K, Wang D, Chakravarty S, Freed EO, Wild CT, Li F. 2011. A single polymorphism in HIV-1 subtype C SP1 is sufficient to confer natural resistance to the maturation inhibitor bevirimat. Antimicrob. Agents Chemother. 55:3324 -3329.
3. Ceccherini-Silberstein F, Malet I, D'Arrigo R, Antinori A, Marcelin AG, Perno CF. 2009. Characterization and structural analysis of HIV-1 integrase conservation. AIDS Rev. 11:17-29.
4. Lataillade M, Chiarella J, Kozal MJ. 2007. Natural polymorphism of the HIV-1 integrase gene and mutations associated with integrase inhibitor resistance. Antivir. Ther. 12:563-570.
5. Myers RE, Pillay D. 2008. Analysis of natural sequence variation and covariation in human immunodeficiency virus type 1 integrase. J. Virol. 82:9228 -9235.
6. Rhee S-Y, Gonzales MJ, Kantor R, Betts BJ, Ravela J, Shafer RW. 2003. Human immunodeficiency virus reverse transcriptase and protease sequence database. Nucleic Acids Res. 31:298 -303.
7. Rhee S-Y, Liu TF, Kiuchi M, Zioni R, Gifford RJ, Holmes SP, Shafer RW. 2008. Natural variation of HIV-1 groupMintegrase: implications for a new class of antiretroviral inhibitors. Retrovirology 5:74.
8. Armenia D, Malet I, Fabeni L, Reigadas S, Guillot V, Dunn D, Kaiser R, Zazzi M, Van Laethem K, Artese A, Garrido C, Masquelier B, Garcia F, Calvez V, Antinori A, Marcelin AG, Perno CF, Geretti AM, Ceccherini- Silberstein F, on behalf of the CORONET Study Group and in collaboration with CHAIN. 2011. Impact of baseline HIV-1 integrase polymorphisms on virological outcome in a large European cohort of patients starting a raltegravir-containing regimen. Antivir. Ther. 16(Suppl 1): A69.
9. Marcelin AG, Delaugerre C, Flandre P, Descamps D, Morand-Joubert L, Amiel C, Ferre V, Izopet J, Masquelier B, Calvez V, the ANRS AC11 Resistance Group. 2011. Factors associated with virological response to raltegravir in experienced HIV-infected patients. Antivir. Ther. 16(Suppl 1): A74.
10. Powderly WG. 2010. Integrase inhibitors in the treatment of HIV-1 infection. J. Antimicrob. Chemother. 65:2485-2488.
11. Kobayashi M, Yoshinaga T, Seki T, Wakasa-Morimoto C, Brown KW, Ferris R, Foster SA, Hazen RJ, Miki S, Suyama-Kagitani A, Kawauchi- Miki S, Taishi T, Kawasuji T, Johns BA, Underwood MR, Garvey EP, Sato A, Fujiwara T. 2011. In vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. Antimicrob. Agents Chemother. 55:813- 821.
12. Sato A, Seki T, Kobayashi M, Yoshinaga T, Fujiwara T, Underwood M, Garvey E, Johns B. 2009. In vitro passage of drug resistant HIV-1 against a next generation integrase inhibitor (INI), S/GSK1349572. Abstr. 49th Intersci. Conf. Antimicrob. Agents Chemother., abstr H-932.
13. Seki T, Kobayashi M, Wakasa-Morimoto C, Yoshinaga T, Sato A, Fujiwara T, Underwood M, Garvey E, Johns B. 2010. S/GSK1349572 is a potent next generation HIV integrase inhibitor and demonstrates a superior resistance profile substantiated with 60 integrase mutant molecular clones. Abstr. 17th Conf. Retroviruses Opportunistic Infect., abstr 555.
14. Min S, Sloan L, DeJesus E, Hawkins T, McCurdy L, Song I, Stroder R, Chen S, Underwood M, Fujiwara T, Piscitelli S, Lalezari J. 2011. Antiviral activity, safety, and pharmacokinetics/pharmacodynamics of dolutegravir as 10-day monotherapy in HIV-1-infected adults. AIDS 25: 1737-1745.
15. Shafer RW. 2006. Rationale and uses of a public HIV drug-resistance database. J. Infect. Dis. 194(Suppl 1):S51-S58.
16. Edgar RC. 2004. MUSCLE: a multiple sequence alignment method with reduced time and space complexity. BMC Bioinformatics 5:113.
17. Nakahara K, Wakasa-Morimoto C, Kobayashi M, Miki S, Noshi T, Seki T, Kanamori-Koyama M, Kawauchi S, Suyama A, Fujishita T, Yoshinaga T, Garvey EP, Johns BA, Foster SA, Underwood MR, Sato A, Fujiwara T. 2009. Secondary mutations in viruses resistant to HIV-1 integrase inhibitors that restore viral infectivity and replication kinetics. Antiviral Res. 81:141-146.
18. Fransen S, Gupta S, Danovich R, Hazuda D, Miller M, Witmer M, Petropoulos CJ, Huang W. 2009. Loss of raltegravir susceptibility by human immunodeficiency virus type 1 is conferred via multiple nonoverlapping genetic pathways. J. Virol. 83:11440 -11446.
19. Cooper DA, Steigbigel RT, Gatell JM, Rockstroh JK, Katlama C, Yeni P, Lazzarin A, Clotet B, Kumar PN, Eron JE, Schechter M, Markowitz M, Loutfy MR, Lennox JL, Zhao J, Chen J, Ryan DM, Rhodes RR, Killar JA, Gilde LR, Strohmaier KM, Meibohm AR, Miller MD, Hazuda DJ, Nessly ML, DiNubile MJ, Isaacs RD, Teppler H, Nguyen B-Y. 2008. Subgroup and resistance analyses of raltegravir for resistant HIV-1 infection. N. Engl. J. Med. 359:355-365.
20. van Lunzen J, Maggiolo F, Arribas JR, Rakhmanova A, Yeni P, Young B, Rockstroh JK, Almond S, Song I, Brothers C, Min S. 2011. Once daily dolutegravir (S/GSK1349572) in combination therapy in antiretroviralnaive adults with HIV: planned interim 48 week results from SPRING-1, a dose-ranging, randomised, phase 2b trial. Lancet Infect. Dis. 12:111-118.
21. Varghese V, Liu TF, Rhee SY, Libiran P, Trevino C, Fessel WJ, Shafer RW. 2010. HIV-1 integrase sequence variability in antiretroviral naïve patients and in triple-class experienced patients subsequently treated with raltegravir. AIDS Res. Hum. Retroviruses 26:1323-1326.
22. Marcelin A-G, Malet I, Fabeni L, Armenia D, Fourati S, Masquelier B, Katlama C, Perno CF, Calvez V, Ceccherini-Silberstein F. 2010. Resistance- associated mutations to integrase inhibitor S/GSK1349572 in HIV-1 integrase inhibitor-naive and raltegravir-experienced patients. Abstr. 17th Conf. Retroviruses Opportunistic Infect., abstr 554.
23. Métifiot M, Marchand C, Maddali K, Pommier Y. 2010. Resistance to integrase inhibitors. Viruses 2:1347-1366.
24. Saladini FP, Meini G, Bianco C, Monno L, Punzi G, Pecorari M, Borghi V, Di Pietro M, Filice G, Gismondo MR, Micheli V, Penco G, Carli T, De Luca A, Zazzi M, Collaborative Group ARCA. 2011. Prevalence of mutations related to possible resistance to dolutegravir in raltegravir naïve and pretreated patients. Abstr. 13th European AIDS Conf., abstr PE5.1/4.
25. Raffi F, Rachlis A, Stellbrink Hardy H-JWD, Torti C, Orkin C, Bloch M, Podzamczer D, Pokrovsky V, Almond S, Margolis D, Min S, the SPRING-2 Team. 2012. Once-daily dolutegravir (DTG; S/GSK1349572) is noninferior to raltegravir (RAL) in antiretroviral-naive adults: 48 week results from SPRING-2 (ING113086). Abstr. 14th Int. AIDS Conf., abstr THLBB04.
26. Walmsley S, Antela A, Clumeck N, Duiculescu D, Eberhard A, Gutiérrez F, Hocqueloux L, Maggiolo F, Sandkovsky U, Granier C, Wynne B, Pappa K. 2012. Dolutegravir (DTG; S/GSK1349572)+ abacavir/lamivudine once daily statistically superior to tenofovir/emtricitabine/efavirenz: 48-week results-SINGLE (ING114467). Abstr. 52nd Intersci. Conf. Antimicrob. Agents Chemother., abstr H-556b.