Dolutegravir for the treatment of HIV

Expert Opinion on Investigational Drugs

Volumn 21, Issue 4, 2012, Pages 523-530

  Katlama, Christine ^a,b   Murphy, Robert ^a,b  

^a SORBONNE UNIVERSITÉ   (France)

^b NORTHWESTERN UNIVERSITY   (United States)

Author keywords

Dolutegravir; GSK1349572; HIV treatment; Integrase inhibitors

Indexed keywords

ABACAVIR PLUS LAMIVUDINE; ALUMINUM MAGNESIUM HYDROXIDE; ATAZANAVIR; ATAZANAVIR PLUS RITONAVIR; CREATININE; DARUNAVIR PLUS RITONAVIR; DOLUTEGRAVIR; EFAVIRENZ; EMTRICITABINE PLUS TENOFOVIR DISOPROXIL; ETRAVIRINE; FOSAMPRENAVIR PLUS RITONAVIR; INTEGRASE; LOPINAVIR PLUS RITONAVIR; OMEPRAZOLE; RALTEGRAVIR;

ABNORMAL DREAMING; ABSCESS; ANTIVIRAL ACTIVITY; AREA UNDER THE CURVE; ARTICLE; ASTHENIA; BRONCHITIS; BURKITT LYMPHOMA; CREATININE BLOOD LEVEL; DIARRHEA; DIZZINESS; DRUG ABSORPTION; DRUG EFFICACY; DRUG ELIMINATION; DRUG HALF LIFE; DRUG METABOLISM; DRUG SAFETY; DRUG TOLERABILITY; DRUG WITHDRAWAL; DYSMENORRHEA; EPIDIDYMITIS; FATIGUE; FEVER; FOOT FRACTURE; HEADACHE; HERPES ZOSTER; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTED PATIENT; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; INSOMNIA; JOINT DISLOCATION; MENTAL DISEASE; MUTATION; NAUSEA; NEUROSYPHILIS; PHASE 2 CLINICAL TRIAL (TOPIC); PHASE 3 CLINICAL TRIAL (TOPIC); RANDOMIZED CONTROLLED TRIAL (TOPIC); RASH; SIDE EFFECT; SUICIDE ATTEMPT; TRIACYLGLYCEROL BLOOD LEVEL; VIRUS RESISTANCE; WRIST FRACTURE;

ANTI-RETROVIRAL AGENTS; CLINICAL TRIALS AS TOPIC; DRUG RESISTANCE, VIRAL; HETEROCYCLIC COMPOUNDS, 3-RING; HIV INFECTIONS; HIV INTEGRASE; HIV INTEGRASE INHIBITORS; HUMANS; RANDOMIZED CONTROLLED TRIALS AS TOPIC;

EID: 84858236098     PISSN: 13543784     EISSN: 17447658     Source Type: Journal    
DOI: 10.1517/13543784.2012.661713     Document Type: Article

References (36)

1. Cohen MS, Chen YQ, McCauley M, et al. Prevention of HIV-1 infection with early antiretroviral therapy. N Engl J Med 2011;365(6):493-505
2. Hazuda DJ, Felock P, Witmer M, et al. Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells. Science 2000;287(5453):646-50 (Pubitemid 30070911)
3. Prada N, Markowitz M. Novel integrase inhibitors for HIV. Expert Opin Investig Drugs 2010;19:1087-98
4. DeJesus E, Berger D, Markowitz M, et al. Antiviral activity, pharmacokinetics, and dose response of the HIV-1 integrase inhibitor GS-9137 (JTK-303) in treatment-naive and treatment-experienced patients. J Acquir Immune Defic Syndr 2006;43(1):1-5 (Pubitemid 44306480)
5. Markowitz M, Morales-Ramirez JO, Nguyen BY, et al. Antiretroviral activity, pharmacokinetics, and tolerability of MK-0518, a novel inhibitor of HIV-1 integrase, dosed as monotherapy for 10 days in treatment-naive HIV-1-infected individuals. J Acquir Immune Defic Syndr 2006;43(5):509-15 (Pubitemid 44885615)
6. Grinsztejn B, Nguyen BY, Katlama C, et al. Safety and efficacy of the HIV-1 integrase inhibitor raltegravir (MK-0518) in treatment-experienced patients with multidrug-resistant virus: a phase II randomised controlled trial. Lancet 2007;369(9569):1261-9 (Pubitemid 46553846)
7. Steigbigel RT, Cooper DA, Kumar PN, et al. Raltegravir with optimized background therapy for resistant HIV-1 infection. N Engl J Med 2008;359(4):339-54
8. Markowitz M, Nguyen BY, Gotuzzo E, et al. Rapid and durable antiretroviral effect of the HIV-1 Integrase inhibitor raltegravir as part of combination therapy in treatment-naive patients with HIV-1 infection: results of a 48-week controlled study. J Acquir Immune Defic Syndr 2007;46(2):125-33 (Pubitemid 47482607)
9. Lennox JL, DeJesus E, Lazzarin A, et al. Safety and efficacy of raltegravir-based versus efavirenz-based combination therapy in treatment-naive patients with HIV-1 infection: a multicentre, double-blind randomised controlled trial. Lancet 2009;374(9692):796-806
10. Cooper DA, Steigbigel RT, Gatell JM, et al. Subgroup and resistance analyses of raltegravir for resistant HIV-1 infection. N Engl J Med 2008;359(4):355-65
11. Cohen C, Elion R, Ruane P, et al. Randomized, phase II evaluation of two single-tablet regimens elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate versus efavirenz/emtricitabine/tenofovir disoproxil fumarate for the initial treatment of HIV infection. AIDS 2011;25:F7-12
12. Katlama C, Murphy R. Emerging role of integrase inhibitors in the management of treatment-experienced patients with HIV infection. Ther Clin Risk Manag 2009;5(2):331-40
13. Lenz JC, Rockstroh JK. S/GSK1349572, a new integrase inhibitor for the treatment of HIV: promises and challenges. Expert Opin Investig Drugs 2011;20(4):537-48
14. Kobayashi M, Yoshinaga T, Seki T, et al. In vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. Antimicrob Agents Chemother 2011;55(2):813-21
15. Hare S, Smith SJ, Metifiot M, et al. Structural and functional analyses of the second-generation integrase strand transfer inhibitor dolutegravir (S/GSK1349572). Mol Pharmacol 2011;80(4):565-72
16. Underwood M, et al. S/GSK1265744: a next generation integrase inhibitor (INI) with activity against raltegravir-resistant clinical isolates. XVIII International AIDS Conference; 18-23 July 2010; Vienna, Austria
17. Min S, Song I, Borland J, et al. Pharmacokinetics and safety of S/GSK1349572, a next-generation HIV integrase inhibitor, in healthy volunteers. Antimicrob Agents Chemother 2010;54(1):254-8
18. Min S, Sloan L, DeJesus E, et al. Antiviral activity, safety, and pharmacokinetics/pharmacodynamics of dolutegravir as 10-day monotherapy in HIV-1-infected adults. AIDS 2011;25(14):1737-45
19. Song I, Min SS, Borland J, et al. Lack of interaction between the HIV integrase inhibitor S/GSK1349572 and tenofovir in healthy subjects. J Acquir Immune Defic Syndr 2010;55(3):365-7
20. Song I, Borland J, Chen S, et al. Effect of atazanavir and atazanavir/ritonavir on the pharmacokinetics of the next-generation HIV integrase inhibitor, S/GSK1349572. Br J Clin 2011;72(1):103-8
21. Song I, Min SS, Borland J, et al. The effect of lopinavir/ritonavir and darunavir/ritonavir on the HIV integrase inhibitor S/GSK1349572 in healthy participants. J Clin Pharmacol 2011;51(2):237-42
22. Song I, Borland J, Min S, et al. Effects of etravirine alone and with ritonavir-boosted protease inhibitors on the pharmacokinetics of dolutegravir. Antimicrob Agents Chemother 2011;55(7):3517-21
23. Patel P, Song I, Borland J, et al. Pharmacokinetics of the HIV integrase inhibitor S/GSK1349572 co-administered with acid-reducing agents and multivitamins in healthy volunteers. J Antimicrob Chemother 2011;66(7):1567-72
24. Lalezari J, Sloan L, Dejesus E, et al. Potent antiviral activity of S/GSK1349572, a next generation integrase inhibitor (INI), in INI-naive HIV-1-infected patients. Abstract TUAB105. Presented at: 5th IAS Conference on HIV Pathogenesis, Treatment and Prevention; 19-22 July 2009; Cape Town, South Africa
25. Eron J, Durant J, Poizot-Martin I, et al. Activity of next generation integrase inhibitor (INI) S/GSK1349572 in subjects with HIV exhibiting raltegravir resistance: initial results of VIKING study (ING112961) [abstract MOAB0105]. In: Abstracts of the Eighteenth International AIDS Conference; Vienna, Austria; 2010
26. Soriano V, Cox J, Eron J, et al. Dolutegravir (DTG, S/GSK1349572) treatment of subjects with raltegravir (RAL) resistance: viral suppression at week 24 in the VIKING Study [Number PS1/2]. 13th EACS; 12-15 October 2011; Belgrade, Serbia
27. Clotet B, Katlama C, Lalezari J, et al. HIV integrase resistance profiles and S/GSK1349572 baseline phenotypic susceptibility for subjects experiencing virologic failure on raltegravir (RAL) in the VIKING study (ING112961). Presented at: XVIII International HIV Drug Resistance Workshop; 8-12 June 2010; Dubrovnik, Croatia
28. van Lunzen J, Maggiolo F, Arribas JR, et al. Once daily dolutegravir (S/GSK1349572) in combination therapy in antiretroviral-naive adults with HIV: planned interim 48 week results from SPRING-1, a dose-ranging, randomised, phase 2b trial. Lancet Infect Dis 2012;12(2):111-8
29. Koteff J, Borland J, Chen S, et al. An Open Label, Placebo-Controlled Study to Evaluate the Effect of Dolutegravir (DTG, S/GSK1349572) on Iohexol and Para-Aminohippurate Clearance in Healthy Subjects [A1-1728]. 51st ICAAC; 17-20 September 2011; Chicago, IL, Poster
30. Seki T, Kobayashi M, Wakasa-Morimoto C, et al. S/GSK1349572 is a potent next generation HIV integrase inhibitor and demonstrates a superior resistance profile substantiated with 60 integrase mutant molecular clones [abstract 555]. 17th Conference on Retroviruses and Opportunistic Infections. CROI; San Francisco; 2010
31. Sato A, Kobayashi1 M, Seki T, et al. S/GSK1349572: a next generation integrase inhibitor (INI) with limited or no-cross resistance to first generation INIs or other classes of anti-virals. 8th European HIV drug Resistance Workshop; Sorrento Italy; 2010
32. Hightower KE, Wang R, Deanda F, et al. Dolutegravir (S/GSK1349572) exhibits significantly slower dissociation than raltegravir and elvitegravir from wild-type and integrase inhibitor-resistant HIV-1 integrase-DNA complexes. Antimicrob Agents Chemother 2011;55(10):4552-9
33. Eron J, Kumar P, Lazzarin A, et al. DTG in Subjects with HIV exhibiting ral resistance: functional monotherapy results of VIKING Study cohort II [abstract 151LB]. 18th Conference on Retroviruses and Opportunistic Infections. 2011 CROI; Boston
34. Canducci F, Ceresola ER, Boeri E, et al. Cross-resistance profile of the novel integrase inhibitor Dolutegravir (S/GSK1349572) using clonal viral variants selected in patients failing raltegravir. J Infect Dis 2011;204(11):1811-15
35. Malet I, Wirden M, Fourati S, et al. Prevalence of resistance mutations related to integrase inhibitor S/GSK1349572 in HIV-1 subtype B raltegravir-naive and-treated patients. J Antimicrob Chemother 2011;66(7):1481-3
36. Garrido C, Soriano V, Geretti AM, et al. Resistance associated mutations to dolutegravir (S/GSK1349572) in HIV-infected patients-impact of HIV subtypes and prior raltegravir experience. Antiviral Res 2011;90(3):164-7