Dolutegravir: A review of its use in the management of HIV-1 infection in adolescents and adults

Drugs

Volumn 74, Issue 11, 2014, Pages 1241-1252

  McCormack, Paul L ^a  

^a ADIS INTERNATIONAL LIMITED   (New Zealand)

Author keywords

[No Author keywords available]

Indexed keywords

ABACAVIR PLUS LAMIVUDINE; ADEFOVIR; ANTICONVULSIVE AGENT; ANTIRETROVIRUS AGENT; ATAZANAVIR PLUS RITONAVIR; CIMETIDINE; COBICISTAT; DARUNAVIR PLUS RITONAVIR; DOFETILIDE; DOLUTEGRAVIR; EFAVIRENZ; EFAVIRENZ PLUS EMTRICITABINE PLUS TENOFOVIR DISOPROXIL; ELVITEGRAVIR; EMTRICITABINE PLUS TENOFOVIR DISOPROXIL; ETRAVIRINE; FOSAMPRENAVIR PLUS RITONAVIR; HERBACEOUS AGENT; INTEGRASE; LOPINAVIR PLUS RITONAVIR; METFORMIN; NEVIRAPINE; RALTEGRAVIR; RIBAVIRIN; RIFAMPICIN; RILPIVIRINE; RITONAVIR; RITONAVIR PLUS TIPRANAVIR; TRIMETHOPRIM; UNINDEXED DRUG; VIRUS RNA; FUSED HETEROCYCLIC RINGS; INTEGRASE INHIBITOR;

ADOLESCENT DISEASE; ADULT DISEASE; AREA UNDER THE CURVE; ARTHRALGIA; CEREBROVASCULAR ACCIDENT; COUGHING; DIARRHEA; DOSE RESPONSE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG CONTRAINDICATION; DRUG DISTRIBUTION; DRUG EFFECT; DRUG EFFICACY; DRUG ELIMINATION; DRUG HALF LIFE; DRUG HYPERSENSITIVITY; DRUG MECHANISM; DRUG METABOLISM; DRUG SAFETY; DRUG TOLERABILITY; DRUG WITHDRAWAL; FATIGUE; HEADACHE; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS 1; HUMAN IMMUNODEFICIENCY VIRUS 1 INFECTION; IC 50; INFLUENZA; INSOMNIA; KIDNEY FAILURE; LIVER DYSFUNCTION; MAXIMUM PLASMA CONCENTRATION; MENTAL DISEASE; NAUSEA; NEUROLOGIC DISEASE; NONHUMAN; PHASE 1 CLINICAL TRIAL (TOPIC); PHASE 2 CLINICAL TRIAL (TOPIC); PHASE 3 CLINICAL TRIAL (TOPIC); RASH; RECOMMENDED DRUG DOSE; REVIEW; RHINOPHARYNGITIS; TIME TO MAXIMUM PLASMA CONCENTRATION; UPPER ABDOMINAL PAIN; UPPER RESPIRATORY TRACT INFECTION; URINARY TRACT INFECTION; VIRUS INHIBITION; VIRUS MUTATION; VIRUS RESISTANCE; VOMITING; ADOLESCENT; ADULT; CLINICAL TRIAL (TOPIC); DISEASE MANAGEMENT; HIV INFECTIONS; PROCEDURES;

HUMAN IMMUNODEFICIENCY VIRUS 1;

ADOLESCENT; ADULT; CLINICAL TRIALS AS TOPIC; DISEASE MANAGEMENT; HETEROCYCLIC COMPOUNDS, 3-RING; HIV INFECTIONS; HIV INTEGRASE INHIBITORS; HIV-1; HUMANS;

EID: 84904740227     PISSN: 00126667     EISSN: 11791950     Source Type: Journal    
DOI: 10.1007/s40265-014-0256-y     Document Type: Review

References (53)

1. EACS: European AIDS Clinical Society. Guidelines version 7.0. 2013. http://www.eacsociety.org/Portals/0/Guidelines-Online-131014.pdf. Accessed 23 June 2014.
2. British HIV Association. British HIV Association guidelines for the treatment of HIV-1-positive adults with antiretroviral therapy 2012 (updated November 2013). 2013. http://www.bhiva.org/documents/Guidelines/Treatment/2012/ hiv1029-2.pdf. Accessed 23 June 2014.
3. World Health Organization. Consolidated guidelines on the use of antiretroviral drugs for treating and preventing HIV infection: recommendations for a public health approach. 2013. http://www.who.int/iris/bitstream/10665/ 85321/1/9789241505727-eng.pdf?ua=1. Accessed 12 May 2014.
4. National Institutes of Health: National Institute of Allergy and Infectious Diseases. Types of HIV/AIDS antiretroviral drugs. 2013. http://www.niaid.nih.gov/topics/HIVAIDS/Understanding/Treatment/pages/ arvdrugclasses.aspx. Accessed 23 June 2014.
5. Freed EO. HIV-1 replication. Somat Cell Mol Genet. 2001;26(1-6):13-33.
6. Pandey KK, Grandgenett DP. HIV-1 integrase strand transfer inhibitors: novel insights into their mechanism of action. Retrovirology. 2008;2:11-6.
7. European Medicines Agency. Isentress (raltegravir): summary of product characteristics. 2013. http://www.ema.europa.eu/docs/en-GB/document-library/ EPAR---Product-Information/human/000860/WC500037405.pdf. Accessed 23 June 2014.
8. European Medicines Agency. Vitekta (elvitegravir): summary of product characteristics. 2013. http://www.ema.europa.eu/docs/en-GB/document-library/ EPAR---Product-Information/human/002577/WC500155576.pdf. Accessed 23 June 2014.
9. 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.
10. European Medicines Agency. Tivicay (dolutegravir): summary of product characteristics. 2014. http://www.ema.europa.eu/docs/en-GB/document-library/ EPAR---Product-Information/human/002753/WC500160680.pdf. Accessed 23 June 2014.
11. 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.
12. Hare S, Smith SJ, Métifiot 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.
13. Underwood MR, Johns BA, Sato A, et al. The activity of the integrase inhibitor dolutegravir against HIV-1 variants isolated from raltegravir-treated adults. J Acquir Immune Defic Syndr. 2012;61(3):297-301.
14. 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):1811-5.
15. 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.
16. 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.
17. Saladini F, Meini G, Bianco C, et al. Prevalence of HIV-1 integrase mutations related to resistance to dolutegravir in raltegravir naïve and pretreated patients. Clin Microbiol Infect. 2012;18(10):E428-30.
18. Cahn P, Pozniak AL, Mingrone H, et al. Dolutegravir versus raltegravir in antiretroviral-experienced, integrase-inhibitor-naive adults with HIV: week 48 results from the randomised, double-blind, non-inferiority SAILING study. Lancet. 2013;382(9893):700-8.
19. Raffi F, Jaeger H, Quiros-Roldan E, et al. Once-daily dolutegravir versus twice-daily raltegravir in antiretroviral-naive adults with HIV-1 infection (SPRING-2 study): 96 week results from a randomised, double-blind, non-inferiority trial. Lancet Infect Dis. 2013;13(11):927-35.
20. Raffi F, Rachlis A, Stellbrink H-J, et al. Once-daily dolutegravir versus raltegravir in antiretroviral-naive adults with HIV-1 infection: 48 week results from the randomised, double-blind, non-inferiority SPRING-2 study. Lancet. 2013;381(9868):735-43.
21. Stellbrink H-J, Reynes J, Lazzarin A, et al. Dolutegravir in antiretroviral-naive adults with HIV-1: 96-week results from a randomized dose-ranging study. AIDS. 2013;27(11):1771-8.
22. 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.
23. Walmsley SL, Antela A, Clumeck N, et al. Dolutegravir plus abacavir-lamivudine for the treatment of HIV-1 infection. N Engl J Med. 2013;369(19):1807-18.
24. Walmsley S, Berenguer J, Khuong-Josses M-A, et al. Dolutegravir regimen statistically superior to tenofovir/emtricitabine/efavirenz: 96-week data (abstract no. 543). Top Antivir Med. 2014;22(e-1):261-2.
25. Clotet B, Feinberg J, van Lunzen J, et al. Once-daily dolutegravir versus darunavir plus ritonavir in antiretroviral-naive adults with HIV-1 infection (FLAMINGO): 48 week results from the randomised open-label phase 3b study. Lancet. 2014. doi:10.1016/S0140-6736(14)60084-2.
26. Eron JJ, Clotet B, Durant J, et al. Safety and efficacy of dolutegravir in treatment-experienced subjects with raltegravir-resistant HIV type 1 infection: 24-week results of the VIKING Study. J Infect Dis. 2013;207(5):740-8.
27. Castagna A, Maggiolo F, Penco G, et al. Dolutegravir in antiretroviral-experienced patients with raltegravir- and/or elvitegravir-resistant HIV-1: 24-week results of the phase III VIKING-3 study. J Infect Dis. 2014. doi:10.1093/infdis/jiu051.
28. Canducci F, Ceresola ER, Saita D, et al. In vitro phenotypes to elvitegravir and dolutegravir in primary macrophages and lymphocytes of clonal recombinant viral variants selected in patients failing raltegravir. J Antimicrob Chemother. 2013;68(11):2525-32.
29. Huang W, Frantzell A, Whitcomb JM, et al. Impact of raltegravir/ elvitegravir selected mutations on dolutegravir cross-resistance (abstract no. 595). Top Antivir Med. 2014;22(e-1):292-3.
30. Quashie PK, Mesplède T, Han Y-S, et al. Characterization of the R263K mutation in HIV-1 integrase that confers low-level resistance to the second-generation integrase strand transfer inhibitor dolutegravir. J Virol. 2012;86(5):2696-705.
31. Mesplède T, Quashie PK, Osman N, et al. Viral fitness cost prevents HIV-1 from evading dolutegravir drug pressure. Retrovirology. 2013;10:22.
32. Vavro C, Hasan S, Madsen H, et al. Prevalent polymorphisms in wild-type HIV-1 integrase are unlikely to engender drug resistance to dolutegravir (S/GSK1349572). Antimicrob Agents Chemother. 2013;57(3):1379-84.
33. Chen S, Min SS, Peppercorn A, et al. Effect of a single supratherapeutic dose of dolutegravir on cardiac repolarization. Pharmacotherapy. 2012;32(4):333-9.
34. Rhodes M, Laffan S, Genell C, et al. Assessing a theoretical risk of dolutegravir-induced developmental immunotoxicity in juvenile rats. Toxicol Sci. 2012;130(1):70-81.
35. Koteff J, Borland J, Chen S, et al. A phase 1 study to evaluate the effect of dolutegravir on renal function via measurement of iohexol and para-aminohippurate clearance in healthy subjects. Br J Clin Pharmacol. 2013;75(4):990-6.
36. Greener BN, Patterson KB, Prince HMA, et al. Dolutegravir pharmacokinetics in the genital tract and colorectum of HIV-negative men after single and multiple dosing. J Acquir Immune Defic Syndr. 2013;64(1):39-44.
37. Adams JL, Patterson KB, Prince HM, et al. Single and multiple dose pharmacokinetics of dolutegravir in the genital tract of HIV-negative women. Antivir Ther. 2013;18(8):1005-13.
38. 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):54-8.
39. Song I, Borland J, Chen S, et al. Effect of food on the pharmacokinetics of the integrase inhibitor dolutegravir. Antimicrob Agents Chemother. 2012;56(3):1627-9.
40. Castellino S, Moss L, Wagner D, et al. Metabolism, excretion, and mass balance of the HIV-1 integrase inhibitor dolutegravir in humans. Antimicrob Agents Chemother. 2013;57(8):3536-46.
41. Reese MJ, Savina PM, Generaux GT, et al. In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor. Drug Metab Dispos. 2013;41(2):353-61.
42. Chen S, St Jean P, Borland J, et al. Evaluation of the effect of UGT1A1 polymorphisms on dolutegravir pharmacokinetics. Pharmacogenomics. 2014;15(1):9-16.
43. Weller S, Borland J, Chen S, et al. Pharmacokinetics of dolutegravir in HIV-seronegative subjects with severe renal impairment. Eur J Clin Pharmacol. 2014;70(1):29-35.
44. Song IH, Borland J, Savina PM, et al. Pharmacokinetics of single-dose dolutegravir in HIV-seronegative subjects with moderate hepatic impairment compared to healthy matched controls. Clin Pharmacol Drug Dev. 2013;2(4):342-8.
45. Cottrell ML, Hadzic T, Kashuba ADM. Clinical pharmacokinetic, pharmacodynamic and drug-interaction profile of the integrase inhibitor dolutegravir. Clin Pharmacokinet. 2013;52(11):981-94.
46. 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.
47. Dooley KE, Sayre P, Borland J, et al. Safety, tolerability, and pharmacokinetics of the HIV integrase inhibitor dolutegravir given twice daily with rifampin or once daily with rifabutin: results of a phase 1 study among healthy subjects. J Acquir Immune Defic Syndr. 2013;62(1):21-7.
48. Lepist E-I, Zhang X, Hao J, et al. Contribution of the organic anion transporter OAT2 to the renal active tubular secretion of creatinine and mechanism for serum creatinine elevations caused by cobicistat. Kidney Int. 2014. doi:10.1038/ki.2014.66.
49. Viani R, Alvero C, Fenton T, et al. Safety and efficacy of dolutegravir in HIV treatment-experienced adolescents: 48 week results (abstract no. 906LB). Top Antivir Med. 2014;22(e-1):474-5.
50. Vavro C, Huang J, Avatapally C, et al. Durable efficacy and limited integrase resistance in subjects receiving dolutegravir after failing a prior INI regimen: week 48 results from VIKING-3 (abstract no. O-10). Rev Antivir Ther Infect Dis. 2014;2:13.
51. US FDA. Tivicay (dolutegravir) tablets for oral use: US prescribing information. 2013. http://www.accessdata.fda.gov/drugsatfda-docs/label/2013/ 204790lbl.pdf. Accessed 23 June 2014.
52. ViiV Healthcare, Shionogi Co Ltd. Tivicay® tablets 50 mg, HIV integrase inhibitor obtains approval in Japan: new treatment option for treatment-naive patients and patients requiring alternative to current treatment regime (media release). 2014. http://www.shionogi.co.jp/en/company/news/2014/ pmrltj0000001ybwatt/e140324-1.pdf. Accessed 24 March 2014.
53. Johnson VA, Calvez V, Günthard HF, et al. Update of the drug resistance mutations in HIV-1: March 2013. Top Antivir Med. 2013;21(1):6-14.