GSK-1349572, a novel integrase inhibitor for the treatment of HIV infection

Current Opinion in Investigational Drugs

Volumn 11, Issue 2, 2010, Pages 203-212

  Vandeckerckhove, Linos ^a  

^a GHENT UNIVERSITY   (Belgium)

Author keywords

[No Author keywords available]

Indexed keywords

ABACAVIR PLUS LAMIVUDINE; ALUMINUM MAGNESIUM HYDROXIDE; ANTACID AGENT; ATAZANAVIR; ATAZANAVIR PLUS RITONAVIR; DARUNAVIR PLUS RITONAVIR; EFAVIRENZ; ELVITEGRAVIR; EMTRICITABINE PLUS TENOFOVIR DISOPROXIL; ETRAVIRINE; GSK 1349572; INTEGRASE INHIBITOR; LOPINAVIR PLUS RITONAVIR; MOXIFLOXACIN; MULTIVITAMIN; RALTEGRAVIR; RITONAVIR; TENOFOVIR; UNCLASSIFIED DRUG;

ALANINE AMINOTRANSFERASE BLOOD LEVEL; ANTIVIRAL ACTIVITY; AREA UNDER THE CURVE; ASPARTATE AMINOTRANSFERASE BLOOD LEVEL; CHOLESTEROL BLOOD LEVEL; DIARRHEA; DIZZINESS; DRUG DOSE ESCALATION; DRUG HALF LIFE; DRUG METABOLISM; FATIGUE; HEADACHE; HEART VENTRICLE TACHYCARDIA; HIGHLY ACTIVE ANTIRETROVIRAL THERAPY; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; MAXIMUM PLASMA CONCENTRATION; MIGRAINE; NAUSEA; PRURITUS; REVIEW; SIDE EFFECT; SINGLE DRUG DOSE; SOMNOLENCE; SORE THROAT; TRIACYLGLYCEROL BLOOD LEVEL; TRIACYLGLYCEROL LIPASE BLOOD LEVEL; VIRAL RESPIRATORY TRACT INFECTION; VOMITING;

ADMINISTRATION, ORAL; CLINICAL TRIALS, PHASE I AS TOPIC; CLINICAL TRIALS, PHASE II AS TOPIC; DRUG ADMINISTRATION SCHEDULE; DRUG RESISTANCE, VIRAL; HIV INFECTIONS; HIV INTEGRASE INHIBITORS; HUMANS;

EID: 77649112672     PISSN: 14724472     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (64)

1. (-)-2′-Deoxy-3′-thiacytidine is a potent, highly selective inhibitor of human immunodefciency virus type 1 and type 2 replication in vitro. Coates JAV, Cammack N, Jenkinson HJ, Jowett AJ, Jowett MI, Pearson BA, Penn CR, Rouse PL, Viner KC, CAMERON JM ANTIMICROB AGENTS CHEMOTHER 1992 36 4 733-739
2. Styrylquinoline derivatives: A new class of potent HIV-1 integrase inhibitors that block HIV-1 replication in CEM cells. Mekouar K, Mouscadet J, Desmaele D, Subra F, Leh H, Savoure D, Auclair C, d'Angelo J J MED CHEM 1998 41 15 2846-2857
3. Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells. Hazuda DJ, Felock P, Witmer M, Wolfe A, Stillmock K, Grobler JA, Espeseth A, Gabryelski L, Schlief W, Blau C, Miller MD SCIENCE 2000 287 5453 646-650
4. Analysis of the three enzymatic activities of HIV-1 integrase in vitro using minigels for detection of the reaction products. Sayasith K, Sauve G, Yelle J ANAL BIOCHEM 1999 269 1 189-192
5. HIV-1 integrase inhibitors that compete with the target DNA substrate defne a unique strand transfer conformation for integrase. Espeseth AS, Felock P, Wolfe A, Witmer M, Grobler J, Anthony N, Egbertson M, Melamed JY, Young S, Hamill T, Cole JL et al PROC NATL ACAD SCI USA 2000 97 21 11244-11249
6. New class of HIV integrase inhibitors that block viral replication in cell culture. Pannecouque C, Pluymers W, van Maele B, Tetz V, Cherepanov P, De Clercq E, Witvrouw M, Debyser Z CURR BIOL 2002 12 14 1169-1177
7. Design and synthesis of 8-hydroxy-[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells. Zhuang L, Wai JS, Embrey MW, Fisher TE, Egbertson MS, Payne LS, Guare JP Jr, Vacca JP, Hazuda DJ, Felock PJ, Wolfe AL et al J MED CHEM 2003 46 4 453-456
8. Results announcement for the second quarter 2003. GlaxoSmithKline plc PRESS RELEASE 2003 July 23
9. Integrase inhibitors and cellular immunity suppress retroviral replication in rhesus macaques. Hazuda DJ, Young SD, Guare JP, Anthony NJ, Gomez RP, Wai JS, Vacca JP, Handt L, Motzel SL, Klein HJ, Dornadula G et al SCIENCE 2004 305 5683 528-532
10. Antiviral activity, pharmacokinetics, and dose response of the HIV-1 integrase inhibitor GS-9137 (JTK-303) in treatment-naive and treatment-experienced patients. DeJesus E, Berger D, Markowitz M, Cohen C, Hawkins T, Ruane P, Elion R, Farthing C, Zhong L, Cheng AK, McColl D et al JAIDS-J ACQUIR IMMUNE DEFIC SYNDR 2006 43 1 1-5
11. Diketo acid inhibitor mechanism and HIV-1 integrase: Implications for metal binding in the active site of phosphotransferase enzymes. Grobler JA, Stillmock K, Hu BH, Witmer M, Felock P, Espeseth AS, Wolfe A, Egbertson M, Bourgeois M, Melamed J, Wai JS et al PROC NATL ACAD SCI USA 2002 99 10 6661-6666
12. Shioniogi R&D presentation. Shionogi & Co Ltd COMPANY PRESENTATION 2008 March 18
13. HIV integrase inhibitors: From diketoacids to heterocyclic templates: A history of HIV integrase medicinal chemistry at Merck West Point and Merck Rome (IRBM). Egbertson MS CURR TOP MED CHEM 2007 7 13 1251-1272
14. 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. Markowitz M, Nguyen BY, Gotuzzo E, Mendo F, Ratanasuwan W, Kovacs C, Prada G, Morales-Ramirez JO, Crumpacker CS, Isaacs RD, Gilde LR et al JAIDS-J ACQUIR IMMUNE DEFIC SYNDR 2007 46 2 125-133
15. HIV-1 DNA integration: Mechanism of viral DNA cleavage and DNA strand transfer. Engelman A, Mizuuchi K, Craigie R CELL 1991 67 6 1211-1221
16. Results of BENCHMRK-1, a phase III study evaluating the effcacy and safety of MK-0518, a novel HIV-1 integrase inhibitor, in patients with triple-class resistant virus. Cooper D, Gatell J, Rockstroh J, Katlama C, Yeni P, Lazzarin A, Chen J, Isaacs R, Teppler H, Nguyen B INT CONF RETROVIRUSES OPPORTUNISTIC INFECT 2007 14 105aLB
17. Repair of gaps in retroviral DNA integration intermediates. Yoder KE, Bushman FD J VIROL 2000 74 23 11191-11200
18. The HIV integrase inhibitor GS-9137 demonstrates potent antiretroviral activity in treatment-experienced patients. Zolopa AR, Mullen M, Berger D, Ruane P, Hawkins T, Zhong L, Chuck S, Enejosa J, Kearney B, Cheng A INT CONF RETROVIRUSES OPPORTUNISTIC INFECT 2007 14 Abs 143LB
19. GSK and Pfzer to establish specialist HIV company. GlaxoSmithKline plc; Pfzer Inc PRESS RELEASE 2009 April 16
20. GSK and Pfzer innovative agreement creates specialist HIV company. laxoSmithKline plc; Pfzer Inc PRESS RELEASE 2009 April 16
21. ISENTRESS (raltegravir), from MSD, was as effective as efavirenz at suppressing HIV viral load and increasing CD4 cell counts in treatment-naïve patients up to 144 weeks when used in combination therapy. Merck & Co Inc PRESS RELEASE 2009 July 20
22. NCT00951015: A dose ranging trial of GSK1349572 and 2 NRTI in HIV-1 infected, therapy naive subjects (ING112276). CLINICALTRIALS.GOV 2009
23. Pharmacokinetics (PK) and safety in healthy and HIV-infected subjects and short-term antiviral effcacy of S/GSK1265744, a next generation once daily HIV integrase inhibitor. Min S, DeJesus E, McCurdy L et al ICAAC 2009 49 14 Abs H-1228
24. Meta-analysis of safety for short-term dosing of an HIV integrase inhibitor, S/GSK1349572, from seven clinical studies. Lou Y, Min S, Chen S, Song I, Borland J, Fujiwara T, Piscitelli S ICAAC 2009 49 12 Abs H-931
25. In vitro passage of drug resistant HIV-1 against a next generation integrase inhibitor (INI), S/GSK1349572. Sato A, Seki T, Kobayashi M, Yoshinaga T, Fujiwara T, Underwood M, Garvey E, Johns B ICAAC 2009 49 Abs H-932
26. Lack of interaction between the HIV integrase inhibitor, S/GSK1349572, and tenofovir disoproxil fumarate (TDF) in healthy subjects. Song I, Min S, Borland J, Lou Y, Chen S, Ishibashi T, Piscitelli S ICAAC 2009 49 Abs A1-1303
27. The effect of ritonavir-boosted protease inhibitors (PIs) on the HIV integrase inhibitor, S/GSK1349572, in healthy subjects. Song I, Min S, Borland J, Lou Y, Chen S, Ishibashi T, Piscitelli S ICAAC 2009 49 12 Abs A1-1304
28. Evaluation of antacid and multivitamin (MVI) effects on S/GSK1349572 pharmacokinetics (PK) in healthy subjects. Song I, Patel A, Min S, Lou Y, Chen S, Patel P, Wajima T, Piscitelli S ICAAC 2009 49 12 Abs A1-1305
29. European Union Commission approves expanded use of ISENTRESS (raltegravir), from MSD, in adult patients with HIV-1 infection. Merck Sharp & Dohme Ltd PRESS RELEASE 2009 September 15
30. Potent antiviral activity of S/GSK1349572, a next generation integrase inhibitor (INI), in INI-naive HIV-1 infected patients. Lalezari J, Sloan L, Dejesus E, Hawkins T, Mccurdy L, Song I, Borland J, Stroder R, Chen S, Lou Y, Underwood M et al INT AIDS SOC CONF HIV PATHOGENESIS TREAT 2009 5 19 Abs TUAB105
31. S/GSK1349572: A next generation integrase inhibitor with activity against integrase inhibitor-resistant clinical isolates from patients experiencing virologic failure while on raltegravir therapy. Underwood M, Johns B, Sato A, Fujiwara T, Spreen W INT AIDS SOC CONF HIV PATHOGENESIS TREAT 2009 5 Abs WEBEA098
32. Pharmacokinetic (PK) and pharmacodynamic (PD) relationship of S/GSK1349572, a next generation integrase inhibitor (INI), in HIV-1 infected patients. Song I, Chen S, Lou Y, Borland J, Fujiwara T, Piscitelli S, Min S INT AIDS SOC CONF HIV PATHOGENESIS TREAT 2009 5 Abs WEPEB250
33. S/GSK1349572 is a potent next generation HIV integrase inhibitor. Sato A, Kobayashi M, Yoshinaga T, Fujiwara T, Underwood M, Johns B, Foster S, Hazen R, Ferris R, Brown K, Garvey E INT AIDS SOC CONF HIV PATHOGENESIS TREAT 2009 5 Abs WEPEA097
34. Pharmacokinetics (PK) and safety in healthy subjects of S/GSK1349572, a next generation, once-daily HIV integrase inhibitor (INI). Min S, Song I, Borland J, Chen S, Lou Y, Fujiwara T, Piscitelli S INT AIDS SOC CONF HIV PATHOGENESIS TREAT 2009 5 Abs WEPEA099
35. Japan Tobacco Inc: Clinical development. Japan Tobacco Inc COMPANY WORLD WIDE WEB SITE 2009 February 09
36. Safety and effcacy of raltegravir-based versus efavirenz-based combination therapy in treatment-naive patients with HIV-1 infection: A multicentre, double-blind randomised controlled trial. Lennox JL, Dejesus E, Lazzarin A, Pollard RB, Madruga JVR, Berger DS, Zhao J, Xu X, Williams-Diaz A, Rodgers AJ, Barnard RJO et al LANCET 2009 374 9692 796-806
37. Gilead Sciences, Inc. Q3 2009 earnings call transcript. ilead Sciences Inc COMPANY PRESENTATION 2009 October 21
38. GSK and Pfzer launch specialist HIV company: ViiV Healthcare. ViiV Healthcare PRESS RELEASE 2009 November 03
39. Pharmacokinetics and safety of S/GSK1349572, a next generation HIV integrase inhibitor, in healthy volunteers. Min S, Song I, Borland J, Chen S, Lou Y, Fujiwara T, Piscitelli SC ANTIMICROB AGENTS CHEMOTHER 2010 54 1 254-258
40. Pneumocystis pneumonia - Los Angeles. Centers for Disease Control (CDC) MMWR MORB MORTAL WKLY REP 1981 30 21 250-252
41. Maintenance antiretroviral therapies in HIV infected subjects with undetectable plasma HIV RNA after triple-drug therapy. AIDS Clinical Trials Group Study 343 Team. Havlir DV, Marschner IC, Hirsch MS, Collier AC, Tebas P, Bassett RL, Ioannidis JPA, Holohan MK, Leavitt R, Boone G, Richman DD N ENGL J MED 1998 339 18 1261-1268
42. Integration of human immunodefciency virus type 1 DNA in vitro. Farnet CM, Haseltine WA PROC NATL ACAD SCI USA 1990 87 11 4164-4168
43. Cellular co-factors of HIV-1 integration. Van Maele B, Busschots K, Vandekerckhove L, Christ F, Debyser Z TRENDS BIOCHEM SCI 2006 31 2 98-105
44. Overexpression of the lens epithelium-derived growth factor/p75 integrase binding domain inhibits human immunodefciency virus replication. De Rijck J, Vandekerckhove L, Gijsbers R, Hombrouck A, Hendrix J, Vercammen J, Engelborghs Y, Christ F, Debyser Z J VIROL 2006 80 23 11498-11509
45. An essential role for LEDGF/p75 in HIV integration. Llano M, Saenz DT, Meehan A, Wongthida P, Peretz M, Walker WH, Teo WL, Poeschla EM SCIENCE 2006 314 5798 461-464
46. LEDGF/p75 is essential for nuclear and chromosomal targeting of HIV-1 integrase in human cells. Maertens G, Cherepanov P, Pluymers W, Busschots K, De Clercq E, Debyser Z, Engelborghs Y J BIOL CHEM 2003 278 35 33528-33539
47. LEDGF/p75 determines cellular traffcking of diverse lentiviral but not murine oncoretroviral integrase proteins and is a component of functional lentiviral preintegration complexes. Llano M, Vanegas M, Fregoso O, Saenz D, Chung S, Peretz M, Poeschla EM J VIROL 2004 78 17 9524-9537
48. Virus evolution reveals an exclusive role for LEDGF/ p75 in chromosomal tethering of HIV. Hombrouck A, De Rijck J, Hendrix J, Vandekerckhove L, Voet A, De Maeyer M, Witvrouw M, Engelborghs Y, Christ F, Gijsbers R, Debyser Z PLOS PATHOGENS (ONLINE) 2007 3 3 e47
49. Transient and stable knockdown of the integrase cofactor LEDGF/p75 reveals its role in the replication cycle of human immunodefciency virus. Vandekerckhove L, Christ F, Van Maele B, De Rijck J, Gijsbers R, Van den Haute C, Witvrouw M, Debyser Z J VIROL 2006 80 4 1886-1896
50. A novel assay for the DNA strand-transfer reaction of HIV-1 integrase. Hazuda DJ, Hastings JC, Wolfe AL, Emini EA NUCLEIC ACIDS RES 1994 22 6 1121-1122
51. Structure-activity relationships and binding mode of styrylquinolines as potent inhibitors of HIV-1 integrase and replication of HIV-1 in cell culture. Zouhiri F, Mouscadet JF, Mekouar K, Desmaele D, Savoure D, Leh H, Subra F, Le Bret M, Auclair C, d'Angelo J J MED CHEM 2000 43 8 1533-1540
52. S-1360 Shionogi-GlaxoSmithKline. Billich A CURR OPIN INVESTIG DRUGS 2003 4 2 206-209
53. Towards universal access: Scaling up priority HIV/ AIDS interventions in the health sector. Progress report 2009. WHO INTERNET SITE 2009 1-164
54. Panel on antiretroviral guidelines for adults and adolescents. Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents. Department of Health and Human Services US DEPARTMENT HEALTH HUM SERVICES 2009 December 01 1-161
55. Antiretroviral therapy and declining AIDS mortality in New York City. Wong T, Chiasson MA, Reggy A, Simonds RJ, Heffess J, Loo V J URBAN HEALTH 2000 77 3 492-500
56. Update of the drug resistance mutations in HIV-1. Johnson VA, Brun-Vezinet F, Clotet B, Gunthard HF, Kuritzkes DR, Pillay D, Schapiro JM, Richman DD TOP HIV MED 2008 16 5 138-145
57. L-743, 726 (DMP-266): A novel, highly potent nonnucleoside inhibitor of the human immunodefciency virus type 1 reverse transcriptase. Young SD, Britcher SF, Tran LO, Payne LS, Lumma WC, Lyle TA, Huff JR, Anderson PS, Olsen DB, Carroll SS, Pettibone DJ et al ANTIMICROB AGENTS CHEMOTHER 1995 39 12 2602-2605
58. Effective blocking of HIV-1 proteinase activity by characteristic inhibitors of aspartic proteinases. Richards AD, Roberts R, Dunn BM, Graves MC, Kay J FEBS LETT 1989 247 1 113-117
59. Characterization of mutant HIV-1 integrase carrying amino acid changes in the catalytic domain. Sayasith K, Sauve G, Yelle J MOL CELLS 2000 10 5 525-532
60. Pharmacokinetic evaluation of drug interactions with ritonavir-boosted HIV integrase inhibitor GS-9137 (elvitegravir) and acid reducing agents. Ramanathan S, Shen G, Hinkle J et al INT WORKSHOP CLIN PHARMACOL HIV THER 2007 8 Abs 69
61. Pharmacologic aspects of new antiretroviral drugs. Long MC, King JR, Acosta EP CURR HIV/AIDS REP 2009 6 1 43-50
62. AIDS epidemic update. UNAIDS COMPANY PUBLICATION 2009 November 1-100
63. Our pipeline. ViiV Healthcare COMPANY WORLD WIDE WEB SITE 2009 December 09
64. Profle and pipeline. ViiV Healthcare COMPANY WORLD WIDE WEB SITE 2009 December 14