-
2
-
-
78049451176
-
Simplification from protease inhibitors to once- Or twice-daily raltegravir: The ODIS trial
-
Vispo E, Barreiro P, Maida I, et al. Simplification from protease inhibitors to once- or twice-daily raltegravir: the ODIS trial. HIV Clin Trials 2010;11:197-204
-
(2010)
HIV Clin Trials
, vol.11
, pp. 197-204
-
-
Vispo, E.1
Barreiro, P.2
Maida, I.3
-
3
-
-
77957862994
-
Mutation Q95K enhances N155H-mediated integrase inhibitor resistance and improves viral replication capacity
-
Fun A, Van Baelen K, van Lelyveld SF, et al. Mutation Q95K enhances N155H-mediated integrase inhibitor resistance and improves viral replication capacity. J Antimicrob Chemother 2010;65:2300-4
-
(2010)
J Antimicrob Chemother
, vol.65
, pp. 2300-2304
-
-
Fun, A.1
Van Baelen, K.2
Van Lelyveld, S.F.3
-
6
-
-
78049293198
-
Pharmacokinetics and bioavailability of an integrase and novel pharmacoenhancer-containing single-tablet fixed-dose combination regimen for the treatment of HIV
-
German P, Warren D, West S, et al. Pharmacokinetics and bioavailability of an integrase and novel pharmacoenhancer-containing single-tablet fixed-dose combination regimen for the treatment of HIV. J Acquir Immune Defic Syndr 2010;55:323-9
-
(2010)
J Acquir Immune Defic Syndr
, vol.55
, pp. 323-329
-
-
German, P.1
Warren, D.2
West, S.3
-
8
-
-
0032601403
-
HIV-1 integrase: Structural organization, conformational changes, and catalysis
-
Asante-Appiah E, Skalka AM. HIV-1 integrase: structural organization, conformational changes, and catalysis. Adv Virus Res 1999;52:351-69
-
(1999)
Adv Virus Res
, vol.52
, pp. 351-369
-
-
Asante-Appiah, E.1
Skalka, A.M.2
-
11
-
-
33645285267
-
Retroviral DNA integration: Reaction pathway and critical intermediates
-
Li M, Mizuuchi M, Burke TR Jr, Craigie R. Retroviral DNA integration: reaction pathway and critical intermediates. EMBO J 2006;25:1295-304
-
(2006)
EMBO J
, vol.25
, pp. 1295-1304
-
-
Li, M.1
Mizuuchi, M.2
Burke Jr., T.R.3
Craigie, R.4
-
12
-
-
77955597658
-
Novel integrase inhibitors for HIV
-
Excellent review of available integrase inhibitors as well as those in clinical development
-
Prada N, Markowitz M. Novel integrase inhibitors for HIV. Expert Opin Investig Drugs 2010;19:1087-98 Excellent review of available integrase inhibitors as well as those in clinical development.
-
(2010)
Expert Opin Investig Drugs
, vol.19
, pp. 1087-1098
-
-
Prada, N.1
Markowitz, M.2
-
13
-
-
0034723439
-
Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells
-
DOI 10.1126/science.287.5453.646
-
Hazuda DJ, Felock P, Witmer M, et al. Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells. Science 2000;287:646-50 (Pubitemid 30070911)
-
(2000)
Science
, vol.287
, Issue.5453
, pp. 646-650
-
-
Hazuda, D.J.1
Felock, P.2
Witmer, M.3
Wolfe, A.4
Stillmock, K.5
Grobler, J.A.6
Espeseth, A.7
Gabryelski, L.8
Schleif, W.9
Blau, C.10
Miller, M.D.11
-
14
-
-
77956886199
-
Resistance to HIV-1 integrase inhibitors: A structural perspective
-
Detailed review of the pharmacologic mechanism of integrase inhibitors and resistance
-
Mouscadet JF, Delelis O, Marcelin AG, Tchertanov L. Resistance to HIV-1 integrase inhibitors: a structural perspective. Drug Resist Updat 2010;13:139-50 Detailed review of the pharmacologic mechanism of integrase inhibitors and resistance.
-
(2010)
Drug Resist Updat
, vol.13
, pp. 139-150
-
-
Mouscadet, J.F.1
Delelis, O.2
Marcelin, A.G.3
Tchertanov, L.4
-
15
-
-
33750532296
-
A platform for designing HIV integrase inhibitors. Part 2: A two-metal binding model as a potential mechanism of HIV integrase inhibitors
-
Kawasuji T, Fuji M, Yoshinaga T, et al. A platform for designing HIV integrase inhibitors. Part 2: a two-metal binding model as a potential mechanism of HIV integrase inhibitors. Bioorg Med Chem 2006;14:8420-9
-
(2006)
Bioorg Med Chem
, vol.14
, pp. 8420-8429
-
-
Kawasuji, T.1
Fuji, M.2
Yoshinaga, T.3
-
16
-
-
0041353616
-
Metal-dependent inhibition of HIV-1 integrase by beta-diketo acids and resistance of the soluble double-mutant (F185K/C280S)
-
DOI 10.1124/mol.64.3.600
-
Marchand C, Johnson AA, Karki RG, et al. Metal-dependent inhibition of HIV-1 integrase by beta-diketo acids and resistance of the soluble doublemutant (F185K/C280S). Mol Pharmacol 2003;64:600-9 (Pubitemid 37048563)
-
(2003)
Molecular Pharmacology
, vol.64
, Issue.3
, pp. 600-609
-
-
Marchand, C.1
Johnson, A.A.2
Karki, R.G.3
Pais, G.C.G.4
Zhang, X.5
Cowansage, K.6
Patel, T.A.7
Nicklaus, M.C.8
Burke Jr., T.R.9
Pommier, Y.10
-
17
-
-
12944270496
-
HIV-1 integrase inhibitors that compete with the target DNA substrate define a unique strand transfer conformation for integrase
-
Espeseth AS, Felock P, Wolfe A, et al. HIV-1 integrase inhibitors that compete with the target DNA substrate define a unique strand transfer conformation for integrase. Proc Natl Acad Sci USA 2000;97:11244-9
-
(2000)
Proc Natl Acad Sci USA
, vol.97
, pp. 11244-11249
-
-
Espeseth, A.S.1
Felock, P.2
Wolfe, A.3
-
18
-
-
73849124557
-
Pharmacokinetics and safety of S/GSK1349572, a next-generation HIV integrase inhibitor, in healthy volunteers
-
Thorough analysis of pharmacokinetics and safety in healthy adults
-
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;54:254-8 Thorough analysis of pharmacokinetics and safety in healthy adults.
-
(2010)
Antimicrob Agents Chemother
, vol.54
, pp. 254-258
-
-
Min, S.1
Song, I.2
Borland, J.3
-
19
-
-
79952690569
-
-
Pharmacokinetics (PK) and safety in healthy subjects of S/GSK1349572, a next generation, once-daily HIV integrase inhibitor (INI) [poster No. WEPEA099]
-
Min S, Song I, Borland J, et al. Pharmacokinetics (PK) and safety in healthy subjects of S/GSK1349572, a next generation, once-daily HIV integrase inhibitor (INI) [poster No. WEPEA099]. 5th IAS Conference on HIV Pathogenesis, Treatment and Prevention; 2009
-
5th IAS Conference on HIV Pathogenesis, Treatment and Prevention; 2009
-
-
Min, S.1
Song, I.2
Borland, J.3
-
20
-
-
79551709965
-
The effect of lopinavir/ritonavir and darunavir/ritonavir on the HIV integrase inhibitor S/GSK1349572 in healthy participants
-
published on 20 May 2010, doi:10.1177/0091270010371113
-
Song I, Min S, Borland J, et al. The effect of lopinavir/ritonavir and darunavir/ritonavir on the HIV integrase inhibitor S/GSK1349572 in healthy participants. J Clin Pharm 2010: published on 20 May 2010, doi:10.1177/ 0091270010371113
-
(2010)
J Clin Pharm
-
-
Song, I.1
Min, S.2
Borland, J.3
-
21
-
-
84855626860
-
-
Available from: Last accessed 15 October 2010
-
GSK1349572 Mass Balance Study. Available from: http://clinicaltrials.gov/ ct2/show/NCT00828763 [Last accessed 15 October 2010]
-
GSK1349572 Mass Balance Study
-
-
-
23
-
-
79952690265
-
S/GSK1349572, a next generation HIV integrase inhibitor, pharmacokinetics are not affected by omeprazole in healthy adults
-
abstract No. H-943
-
Patel P, Song I, Borland J, et al. S/GSK1349572, a next generation HIV integrase inhibitor, pharmacokinetics are not affected by omeprazole in healthy adults [abstract No. H-943]. 50th Interscience Conference on Antimicrobial Agents and Chemotherapy; 2010
-
50th Interscience Conference on Antimicrobial Agents and Chemotherapy; 2010
-
-
Patel, P.1
Song, I.2
Borland, J.3
-
24
-
-
79952645320
-
-
Effect of atazanavir and atazanavir/ritonavir on the pharmacokinetics of the next generation integrase inhibitor, S/GSK1349572 [poster no. 616]
-
Song I, Borland J, Chen S, et al. Effect of atazanavir and atazanavir/ritonavir on the pharmacokinetics of the next generation integrase inhibitor, S/GSK1349572 [poster no. 616]. 17th Conference on Retroviruses and Opportunistic Infections; 2010
-
17th Conference on Retroviruses and Opportunistic Infections; 2010
-
-
Song, I.1
Borland, J.2
Chen, S.3
-
25
-
-
78049297410
-
Lack of interaction between the HIV integrase inhibitor S/GSK1349572 and tenofovir in healthy subjects
-
published on 25 June 2010, doi: 10.1097/QAI.0b013e3181e67909
-
Song I, Min S, 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: published on 25 June 2010, doi: 10.1097/QAI. 0b013e3181e67909
-
(2010)
J Acquir Immune Defic Syndr
-
-
Song, I.1
Min, S.2
Borland, J.3
-
26
-
-
79952666825
-
The effect of etravirine anlone and with boosted protease inhibitors on the pharmacokinetics of the integrase inhibitor, S/GSK1349572
-
abstract No. 26
-
Song I, Min S, Borland J, et al. The effect of etravirine anlone and with boosted protease inhibitors on the pharmacokinetics of the integrase inhibitor, S/GSK1349572 [abstract No. 26]. 11th International Workshop on Clinical Pharmakology of HIV Therapy; 2010
-
11th International Workshop on Clinical Pharmakology of HIV Therapy; 2010
-
-
Song, I.1
Min, S.2
Borland, J.3
-
27
-
-
84855624594
-
-
Available from: [Last accessed 15 October 2010]
-
GSK1349572 drug interaction study with efavirenz. Available from: http://clinicaltrials.gov/ct2/show/NCT01098526 [Last accessed 15 October 2010]
-
GSK1349572 Drug Interaction Study with Efavirenz
-
-
-
30
-
-
79952634738
-
-
Activity of the next generation integrase inhibitor S/GSK1349572 and two first generation inhibitors across a broad panel of HIV subtype isolates in PBMCs and MDMs [poster No. MOPE0032]
-
Underwood M, Vavro C, Ptak R, et al. Activity of the next generation integrase inhibitor S/GSK1349572 and two first generation inhibitors across a broad panel of HIV subtype isolates in PBMCs and MDMs [poster No. MOPE0032]. 18th International AIDS Conference; 2010
-
18th International AIDS Conference; 2010
-
-
Underwood, M.1
Vavro, C.2
Ptak, R.3
-
33
-
-
79952677734
-
In vitro virology of S/GSK1349572, a next-generation HIV integrase inhibitor
-
Epub ahead of print
-
Kobayashi M, Yoshinaga T, Seki T, et al. In vitro virology of S/GSK1349572, a next-generation HIV integrase inhibitor. Antimicrob Agents Chemother 2010. [Epub ahead of print]
-
(2010)
Antimicrob Agents Chemother
-
-
Kobayashi, M.1
Yoshinaga, T.2
Seki, T.3
-
34
-
-
79952660263
-
-
S/GSK1349572: a next generation integrase inhibitor with activity against integrase inhibitor-resistant clinical isolates from patients experiencing virologic failure while on raltegravir therapy [poster No. WEPEA098]
-
Underwood M, Johns B, Sato A, et al. S/GSK1349572: a next generation integrase inhibitor with activity against integrase inhibitor-resistant clinical isolates from patients experiencing virologic failure while on raltegravir therapy [poster No. WEPEA098]. 5th IAS Conference on HIV Pathogenesis, Treatment and Prevention; 2009
-
5th IAS Conference on HIV Pathogenesis, Treatment and Prevention; 2009
-
-
Underwood, M.1
Johns, B.2
Sato, A.3
-
35
-
-
78349311194
-
In-vitro phenotypic susceptibility of HIV-2 clinical isolates to the integrase inhibitor S/GSK1349572
-
published on 4 September 2010, doi: 10.1097/QAD.0b013e32833f9e36
-
Charpentier C, Larrouy L, Collin G, et al. In-vitro phenotypic susceptibility of HIV-2 clinical isolates to the integrase inhibitor S/GSK1349572. AIDS 2010: published on 4 September 2010, doi: 10.1097/QAD.0b013e32833f9e36
-
(2010)
AIDS
-
-
Charpentier, C.1
Larrouy, L.2
Collin, G.3
-
36
-
-
70350166248
-
Potent antiviral activity of S/GSK1349572, a next generation integrase inhibitor (INI), in INI-naive HIV-1-infected patients
-
abstract No. TUAB105
-
Lalezari J, Sloan L, Dejesus E. Potent antiviral activity of S/GSK1349572, a next generation integrase inhibitor (INI), in INI-naive HIV-1-infected patients [abstract No. TUAB105]. 5th IAS Conference on HIV Pathogenesis, Treatment and Prevention; 2009
-
5th IAS Conference on HIV Pathogenesis, Treatment and Prevention; 2009
-
-
Lalezari, J.1
Sloan, L.2
Dejesus, E.3
-
37
-
-
84872056682
-
Pharmacokinetic (PK) and pharmacodynamic (PD) relationship of S/GSK1349572, a next generation integrase inhibitor (INI), in HIV-1 infected patients
-
abstract No. WEPEB250
-
Song I, Chen S, Lou Y, et al. Pharmacokinetic (PK) and pharmacodynamic (PD) relationship of S/GSK1349572, a next generation integrase inhibitor (INI), in HIV-1 infected patients [abstract No. WEPEB250]. 5th IAS Conference on HIV Pathogenesis, Treatment and Prevention; 2009
-
5th IAS Conference on HIV Pathogenesis, Treatment and Prevention; 2009
-
-
Song, I.1
Chen, S.2
Lou, Y.3
-
38
-
-
79959262516
-
Once-daily S/GSK1349572 as part of combination therapy in antiretroviral naive adults: Rapid and potent antiviral responses in the interim 16-week analysis from SPRING-1 (ING112276)
-
abstract No. THLBB205
-
Arribas J, Lazzarin A, Raffi F, et al. Once-daily S/GSK1349572 as part of combination therapy in antiretroviral naive adults: rapid and potent antiviral responses in the interim 16-week analysis from SPRING-1 (ING112276) [abstract No. THLBB205]. 18th International AIDS Conference; 2010
-
18th International AIDS Conference; 2010
-
-
Arribas, J.1
Lazzarin, A.2
Raffi, F.3
-
39
-
-
79952634113
-
Once-daily S/GSK1349572 combination therapy in antiretroviral-naive adults: Rapid and potent 24-week antiviral responses in SPRING-1 (ING112276)
-
Rockstroh J, Felizarta F, Maggiolo F, et al. Once-daily S/GSK1349572 combination therapy in antiretroviral-naive adults: rapid and potent 24-week antiviral responses in SPRING-1 (ING112276). J Int AIDS Soc 2010;13(Suppl 4):O50
-
(2010)
J Int AIDS Soc
, vol.13
, Issue.SUPPL. 4
-
-
Rockstroh, J.1
Felizarta, F.2
Maggiolo, F.3
-
40
-
-
79959249153
-
Activity of next generation integrase inhibitor (INI) S/GSK1349572 in subjects with HIV exhibiting raltegravir resistance: Initial results of VIKING study (ING112961)
-
abstract No. MOAB0105
-
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 No. MOAB0105]. 18th International AIDS Conference; 2010
-
18th International AIDS Conference; 2010
-
-
Eron, J.1
Durant, J.2
Poizot-Martin, I.3
-
41
-
-
79952653025
-
Activity of integrase inhibitor, S/GSK1349572 in subjects with HIV exhibiting raltegravir resistance: Week 24 results of VIKING study (ING112961)
-
Eron J, Livrozet JM, Morlat P, et al. Activity of integrase inhibitor, S/GSK1349572 in subjects with HIV exhibiting raltegravir resistance: week 24 results of VIKING study (ING112961). J Int AIDS Soc 2010;13(Suppl 4):O51
-
(2010)
J Int AIDS Soc
, vol.13
, Issue.SUPPL. 4
-
-
Eron, J.1
Livrozet, J.M.2
Morlat, P.3
-
42
-
-
79952668401
-
-
HIV integrase genotypic and phenotypic changes between day 1 and day 11 in subjects with raltegravir resistant HIV treated with S/GSK1349572: results of VIKING study [poster No. TUPE130]
-
Clotet B, DeJesus E, Lazzarin A, et al. HIV integrase genotypic and phenotypic changes between day 1 and day 11 in subjects with raltegravir resistant HIV treated with S/GSK1349572: results of VIKING study [poster No. TUPE130]. 18th International AIDS Conference; 2010
-
18th International AIDS Conference; 2010
-
-
Clotet, B.1
DeJesus, E.2
Lazzarin, A.3
-
43
-
-
79952638662
-
HIV integrase resistance profiles and S/GSK1349572 baseline phenotypic susceptibility for subjects experiencing virologic failure on raltegravir (RAL) in the VIKING study (ING112961)
-
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). International HIV and Hepatitis Drug Resistance Workshop; 8-12 June 2010; Dubrovnik Croatia
-
International HIV and Hepatitis Drug Resistance Workshop; 8-12 June 2010; Dubrovnik Croatia
-
-
Clotet, B.1
Katlama, C.2
Lalezari, J.3
-
44
-
-
79952681789
-
-
Meta-analysis of safety for short-term dosing of an HIV Integrase inhibitor, S/GSK1349572, from seven clinical studies [poster No. H-931]
-
Lou Y, Min S, Chen I, et al. Meta-analysis of safety for short-term dosing of an HIV Integrase inhibitor, S/GSK1349572, from seven clinical studies [poster No. H-931]. 49th Interscience Conference on Antimicrobial Agents and Chemotherapy; 2009
-
49th Interscience Conference on Antimicrobial Agents and Chemotherapy; 2009
-
-
Lou, Y.1
Min, S.2
Chen, I.3
-
47
-
-
84855639140
-
-
GSK press release issued 21 July 2009, Cape Town, South Africa. Available from: Last accessed 20 October 2010
-
GSK press release issued 21 July 2009, Cape Town, South Africa. Available from: http://www.gsk.com/media/pressreleases/2009/2009-pressrelease-10080.htm [Last accessed 20 October 2010]
-
-
-
-
48
-
-
84855639141
-
-
GSK press release issued 16 April 2009, London UK & Philadelphia, US. Available from: Last accessed 20 October 2010
-
GSK press release issued 16 April 2009, London UK & Philadelphia, US. Available from: http://www.gsk.com/media/pressreleases/2009/2009-pressrelease- 10041.htm [Last accessed 20 October 2010]
-
-
-
-
49
-
-
84855625720
-
-
ViiV Healthcare press release issued 22 July 2010, Vienna, Austria. Available from: Last accessed 20 October 2010
-
ViiV Healthcare press release issued 22 July 2010, Vienna, Austria. Available from: http://www.viivhealthcare.com/media-room/press-releases/2010-07- 22.aspx [Last accessed 20 October 2010]
-
-
-
-
50
-
-
70350666377
-
Loss of raltegravir susceptibility by human immunodeficiency virus type 1 is conferred via multiple nonoverlapping genetic pathways
-
Fransen S, Gupta S, Danovich R, et al. Loss of raltegravir susceptibility by human immunodeficiency virus type 1 is conferred via multiple nonoverlapping genetic pathways. J Virol 2009;83(22):11440-6
-
(2009)
J Virol
, vol.83
, Issue.22
, pp. 11440-11446
-
-
Fransen, S.1
Gupta, S.2
Danovich, R.3
-
51
-
-
62149093020
-
The G140S mutation in HIV integrases from raltegravir-resistant patients rescues catalytic defect due to the resistance Q148H mutation
-
Delelis O, Malet I, Na L, et al. The G140S mutation in HIV integrases from raltegravir-resistant patients rescues catalytic defect due to the resistance Q148H mutation. Nucleic Acids Res 2009;37(4):1193-201
-
(2009)
Nucleic Acids Res
, vol.37
, Issue.4
, pp. 1193-1201
-
-
Delelis, O.1
Malet, I.2
Na, L.3
|