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Volumn 10, Issue 2, 2009, Pages 190-200

Elvitegravir, an oral HIV integrase inhibitor, for the potential treatment of HIV infection

Author keywords

[No Author keywords available]

Indexed keywords

ABACAVIR; ALUMINUM MAGNESIUM HYDROXIDE; AMPRENAVIR PHOSPHATE; ATAZANAVIR; ATAZANAVIR PLUS RITONAVIR; DARUNAVIR PLUS RITONAVIR; DIDANOSINE; ELVITEGRAVIR; EMTRICITABINE PLUS TENOFOVIR DISOPROXIL; ENFUVIRTIDE; ETRAVIRINE; GLUCURONOSYLTRANSFERASE 1A1; GLUCURONOSYLTRANSFERASE 1A3; INTEGRASE INHIBITOR; LOPINAVIR PLUS RITONAVIR; MARAVIROC; N (4 FLUOROBENZYL) 8 HYDROXY 5 (TETRAHYDRO 2H 1,2 THIAZIN 2 YL) 1,6 NAPHTHYRIDINE 7 CARBOXAMIDE S,S DIOXIDE; OMEPRAZOLE; PLACEBO; RALTEGRAVIR; RIFABUTIN; RITONAVIR; RITONAVIR PLUS TIPRANAVIR; STAVUDINE; ZIDOVUDINE;

EID: 62249163679     PISSN: 14724472     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review
Times cited : (51)

References (46)
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    • 10 copies/ml, respectively). Pharmacokinetics were doseproportional, and increased exposure was observed when elvitegravir was coadministered with ritonavir. Elvitegravir was generally well tolerated, and exhibited a similar safety profile to placebo.
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    • 10 copies/ ml). Data from this trial were also presented at the International Conference on Retroviruses and Opportunistic Infections [958850].
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  • 29
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    • 958846 Safety and pharmacokinetics of single oral dose of JTK-303/ GS 9137, a novel HIV integrase inhibitor, in healthy volunteers. Kawaguchi I, Ishikawa T, Ishibashi M, Irie S, Kakee A INT CONF RETROVIRUSES OPPORTUNISTIC INFECT 2006 13 Abs 580
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    • 958847 Lack of clinically relevant drug interactions between ritonavir-boosted elvitegravir and TMC125. Ramanathan S, West S, Kakuda TN, Mack R, Holmes C, Kearney BP ICAAC 2007 47 September 17-20 Abs H-1049
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    • 958850 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 •• This abstract presented data from a phase II, 48-week clinical trial in HIV-1-infected, treatment-experienced patients (n, 278; HIV-1 RNA ≥ 1000 copies/ml) randomized to receive elvitegravir/ritonavir (20/100, 50/100 or 125/100 mg po, qd) or ritonavir-boosted comparator PI; both groups received optimized background therapy. At week 16, the elvitegravir/ritonavir (125/100 mg po, qd) arm demonstrated statistically greater reductions in HIV-1 RNA levels compared with the PI/ritonavir arm, 1.7 versus -1.2 log10 copies/ml; p, 0.01, similar data were observed at week 24, 1.7 versus -1.2 log 10 copies/ml; p, 0.02, Data from this trial were also pre
    • 10 copies/ml; p = 0.02). Data from this trial were also presented at the HIV Drug Resistance Workshop [939223].
  • 33
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    • 959012 Pharmacokinetic characterization of GS-9137 an HIV integrase inhibitor dosed with ritonavir. Mathias A, Jain A, Hui J, Shen G, Kearney B INT WORKSHOP CLIN PHARMACOL HIV THER 2006 7 Abs 75 •• This abstract describes the first clinical pharmacokinetic trial demonstrating the increased bioavailability and higher systemic exposure to elvitegravir when the drug was coadministered with ritonavir. Healthy volunteers (n, 12) received elvitegravir alone (100 mg po, bid for 10 days, followed by ritonavir-boosted elvitegravir 100/100 mg po, bid for 10 days, Steady-state elimination t1/2 values were increased from 3.5 to 9.5 h by coadministration of ritonavir. Furthermore, steady-state AUCτ, Cmax and Cτ values were increased by 19.9, 11.1- and 90-fold, respectively, and relative oral bioavailability was increased by 6- to 7-fold
    • τ values were increased by 19.9-, 11.1- and 90-fold, respectively, and relative oral bioavailability was increased by 6- to 7-fold.
  • 34
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    • 959013 Clinical pharmacokinetics of once-daily elvitegravir boosted by atazanavir versus ritonavir. Ramanthan S, West S, Hui J, Chuck SL, Kearney BP INT WORKSHOP CLIN PHARMACOL HIV THER 2008 9 Abs O18
    • 959013 Clinical pharmacokinetics of once-daily elvitegravir boosted by atazanavir versus ritonavir. Ramanthan S, West S, Hui J, Chuck SL, Kearney BP INT WORKSHOP CLIN PHARMACOL HIV THER 2008 9 Abs O18
  • 35
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    • 959015 Lack of clinically relevant drug-drug interaction between ritonavir-boosted GS-9137 (elvitegravir) and fosamprenavir/r. Ramanathan S, Mathias AA, Shen G, Holmes C, Kearney BP INT AIDS SOC CONF HIV PATHOGENESIS TREAT 2007 4 Abs WEPEB014
    • 959015 Lack of clinically relevant drug-drug interaction between ritonavir-boosted GS-9137 (elvitegravir) and fosamprenavir/r. Ramanathan S, Mathias AA, Shen G, Holmes C, Kearney BP INT AIDS SOC CONF HIV PATHOGENESIS TREAT 2007 4 Abs WEPEB014
  • 36
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    • 959016 Pharmacokinetic interaction between elvitegravir/ritonavir and dose-adjusted rifabutin. German PI, West S, Hui J, Kearney BP INT WORKSHOP CLIN PHARMACOL HIV THER 2008 9 Abs P19
    • 959016 Pharmacokinetic interaction between elvitegravir/ritonavir and dose-adjusted rifabutin. German PI, West S, Hui J, Kearney BP INT WORKSHOP CLIN PHARMACOL HIV THER 2008 9 Abs P19
  • 37
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    • 959017 Pharmacokinetic evaluation of drug interactions with ritonavir-boosted HIV integrase inhibitor GS-9137 (elvitegravir) and acid reducing agents. Ramanathan S, Shen G, Hinkle J, Enejosa J, Kearney B INT WORKSHOP CLIN PHARMACOL HIV THER 2007 8 Abs 69
    • 959017 Pharmacokinetic evaluation of drug interactions with ritonavir-boosted HIV integrase inhibitor GS-9137 (elvitegravir) and acid reducing agents. Ramanathan S, Shen G, Hinkle J, Enejosa J, Kearney B INT WORKSHOP CLIN PHARMACOL HIV THER 2007 8 Abs 69
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    • 959018 The HIV integrase inhibitor GS-9137 (JTK-303) exhibits potent antiviral activity in treatment-naive and experienced patients. DeJesus E, Berger D, Markowitz M, Cohen C, Hawkins T, Ruane P, Elion R, Farthing C, Cheng A, Kearney B INT CONF RETROVIRUSES OPPORTUNISTIC INFECT 2006 13 Abs 160LB
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* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.