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01.01.2008 | Adis Drug Profile

Raltegravir

verfasst von: Jamie D. Croxtall, Katherine A. Lyseng-Williamson, Caroline M. Perry

Erschienen in: Drugs | Ausgabe 1/2008

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Abstract

▲ Raltegravir, the first in a new class of orally administered HIV type-1 (HIV-1) integrase inhibitors, selectively inhibits the strand transfer activity of HIV-1 and its integration into human DNA, a key stage in retroviral propagation, thereby limiting viral replication and the infection of new cells.
▲ In two randomized, double-blind (with in-house blinding), placebo-controlled, multicentre, ongoing phase III trials, the proportion of patients achieving HIV-1 RNA loads of <400 copies/mL (primary endpoint) was significantly greater in raltegravir plus optimized background therapy (OBT) recipients than in placebo plus OBT recipients (preliminary 24-week results).
▲ The proportion of patients achieving viral loads of <50 copies/mL was significantly greater with raltegravir plus OBT than with placebo plus OBT in the two studies.
▲ In addition, mean CD4+ cell counts (secondary endpoint) were significantly increased from baseline in patients receiving raltegravir plus OBT relative to those receiving placebo plus OBT.
▲ Raltegravir therapy was well tolerated overall. The incidence of mild to moderate adverse events was similar in the raltegravir and placebo arms of the two randomized trials.

The use of trade names is for identification purposes only and does not imply endorsement.

UNAIDS WHO. AIDS epidemic update [online]. Available from URL: http://www.who.int/hiv/mediacentre/2006_Epi-Update_en.pdf [Accessed 2007 Oct 26]

Joint United Nations Programme on HIV/AIDS. 2006 report on the global AIDS epidemic [online]. Available from URL: http://www.unaids.org/en/HIV-data/epi2006/default.asp [Accessed 2007 Sep 19]

DHHS panel on antiretroviral guidelines for adults and adolescents: a working group of the Office of AIDS Research Advisory Council. Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents [online]. Available from URL: http://aidsinfo.nih.gov/contentfiles/AdultandAdolescentGL.pdf [Accessed 2007 Oct 26]

Gazzard B. British HIV Association (BHIVA) guidelines for the treatment of HIV-infected adults with antiretroviral therapy (2005). HIV Med 2005 Jul; 6 Suppl. 2: 1–61

Richman DD. HIV chemotherapy. Nature 2001; 410: 995–1001CrossRef

Pommier Y, Johnson AA, Marchand C. Integrase inhibitors to treat HIV/AIDS. Nat Rev Drug Discov 2005 Mar; 4(3): 236–48CrossRef

Isentress (Raltegravir): US prescribing information. Whitehouse Station (NJ): Merck and Co., Inc, 2007

Cooper D, Gatell J, Rockstroh J, et al. Results of BENCHMRK-1, a phase III study evaluating the efficacy and safety of MK-0518, a novel HIV-1 integrase inhibitor, in patients with triple-class resistant virus [abstract no. 105aLB]. 14th Conference on Retroviruses and Opportunistic Infections; 2007 Feb 25–28; Los Angeles (CA)

Steigbigel R, Kumar P, Eron J, et al. Results of BENCHMRK-2, a phase III study evaluating the efficacy and safety of MK-0518, a novel HIV-1 integrase inhibitor, in patients with triple-class resistant virus [abstract no. 105bLB]. 14th Conference on Retroviruses and Opportunistic Infections; 2007 Feb 25–28; Los Angeles (CA)

10.

Miller M, Witmer M, Stillmock K, et al. Biochemical and antiviral activity of MK-0518, a potent HIV integrase inhibitor [abstract no. 1045050]. 16th International AIDS Conference; 2006 Aug 13–18; Toronto (ON)

11.

Hazuda DJ, Miller MD, Nguyen BY. Resistance to the HIV-integrase inhibitor raltegravir: analysis of protocol 005, a phase II study in patients with triple-class resistant HIV-1 infection [abstract no. 8]. Antivi Ther 2007 June 12–16; 12 (5): S10

12.

Hazuda DJ, Felock P, Witmer M, et al. Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells. Science 2000 Jan 28; 287: 646–50CrossRef

13.

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 Apr 14; 369(9569): 1261–9CrossRef

14.

Teppler H, Azrolan N, Chen J, et al. Differential effect of MK-0518 and efavirenz on serum lipids and lipoproteins in antiretroviral therapy-naive patients [abstract no. H-256a]. 46th Interscience Conference on Antimicrobial Agents and Chemotherapy; 2006 Sep 27–30; San Francisco (CA), 183

15.

Wenning L, Anderson M, Petry A, et al. Raltegravir (RAL) dose proportionality and effect of food [abstract no. H-1046]. 47th Interscience Conference on Antimicrobial Agents and Chemotherapy; 2007 Sep 17–20; Chicago (IL)

16.

Kassahun K, McIntosh I, Cui D, et al. Metabolism and disposition in humans of raltegravir (MK-0518), an anti-AIDS drug targeting the HIV-1 integrase enzyme. Drug Metab Dispos 2007 Jun 25; 35(9): 1657–63CrossRef

17.

Mistry G, Wenning L, Petry A, et al. Atazanavir modestly increases plasma levels of MK-0518 [abstract no. MOPEB109]. 4th International AIDS Society Conference on HIV Pathogenesis, Treatment and Prevention; 2007 Jul 22–25; Sydney, 76

18.

Iwamoto M, Wenning LA, Petry AS, et al. Minimal effect of ritonavir and efavirenz on the pharmacokinetics of MK-0518 [abstract no. A-373]. 46th Interscience Conference on Antimicrobial Agents and Chemotherapy; 2006 Sep 27–30; San Francisco (CA), 7

19.

Iwamoto M, Wenning LA, Petry AS, et al. Safety, tolerability, and pharmacokinetics of raltegravir after single and multiple doses in healthy subjects. Clin Pharmacol Ther. Epub 2007 Aug 22

20.

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 Dec 15; 43(5): 509–15CrossRef

21.

Kassahun K, McIntosh I, Hreniuk D, et al. Absorption, metabolism and excretion of MK-0518, a potent HIV-1 integrase inhibitor, in healthy male volunteers [abstract no. A-372]. 46th Interscience Conference on Antimicrobial Agents and Chemotherapy; 2006 Sep 27–30; San Francisco (CA), 7

22.

The US National Institutes of Health. A study to evaluate the safety and efficacy of MK-0518 in HIV-infected patients failing current antiretroviral therapies [online]. Available from URL: http://clinicaltrials.gov/ct2/show/NCT002932547term=Raltegravir&rank=17 [Accessed 2007 Dec 11]

23.

Markowitz M, Nguyen B-Y, Gotuzzo E, et al. Rapid and durable antiretroviral effect of the HIV-1 integrase inhibitor raltegravir as part combination therapy in treatment-naive patients with HIV-1 infection. Acquir Immune Defic Syndr 2007; 46(2): 125–33CrossRef

24.

Kumar P, Cooper D, Steigbigel R, et al. Efficacy of raltegravir, an HIV integrase inhibitor, in combination with regimens containing enfuvirtide, darunavir, or tipranavir in patients with triple-class resistant virus: combined results from BENCHMRK-1 and BENCHMRK-2 [abstract no. P7.2/06]. 11th European AIDS Conference/EACS; 2007 October 24–27; Madrid

25.

Grinsztejn B, Nguyen B, Katlama C, et al. 48 Week efficacy and safety of MK-0518, a novel HIV-1 integrase inhibitor, in patients with triple-class resistant virus [abstract no. H-713]. 47th Interscience Conference on Antimicrobial Agents and Chemotherapy; 2007 Sep 17–20; Chicago (IL)

26.

National AIDS Treatment Advocacy Project. Merck updated data on malignancies-raltegravir [online]. Available from URL: http://www.natap.org/2007/HIV/091007_01.htm [Accessed 2007 Nov 13]

Titel: Raltegravir
verfasst von: Jamie D. Croxtall
Katherine A. Lyseng-Williamson
Caroline M. Perry
Publikationsdatum: 01.01.2008
Verlag: Springer International Publishing
Erschienen in: Drugs / Ausgabe 1/2008
Print ISSN: 0012-6667
Elektronische ISSN: 1179-1950
DOI: https://doi.org/10.2165/00003495-200868010-00009

Die Highlights vom Kongress des American College of Cardiology 2024

Springer Medizin

Raltegravir

Abstract

Die Highlights vom Kongress des American College of Cardiology 2024

Springer Medizin

Abstract

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