MK-0518

Medical Advocates
Raltegravir (Isentress/MK-0518)

Journal Papers, Abstracts and
Commentaries

General Reports
Pharmacokinetics
Drug/Drug Interactions
Efficacy
Diagnostic/Monitoring
Resistance
Therapeutic Strategies

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Last Update: August 26, 2008

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General Reports

A WEEK IN REVIEW FEATURED REPORT
Raltegravir with optimized background therapy for resistant HIV-1 infection.
Steigbigel RT, Cooper DA, Kumar PN, et al
N Engl J Med. 2008 Jul 24;359(4):339-54.
Abstract
Raltegravir Thorough QT/QTc Study: A Single Supratherapeutic Dose of Raltegravir Does Not
Prolong the QTcF Interval.
Iwamoto M, Kost JT, Mistry GC, et al
J Clin Pharmacol. 2008 Apr 25
Abstract
A WEEK IN REVIEW FEATURED REPORT
Raltegravir: an integrase inhibitor for HIV-1.
Evering TH, Markowitz M.
Expert Opin Investig Drugs. 2008 Mar;17(3):413-22.
Abstract
Antiretroviral therapy with the integrase inhibitor raltegravir alters decay kinetics of HIV,
significantly reducing the second phase.
Murray JM, Emery S, Kelleher AD, et al
AIDS. 2007 Nov 12;21(17):2315-21.
Abstract
Raltegravir (MK-0518): a novel integrase inhibitor for the treatment of HIV infection.
Anker M, Corales RB.
Expert Opin Investig Drugs. 2008 Jan;17(1):97-103.
Abstract

A WEEK-IN-REVIEW FEATURED REPORT
Metabolism and Disposition in Humans of Raltegravir (MK-0518), an Anti-AIDS Drug Targeting
the HIV-1 Integrase Enzyme.
Kassahun K, McIntosh I, Cui D, et al
Drug Metab Dispos. 2007 Jun 25;
Abstract

Pharmacokinetics

A WEEK-IN-REVIEW FEATURED REPORT
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.
Markowitz M, Morales-Ramirez JO, Nguyen BY, et al
J Acquir Immune Defic Syndr. 2006 Dec 15;43(5):509-515.|
Abstract

Drug/Drug Interactions

Lack of a significant drug interaction between raltegravir and tenofovir.
Wenning LA, Friedman EJ, Kost JT, et al
Antimicrob Agents Chemother. 2008 Jul 14.
Abstract

Atazanavir modestly increases plasma levels of raltegravir in healthy subjects.
Iwamoto M, Wenning LA, Mistry GC, et al
Clin Infect Dis. 2008 Jul 1;47(1):137-40
Abstract

Efficacy

A WEEK-IN-REVIEW FEATURED REPORT
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, et al
J Acquir Immune Defic Syndr. 2007 Aug 23
Abstract
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.
Grinsztejn B, Nguyen BY, Katlama C, et al
Lancet. 2007 Apr 14;369(9569):1261-9.
Abstract

Diagnostics/Monitoring

A sensitive HPLC-MS-MS method for the determination of raltegravir in human plasma.
Long MC, Bennetto-Hood C, Acosta EP.
J Chromatogr B Analyt Technol Biomed Life Sci. 2008 Apr 1
Abstract
Quantification of the HIV-integrase inhibitor raltegravir (MK-0518) in human plasma by
high-performance liquid chromatography with fluorescence detection.
Poirier JM, Robidou P, Jaillon P.
J Chromatogr B Analyt Technol Biomed Life Sci. 2008 Apr 4
Abstract
Determination of the HIV integrase inhibitor, MK-0518 (raltegravir), in human plasma using
96-well liquid-liquid extraction and HPLC-MS/MS.
Merschman SA, Vallano PT, Wenning LA, et al
J Chromatogr B Analyt Technol Biomed Life Sci. 2007 Jul 5;
Abstract

Resistance

A WEEK IN REVIEW FEATURED REPORT
Comparison of Raltegravir and Elvitegravir on HIV-1 Integrase Catalytic Reactions and on a Series of Drug-Resistant Integrase Mutants.
Marinello J, Marchand C, Mott BT, et al
Biochemistry. 2008 Aug 15.
Abstract

Genetic diversity of integrase (IN) sequences in antiretroviral treatment-naive and treatment-experienced HIV type 2 patients.
Xu L, Anderson J, Ferns B, et al
AIDS Res Hum Retroviruses. 2008 Jul;24(7):1003-7.
Abstract

Drug resistance profiles for the HIV integrase gene in patients failing raltegravir salvage therapy.
Charpentier C, Karmochkine M, Laureillard D, et al
HIV Med. 2008 Jul 21.
Abstract

Subgroup and resistance analyses of raltegravir for resistant HIV-1 infection.
Cooper DA, Steigbigel RT, Gatell JM, et al
N Engl J Med. 2008 Jul 24;359(4):355-65.
Abstract

A WEEK IN REVIEW FEATURED REPORT
Mutations Associated with Failure of Raltegravir Treatment affect integrase sensitivity to
the inhibitor in vitro.
Malet I, Delelis O, Valantin MA, et al
Antimicrob Agents Chemother. 2008 Jan 28
Abstract

Therapeutic Strategies

Outcomes of multidrug-resistant patients switched from enfuvirtide to raltegravir within a virologically suppressive
regimen.
Harris M, Larsen G, Montaner JS.
AIDS. 2008 Jun 19;22(10):1224-6.
Abstract

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