Literature DB >> 19496631

Raltegravir: a review of its use in the management of HIV infection in treatment-experienced patients.

Jamie D Croxtall1, Susan J Keam.   

Abstract

Raltegravir (Isentress), an integrase inhibitor, inhibits the insertion of HIV-1 complementary DNA into the host genome. It is indicated in combination with other antiretroviral therapy (ART) agents for the treatment of HIV-1 infection in treatment-experienced adult patients who have evidence of viral replication and HIV-1 strains resistant to multiple ART agents. It is the first of a new class of ART agents to be approved that, as a result of a different mechanism of action to other ART agents, has good activity against multidrug-resistant HIV-1 strains. In clinical trials in treatment-experienced patients with HIV-1 infection and evidence of viral replication, the addition of oral raltegravir to an optimized background therapy (OBT) regimen improved virological and immunological responses at 16 and 48 weeks to a greater extent than placebo plus OBT. Raltegravir therapy was generally well tolerated, with a similar incidence of mild to moderate adverse events in the treatment and placebo arms. The introduction of integrase inhibitors extends the options available for managing treatment-experienced patients with multiple-drug-resistant HIV-1 infection. Results to date suggest that the combination of raltegravir and OBT will be a valuable treatment option for this difficult-to-treat patient group.

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Year:  2009        PMID: 19496631     DOI: 10.2165/00003495-200969080-00007

Source DB:  PubMed          Journal:  Drugs        ISSN: 0012-6667            Impact factor:   9.546


  41 in total

1.  Selection of the Q148R integrase inhibitor resistance mutation in a failing raltegravir containing regimen.

Authors:  Bénédicte Roquebert; Laurent Blum; Gilles Collin; Florence Damond; Gilles Peytavin; Juliette Leleu; Sophie Matheron; Geneviève Chêne; Françoise Brun-Vézinet; Diane Descamps
Journal:  AIDS       Date:  2008-10-01       Impact factor: 4.177

Review 2.  The discovery of raltegravir, an integrase inhibitor for the treatment of HIV infection.

Authors:  Michael Rowley
Journal:  Prog Med Chem       Date:  2008

Review 3.  Integrase inhibitors to treat HIV/AIDS.

Authors:  Yves Pommier; Allison A Johnson; Christophe Marchand
Journal:  Nat Rev Drug Discov       Date:  2005-03       Impact factor: 84.694

4.  Safety, tolerability, and pharmacokinetics of raltegravir after single and multiple doses in healthy subjects.

Authors:  M Iwamoto; L A Wenning; A S Petry; M Laethem; M De Smet; J T Kost; S A Merschman; K M Strohmaier; S Ramael; K C Lasseter; J A Stone; K M Gottesdiener; J A Wagner
Journal:  Clin Pharmacol Ther       Date:  2007-08-22       Impact factor: 6.875

5.  Antiretroviral treatment of adult HIV infection: 2008 recommendations of the International AIDS Society-USA panel.

Authors:  Scott M Hammer; Joseph J Eron; Peter Reiss; Robert T Schooley; Melanie A Thompson; Sharon Walmsley; Pedro Cahn; Margaret A Fischl; Jose M Gatell; Martin S Hirsch; Donna M Jacobsen; Julio S G Montaner; Douglas D Richman; Patrick G Yeni; Paul A Volberding
Journal:  JAMA       Date:  2008-08-06       Impact factor: 56.272

6.  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.

Authors:  Martin Markowitz; Bach-Yen Nguyen; Eduardo Gotuzzo; Fernando Mendo; Winai Ratanasuwan; Colin Kovacs; Guillermo Prada; Javier O Morales-Ramirez; Clyde S Crumpacker; Robin D Isaacs; Lucinda R Gilde; Hong Wan; Michael D Miller; Larissa A Wenning; Hedy Teppler
Journal:  J Acquir Immune Defic Syndr       Date:  2007-10-01       Impact factor: 3.731

7.  Lack of a clinically important effect of moderate hepatic insufficiency and severe renal insufficiency on raltegravir pharmacokinetics.

Authors:  Marian Iwamoto; William D Hanley; Amelia S Petry; Evan J Friedman; James T Kost; Sheila A Breidinger; Kenneth C Lasseter; Richard Robson; Norman M Lunde; Larissa A Wenning; Julie A Stone; John A Wagner
Journal:  Antimicrob Agents Chemother       Date:  2009-02-17       Impact factor: 5.191

8.  Effect of rifampin, a potent inducer of drug-metabolizing enzymes, on the pharmacokinetics of raltegravir.

Authors:  Larissa A Wenning; William D Hanley; Diana M Brainard; Amelia S Petry; Kalyan Ghosh; Bo Jin; Eric Mangin; Thomas C Marbury; Jolene K Berg; Jeffrey A Chodakewitz; Julie A Stone; Keith M Gottesdiener; John A Wagner; Marian Iwamoto
Journal:  Antimicrob Agents Chemother       Date:  2009-05-11       Impact factor: 5.191

9.  Atazanavir modestly increases plasma levels of raltegravir in healthy subjects.

Authors:  Marian Iwamoto; Larissa A Wenning; Goutam C Mistry; Amelia S Petry; Sarah Y Liou; Kaylan Ghosh; Sheila Breidinger; Neal Azrolan; Maria J Gutierrez; William E Bridson; Julie A Stone; Keith M Gottesdiener; John A Wagner
Journal:  Clin Infect Dis       Date:  2008-07-01       Impact factor: 9.079

10.  Clade-specific HIV-1 integrase polymorphisms do not reduce raltegravir and elvitegravir phenotypic susceptibility.

Authors:  Kurt Van Baelen; Veerle Van Eygen; Evelien Rondelez; Lieven J Stuyver
Journal:  AIDS       Date:  2008-09-12       Impact factor: 4.177

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  14 in total

1.  Raltegravir, tenofovir, and emtricitabine in an HIV-infected patient with HCV chronic hepatitis, NNRTI intolerance and protease inhibitors-induced severe liver toxicity.

Authors:  F Ortu; L E Weimer; Marco Floridia; P E Manconi
Journal:  Eur J Med Res       Date:  2010-02-26       Impact factor: 2.175

Review 2.  Authentic HIV-1 integrase inhibitors.

Authors:  Chenzhong Liao; Christophe Marchand; Terrence R Burke; Yves Pommier; Marc C Nicklaus
Journal:  Future Med Chem       Date:  2010-07       Impact factor: 3.808

3.  Impact of Y143 HIV-1 integrase mutations on resistance to raltegravir in vitro and in vivo.

Authors:  Olivier Delelis; Sylvain Thierry; Frédéric Subra; Françoise Simon; Isabelle Malet; Chakib Alloui; Sophie Sayon; Vincent Calvez; Eric Deprez; Anne-Geneviève Marcelin; Luba Tchertanov; Jean-François Mouscadet
Journal:  Antimicrob Agents Chemother       Date:  2009-11-09       Impact factor: 5.191

4.  High concentration of raltegravir in semen of HIV-infected men: results from a substudy of the EASIER-ANRS 138 trial.

Authors:  Caroline Barau; Constance Delaugerre; Joséphine Braun; Nathalie de Castro; Valérie Furlan; Isabelle Charreau; Laurence Gérard; Caroline Lascoux-Combe; Jean-Michel Molina; Anne-Marie Taburet
Journal:  Antimicrob Agents Chemother       Date:  2009-12-07       Impact factor: 5.191

5.  Analytical and biological considerations in the measurement of cell-associated CCR5 and CXCR4 mRNA and protein.

Authors:  D E Campbell; J P Lai; N B Tustin; E Riedel; R Tustin; J Taylor; J Murray; S D Douglas
Journal:  Clin Vaccine Immunol       Date:  2010-05-12

Review 6.  Raltegravir: in treatment-naive patients with HIV-1 infection.

Authors:  Jamie D Croxtall; Lesley J Scott
Journal:  Drugs       Date:  2010-03-26       Impact factor: 9.546

Review 7.  Raltegravir Once-Daily Tablet: A Review in HIV-1 Infection.

Authors:  Emma D Deeks
Journal:  Drugs       Date:  2017-10       Impact factor: 9.546

Review 8.  Recent Advances in the Development of Integrase Inhibitors for HIV Treatment.

Authors:  Jay Trivedi; Dinesh Mahajan; Russell J Jaffe; Arpan Acharya; Debashis Mitra; Siddappa N Byrareddy
Journal:  Curr HIV/AIDS Rep       Date:  2020-02       Impact factor: 5.071

Review 9.  Raltegravir: molecular basis of its mechanism of action.

Authors:  Jean-Francois Mouscadet; Luba Tchertanov
Journal:  Eur J Med Res       Date:  2009-11-24       Impact factor: 2.175

Review 10.  Raltegravir: a review of its use in the management of HIV-1 infection in children and adolescents.

Authors:  Caroline M Perry
Journal:  Paediatr Drugs       Date:  2014-02       Impact factor: 3.930

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