Raltegravir: an integrase inhibitor for HIV-1
- 6 March 2008
- journal article
- review article
- Published by Informa Healthcare in Expert Opinion on Investigational Drugs
- Vol. 17 (3) , 413-422
- https://doi.org/10.1517/13543784.17.3.413
Abstract
The need to develop antiretroviral agents with novel mechanisms of action persists for the treatment of both antiretroviral- experienced and antiretroviral-naive patients with HIV/AIDS. This is mandated, in part, by the perpetual advent of antiretroviral-resistant HIV-1 strains. Raltegravir has been shown to specifically inhibit the essential, HIV-1-encoded, integrase enzyme. As a result, this agent represents a promising chemotherapeutic agent for the treatment of HIV/AIDS. To form an evidence-based determination of the clinical efficacy, pharmacokinetics and safety profile of raltegravir. We discuss available peer-reviewed publications, preliminary data presented in abstract from relevant scientific meetings and data available from the US Food and Drug Administration (FDA). Current evidence strongly supports raltegravir use in highly active antiretroviral therapy (HAART) regimens constructed to treat patients failing current therapies with multi-drug-resistant HIV-1. Additional data are needed to determine its role in the treatment of less advanced patients. Issue surrounding long-term adverse effects and genetic barriers to raltegravir resistance will be critical in determining the potential of this agent.Keywords
This publication has 20 references indexed in Scilit:
- Rapid and Durable Antiretroviral Effect of the HIV-1 Integrase Inhibitor Raltegravir as Part of Combination Therapy in Treatment-Naive Patients With HIV-1 InfectionJAIDS Journal of Acquired Immune Deficiency Syndromes, 2007
- Integrase inhibitors to treat HIV/AidsNature Reviews Drug Discovery, 2005
- HIV Integrase Structure and FunctionPublished by Elsevier ,1999
- HIV-1 Integrase: Structural Organization, Conformational Changes, and CatalysisPublished by Elsevier ,1999
- Declining Morbidity and Mortality among Patients with Advanced Human Immunodeficiency Virus InfectionNew England Journal of Medicine, 1998
- Kinetics of CD4+ T cell repopulation of lymphoid tissues after treatment of HIV-1 infectionProceedings of the National Academy of Sciences, 1998
- Biphasic kinetics of peripheral blood T cells after triple combination therapy in HIV-1 infection: A composite of redistribution and proliferationNature Medicine, 1998
- Reduction of HIV-1 in blood and lymph nodes following potent antiretroviral therapy and the virologic correlates of treatment failureProceedings of the National Academy of Sciences, 1997
- Positive Effects of Combined Antiretroviral Therapy on CD4 + T Cell Homeostasis and Function in Advanced HIV DiseaseScience, 1997
- Association of integrase, matrix, and reverse transcriptase antigens of human immunodeficiency virus type 1 with viral nucleic acids following acute infection.Proceedings of the National Academy of Sciences, 1993