Raltegravir: an integrase inhibitor for HIV-1.
BACKGROUND
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.


OBJECTIVE
To form an evidence-based determination of the clinical efficacy, pharmacokinetics and safety profile of raltegravir.


METHODS
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).


CONCLUSIONS
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.
Evering
Teresa H
TH
The Aaron Diamond AIDS Research Center/Rockefeller University, 455 First Avenue, New York, NY 10016, USA.
Markowitz
Martin
M
D023241:Antiretroviral Therapy, Highly Active; D002986:Clinical Trials as Topic; D015658:HIV Infections / Q000188:drug therapy* / Q000821:virology; D019428:HIV Integrase Inhibitors / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D015497:HIV-1 / Q000187:drug effects* / Q000201:enzymology / Q000302:isolation & purification; D006801:Humans; D009930:Organic Chemicals / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D011760:Pyrrolidinones; D012367:RNA, Viral / Q000032:analysis; D000068898:Raltegravir Potassium
D019428:HIV Integrase Inhibitors; D009930:Organic Chemicals; D011760:Pyrrolidinones; D012367:RNA, Viral; D000068898:Raltegravir Potassium