Raltegravir: the first HIV-1 integrase strand transfer inhibitor in the HIV armamentarium

Ann N Y Acad Sci. 2011 Mar:1222:83-9. doi: 10.1111/j.1749-6632.2011.05972.x.

Abstract

Raltegravir is the first integrase strand transfer inhibitor approved for the treatment of HIV-1 infection. As the first agent in this new class of antiretroviral therapies, raltegravir has demonstrated safety and efficacy in treatment-naive as well as heavily pretreated HIV-infected patients failing therapy with multidrug-resistant virus. Raltegravir has a favorable drug interaction profile that permits both administration to a wide, demographically diverse patient population and coadministration with many other therapeutic agents, including antiretroviral agents and supportive medications, without restrictions or dose adjustment. Data through 96 weeks of follow-up in three phase III studies, protocol 021 (STARTMRK) in treatment-naive patients, and protocols 018 (BENCHMRK-1) and 019 (BENCHMRK-2) in treatment-experienced patients, demonstrated the potent and durable antiretroviral and immunologic effects and the favorable long-term safety profile of raltegravir in both treatment-naive and treatment-experienced patients. Raltegravir represents an important addition to the current armamentarium for the treatment of HIV infection.

Publication types

  • Evaluation Study
  • Review

MeSH terms

  • Anti-HIV Agents / administration & dosage
  • Anti-HIV Agents / chemical synthesis
  • Anti-HIV Agents / therapeutic use*
  • Anti-Retroviral Agents / administration & dosage
  • Anti-Retroviral Agents / therapeutic use
  • Clinical Trials, Phase III as Topic
  • HIV Infections / drug therapy*
  • HIV Integrase / metabolism
  • HIV Integrase Inhibitors / administration & dosage
  • HIV Integrase Inhibitors / chemical synthesis
  • HIV Integrase Inhibitors / therapeutic use*
  • HIV-1 / drug effects
  • HIV-1 / physiology
  • Humans
  • Pyrrolidinones / administration & dosage
  • Pyrrolidinones / adverse effects
  • Pyrrolidinones / chemical synthesis
  • Pyrrolidinones / therapeutic use*
  • Raltegravir Potassium
  • Treatment Outcome

Substances

  • Anti-HIV Agents
  • Anti-Retroviral Agents
  • HIV Integrase Inhibitors
  • Pyrrolidinones
  • Raltegravir Potassium
  • HIV Integrase
  • p31 integrase protein, Human immunodeficiency virus 1