Antiviral hyperactivation-limiting therapeutics as a novel class for the treatment of HIV/AIDS: focus on VS411

Expert Opin Investig Drugs. 2011 Apr;20(4):559-65. doi: 10.1517/13543784.2011.565047. Epub 2011 Mar 11.

Abstract

Introduction: Immune activation plays a central pathogenetic role in both HIV-1 replication and depletion of CD4(+) T cells leading to disease progression and the onset of the AIDS. While current antiretroviral therapies suppress viral replication to undetectable levels, they do not normalize the excessive level of T-cell activation and proliferation. A new class of anti-HIV-1 drugs known as antiviral hyperactivation-limiting therapeutics (AV-HALTs) combines direct antiviral activity with an antiproliferative action to limit the hyperactivation of the immune system now recognized as the key driver of the progressive loss of CD4(+) T cells that occurs over the natural course of the HIV-1 infection.

Areas covered: Areas covered include preclinical, Phase I and Phase IIa studies of VS411, the first drug product in a novel class of anti-HIV drugs, AV-HALT agents.

Expert opinion: The two drug combination VS411 safely achieved the goals established for the AV-HALT class based on the results of a Phase IIA proof-of-concept study. Additional work is underway to identify and develop new agents that combine the dual attributes of AV-HALTs, direct reduction of both HIV-1 viral load and markers of excessive immune activation, in a single molecule.

Publication types

  • Review

MeSH terms

  • Acquired Immunodeficiency Syndrome / drug therapy*
  • Acquired Immunodeficiency Syndrome / immunology
  • Anti-HIV Agents / administration & dosage
  • Anti-HIV Agents / pharmacology*
  • Anti-HIV Agents / therapeutic use*
  • CD4 Lymphocyte Count
  • CD4-Positive T-Lymphocytes / drug effects
  • Clinical Trials as Topic
  • Didanosine / administration & dosage
  • Didanosine / pharmacology*
  • Didanosine / therapeutic use*
  • Drug Combinations
  • Drug Evaluation, Preclinical
  • HIV Infections / drug therapy*
  • HIV Infections / immunology
  • Humans
  • Hydroxyurea / administration & dosage
  • Hydroxyurea / pharmacology
  • Hydroxyurea / therapeutic use
  • Lymphocyte Activation
  • Urea / analogs & derivatives*
  • Urea / pharmacology
  • Urea / therapeutic use
  • Viral Load / drug effects

Substances

  • Anti-HIV Agents
  • Drug Combinations
  • VS411 drug combination
  • Urea
  • Didanosine
  • Hydroxyurea