Potent suppression of HIV-1 replication in humans by T-20, a peptide inhibitor of gp41-mediated virus entry

Nat Med. 1998 Nov;4(11):1302-7. doi: 10.1038/3293.


T-20, a synthetic peptide corresponding to a region of the transmembrane subunit of the HIV-1 envelope protein, blocks cell fusion and viral entry at concentrations of less than 2 ng/ml in vitro. We administered intravenous T-20 (monotherapy) for 14 days to sixteen HIV-infected adults in four dose groups (3, 10, 30 and 100 mg twice daily). There were significant, dose-related declines in plasma HIV RNA in all subjects who received higher dose levels. All four subjects receiving 100 mg twice daily had a decline in plasma HIV RNA to less than 500 copies/ml, by bDNA assay. A sensitive RT-PCR assay (detection threshold 40 copies/ml) demonstrated that, although undetectable levels were not achieved in the 14-day dosing period, there was a 1.96 log10 median decline in plasma HIV RNA in these subjects. This study provides proof-of-concept that viral entry can be successfully blocked in vivo. Short-term administration of T-20 seems safe and provides potent inhibition of HIV replication comparable to anti-retroviral regimens approved at present.

Publication types

  • Clinical Trial
  • Controlled Clinical Trial
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adult
  • Anti-HIV Agents / blood
  • Anti-HIV Agents / pharmacokinetics*
  • Anti-HIV Agents / therapeutic use*
  • CD4 Lymphocyte Count
  • Dose-Response Relationship, Drug
  • Enfuvirtide
  • HIV Envelope Protein gp41 / blood*
  • HIV Envelope Protein gp41 / physiology*
  • HIV Envelope Protein gp41 / therapeutic use*
  • HIV Infections / drug therapy*
  • HIV Infections / virology
  • HIV-1 / drug effects
  • HIV-1 / isolation & purification
  • HIV-1 / physiology*
  • Half-Life
  • Humans
  • Metabolic Clearance Rate
  • Peptide Fragments / blood*
  • Peptide Fragments / therapeutic use*
  • Virus Replication / drug effects*


  • Anti-HIV Agents
  • HIV Envelope Protein gp41
  • Peptide Fragments
  • Enfuvirtide