Phase I/II evaluation of nevirapine alone and in combination with zidovudine for infection with human immunodeficiency virus

J Acquir Immune Defic Syndr Hum Retrovirol. 1995 Feb 1;8(2):141-51.


In these Phase I/II open-label clinical trials, 62 persons with human immunodeficiency virus type 1 (HIV-1) infection and CD4+ cell counts < 400/mm3 received nevirapine at doses of 12.5, 50, and 200 mg/day, alone or in combination with zidovudine, 200 mg q8h. Nevirapine was well tolerated in the doses tested. Mean steady-state trough levels were 0.23, 1.1, and 1.9 micrograms/ml for the 12.5, 50, and 200 mg/day doses, respectively. Early suppression of p24 antigen levels and increase in CD4+ cell count were reversed following rapid emergence of virus less susceptible to nevirapine. Resistant strains were isolated from all participants by 8 weeks. Nevertheless, reduction of p24 antigen levels to < 50% of baseline values persisted for 12 weeks or more in four of seven persons who received 200 mg nevirapine/day in combination with zidovudine: these individuals had been antigenemic on long-term zidovudine therapy. This study demonstrates a direct relationship between drug resistance and effects on surrogate markers in HIV-1 infection.

Publication types

  • Clinical Trial
  • Clinical Trial, Phase I
  • Clinical Trial, Phase II
  • Controlled Clinical Trial
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adult
  • Antiviral Agents / therapeutic use*
  • CD4 Lymphocyte Count
  • Dose-Response Relationship, Drug
  • Drug Therapy, Combination
  • Female
  • HIV Core Protein p24 / blood
  • HIV Infections / blood
  • HIV Infections / drug therapy*
  • HIV-1 / drug effects*
  • Humans
  • Male
  • Middle Aged
  • Nevirapine
  • Pyridines / adverse effects
  • Pyridines / pharmacokinetics
  • Pyridines / therapeutic use*
  • Reverse Transcriptase Inhibitors
  • United States
  • Zidovudine / therapeutic use*


  • Antiviral Agents
  • HIV Core Protein p24
  • Pyridines
  • Reverse Transcriptase Inhibitors
  • Zidovudine
  • Nevirapine