High exposure to nevirapine in plasma is associated with an improved virological response in HIV-1-infected individuals

AIDS. 2001 Jun 15;15(9):1089-95. doi: 10.1097/00002030-200106150-00003.

Abstract

Objective: To explore relationships between exposure to nevirapine and the virological response in HIV-1-infected individuals participating in the INCAS trial.

Methods: The elimination rate constant of plasma HIV-1 RNA (k) was calculated during the first 2 weeks of treatment with nevirapine, zidovudine and didanosine in 51 antiretroviral-naive HIV-1-infected patients. The relationships between the value of k, the time to reach an undetectable HIV-1 RNA concentration in plasma (< 20 copies/ml) and the success of therapy after 52 weeks of treatment as dependent variables and the exposure to nevirapine, baseline HIV-1 RNA and baseline CD4 cell count as independent variables, were explored using linear regression analyses, proportional hazard models and logistic analyses, respectively.

Results: The value of k for HIV-1 RNA in plasma was positively and significantly associated with the mean plasma nevirapine concentration during the first 2 weeks of therapy (P = 0.011) and the baseline HIV-1 RNA (P = 0.008). Patients with a higher exposure to nevirapine reached undetectable levels of HIV-1 RNA in plasma more rapidly (P = 0.03). From 12 weeks on, the median nevirapine plasma concentration was significantly correlated with success of therapy after 52 weeks (P < 0.02).

Conclusions: A high exposure to nevirapine (in a twice daily regimen) is significantly associated with improved virological response in the short as well as in the long term. These findings suggest that optimization of nevirapine concentration might be used as a tool to improve virological outcome in (antiretroviral-naive) patients treated with nevirapine.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial

MeSH terms

  • Anti-HIV Agents / blood
  • Anti-HIV Agents / pharmacokinetics*
  • Anti-HIV Agents / therapeutic use
  • Didanosine / therapeutic use
  • Double-Blind Method
  • Drug Therapy, Combination
  • HIV Infections / blood
  • HIV Infections / drug therapy
  • HIV Infections / immunology
  • HIV Infections / virology*
  • HIV-1 / drug effects*
  • HIV-1 / genetics
  • HIV-1 / growth & development
  • Humans
  • Nevirapine / blood
  • Nevirapine / pharmacokinetics*
  • Nevirapine / therapeutic use
  • RNA, Viral / blood
  • Retrospective Studies
  • Reverse Transcriptase Inhibitors / blood
  • Reverse Transcriptase Inhibitors / pharmacokinetics*
  • Reverse Transcriptase Inhibitors / therapeutic use
  • Time Factors
  • Treatment Outcome
  • Zidovudine / therapeutic use

Substances

  • Anti-HIV Agents
  • RNA, Viral
  • Reverse Transcriptase Inhibitors
  • Zidovudine
  • Nevirapine
  • Didanosine