TMC125 exerts similar initial antiviral potency as a five-drug, triple class antiretroviral regimen

AIDS. 2003 Dec 5;17(18):2623-7. doi: 10.1097/00002030-200312050-00009.

Abstract

Objective: TMC125, a next generation, non-nucleoside reverse transcriptase inhibitor (NNRTI), demonstrated a remarkable decline of plasma HIV-1 RNA during a phase IIa study. We compared the initial rate of decline of plasma HIV-1 RNA achieved by TMC125 monotherapy with that of a triple class, five-drug regimen, containing drugs from all three currently licensed classes (zidovudine, lamivudine, abacavir, indinavir and nevirapine).

Methods: The decline in plasma HIV-1 RNA of 12 HIV-1 infected, antiretroviral (ART) naive patients treated for 1 week with TMC125 monotherapy was compared with that observed in the ERA study (n = 11). The plasma HIV-1 RNA elimination rate constant was calculated based on at least four plasma HIV-1 RNA measurements during the first week of treatment (first-order elimination) and compared using the Student's t test.

Results: Median ages were 23 and 38 years for TMC125 and ERA patients, respectively (P = 0.001), median baseline plasma HIV-1 RNA levels were 4.2 and 4.8 log10 copies/ml (P = 0.001) and median baseline CD4 T-cell counts were 458 x 10(6) and 360 x 10(6) cells/l (P = 0.08). The median plasma HIV-1 RNA elimination rate constant was 0.68/day in TMC125 treated patients, and 0.56/day in ERA participants (P = 0.24). The median decline in plasma HIV-1 RNA after 7 days was 1.92 and 1.76 log10 copies (P = 0.77) and the median increase of CD4 T cells was 119 x 10(6) and 60 x 10(6) cells/l, respectively (P = 0.29).

Conclusion: Monotherapy with TMC125 in ART-naive, HIV-1-infected individuals resulted in a similar rate of decline of plasma HIV-1 RNA during 1 week of therapy as therapy with a five-drug regimen.

Publication types

  • Clinical Trial
  • Clinical Trial, Phase II
  • Comparative Study
  • Multicenter Study
  • Randomized Controlled Trial

MeSH terms

  • Adult
  • Anti-HIV Agents / therapeutic use*
  • Antiretroviral Therapy, Highly Active*
  • CD4 Lymphocyte Count
  • Dideoxynucleosides / therapeutic use
  • Double-Blind Method
  • Drug Therapy, Combination
  • Female
  • HIV Infections / blood
  • HIV Infections / drug therapy*
  • HIV Protease Inhibitors / therapeutic use
  • HIV-1*
  • Humans
  • Indinavir / therapeutic use
  • Lamivudine / therapeutic use
  • Male
  • Nevirapine / therapeutic use
  • Nitriles
  • Pyridazines / therapeutic use*
  • Pyrimidines
  • RNA, Viral / blood
  • Reverse Transcriptase Inhibitors / therapeutic use*
  • Treatment Outcome
  • Zidovudine / therapeutic use

Substances

  • Anti-HIV Agents
  • Dideoxynucleosides
  • HIV Protease Inhibitors
  • Nitriles
  • Pyridazines
  • Pyrimidines
  • RNA, Viral
  • Reverse Transcriptase Inhibitors
  • etravirine
  • Lamivudine
  • Zidovudine
  • Indinavir
  • Nevirapine
  • abacavir