Safety and pharmacokinetics of nelfinavir during the second and third trimesters of pregnancy and postpartum

HIV Clin Trials. 2012 Jan-Feb;13(1):46-59. doi: 10.1310/hct1301-046.

Abstract

Purpose: Evaluate the safety, tolerability, and pharmacokinetics (PK) of nelfinavir during pregnancy and postpartum in HIV-infected women.

Methods: Phase IV, non-randomized, open-label study of nelfinavir 625 mg tablets (1250 mg) in combination with lamivudine/zidovudine twice daily. Primary endpoint was treatment-related or possibly treatment-related gastrointestinal or hepatic adverse events (AEs). Selected maternal and infant outcomes were recorded. Frequent plasma samples were collected for PK studies during the 2nd and 3rd trimesters, and 6 weeks postpartum, to analyze total and free nelfinavir and M8 concentrations.

Results: Sixteen HIV+ pregnant women were enrolled. Six mild treatment-related AEs and 3 serious AEs occurred; 1 serious AE (elevated AST) met the primary endpoint. Compared with 6 weeks postpartum, levels of total nelfinavir were reduced by 44% and 46%, total M8 by 82% and 83%, free nelfinavir by 48% and 39%, and free M8 by 83% and 79% in the 2nd and 3rd trimesters, respectively. At 6 weeks postpartum, 75% and 50% of subjects maintained HIV-1 RNA levels <400 and <50 copies/mL, respectively. All pregnancies resulted in live births without transmission in 15 infants.

Conclusions: Nelfinavir in combination with lamivudine/zidovudine was generally well tolerated. Total and free nelfinavir and M8 exposure were reduced in late pregnancy.

Publication types

  • Clinical Trial, Phase IV
  • Multicenter Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • CD4 Lymphocyte Count
  • Female
  • HIV Infections / drug therapy*
  • HIV Protease Inhibitors / adverse effects*
  • HIV-1 / genetics
  • HIV-1 / isolation & purification
  • Humans
  • Nelfinavir / adverse effects*
  • Nelfinavir / pharmacokinetics
  • Postpartum Period
  • Pregnancy
  • Pregnancy Complications, Infectious / drug therapy*
  • Pregnancy Trimester, Second
  • Pregnancy Trimester, Third
  • RNA, Viral / blood

Substances

  • HIV Protease Inhibitors
  • RNA, Viral
  • Nelfinavir