Placental transfer of darunavir in an ex vivo human cotyledon perfusion model

Antimicrob Agents Chemother. 2014 Sep;58(9):5617-20. doi: 10.1128/AAC.03184-14. Epub 2014 Jun 30.

Abstract

Placental transfer of the HIV protease inhibitor darunavir was investigated in 5 term human cotyledons perfused with darunavir (1,000 ng/ml) in the maternal to fetal direction. The mean (± the standard deviation [SD]) fetal transfer rate (FTR) (fetal/maternal concentration at steady state from 30 to 90 min) was 15.0%±2.1%, and the mean (±SD) clearance index (darunavir FTR/antipyrine FTR) was 40.3%±5.8%. This shows that darunavir crosses the placenta at a relatively low rate, resulting in fetal exposure.

MeSH terms

  • Biological Transport
  • Darunavir
  • Female
  • HIV Protease Inhibitors / metabolism*
  • HIV Protease Inhibitors / therapeutic use
  • Humans
  • Maternal-Fetal Exchange*
  • Placenta / metabolism*
  • Pregnancy
  • Sulfonamides / metabolism*
  • Sulfonamides / therapeutic use

Substances

  • HIV Protease Inhibitors
  • Sulfonamides
  • Darunavir