Maternal-fetal transfer of saquinavir studied in the ex vivo placental perfusion model.
OBJECTIVE
This study was undertaken to determine the placental transfer of the human immunodeficiency virus protease inhibitor saquinavir.


METHODS
An ex vivo perfused human placental cotyledon model was used. Ten placental perfusion studies were performed, with concentrations of saquinavir in the maternal compartment ranging from 322 to 2197 ng/mL (within reference therapeutic ranges). Drug concentrations were determined by high-performance liquid chromatography.


RESULTS
The mean (+/- SD) fetal transfer rate of saquinavir was 1.8% +/- 1.6%, and the mean (+/- SD) clearance index was 0.05 +/- 0.05. A mean (+/- SD) of 1.6% +/- 3.1% of the perfused saquinavir was retained by the cotyledon. The small amount of saquinavir that crossed the placenta corresponded to the fraction not bound to human serum albumin.


CONCLUSIONS
The low rate of placental transfer of saquinavir suggests that use of this antiretroviral drug by pregnant women may not lead to significant exposure of the fetus.
Forestier
F
F
Université Paris Sud, Paris, France.
de Renty
P
P
Peytavin
G
G
Dohin
E
E
Farinotti
R
R
Mandelbrot
L
L
D005260:Female; D017320:HIV Protease Inhibitors / Q000378:metabolism*; D006801:Humans; D066298:In Vitro Techniques; D007700:Kinetics; D008431:Maternal-Fetal Exchange; D010920:Placenta / Q000378:metabolism*; D011247:Pregnancy; D019258:Saquinavir / Q000378:metabolism*
D017320:HIV Protease Inhibitors; D019258:Saquinavir