DMD Highlight: Multiple SLC and ABC Transporters Contribute to the Placental Transfer of Entecavir
Entecavir (ETV) is recommended as a first-line antiviral drug for the treatment of chronic hepatitis B, but is classified as a pregnancy category C drug. Here, from in vitro and in vivo approaches, the authors concluded that ETV uptake from the maternal circulation to trophoblast cells occurs via the transporters CNT2/3, ENT1/2, and OCTN2, whereas ETV efflux from trophoblast cells to the fetal circulation is mediated by OCT3, and efflux from trophoblast cells to the maternal circulation may be mediated by BCRP, multidrug resistance-associated protein 2, and P-glycoprotein. The results indicate that ETV could cross human placenta, but the fetal exposure of ETV in human is predicted to be low. Therefore, ETV probably could be a candidate for HBV treatment to reduce perinatal transmission at delivery.
See the article by Ma et al. at Drug Metabolism and Disposition March 2017, 45 (3) 269-278; DOI: https://doi.org/10.1124/dmd.116.073304