Multiple SLC and ABC Transporters Contribute to the Placental Transfer of Entecavir

• DOI: 10.1124/dmd.116.073304
• Publication Date: 2017-01-07T02:08:25Z
• Authors: Zhiyuan Ma; Xi Yang; Ting Jiang; Mengru Bai; Caihong Zheng; Su Zeng; Dongli Sun; Huidi Jiang
• Keywords: Entecavir; Efflux; Trophoblast; P-glycoprotein; Abcg2

Entecavir (ETV), a nucleoside analog with high efficacy against hepatitis B virus, is recommended as first-line antiviral drug for the treatment of chronic B. However, scant information available on use ETV in pregnancy. To better understand safety pregnant women, we aimed to demonstrate whether could permeate placental barrier and underlying mechanism. Our study showed that small amount across placenta mice. accumulation activated or nonactivated BeWo cells (treated without forskolin) was sharply reduced presence 100 <i>µ</i>M adenosine, cytidine, Na⁺ free medium, indicating transporters possibly mediate uptake ETV. Furthermore, proved be substrate concentrative transporter (CNT) 2 CNT3, organic cation (OCT) 3, breast cancer resistance protein (BCRP) using transfected expressing respective transporters. The inhibition primary human trophoblast further confirmed equilibrative (ENT) 1/2, CNT2/3, OCT3, cation/carnitine (OCTN) might involved transfer placenta. Therefore, from maternal circulation transported by ENT1/2, OCTN2, whereas efflux fetal mediated BCRP, multidrug resistance-associated 2, P-glycoprotein. obtained present may provide basis