Effect of drug efflux transporters on placental transport of antiretroviral agent abacavir.
作者： Zuzana Neumanova , Lukas Cerveny , Susan L. Greenwood , Martina Ceckova , Frantisek Staud
DOI: 10.1016/J.REPROTOX.2015.07.070
关键词:
摘要: Abacavir is as a frequent part of combination antiretroviral therapy used in pregnant women. The aim this study was to investigate, using vitro, situ and ex vivo experimental approaches, whether the transplacental pharmacokinetics abacavir affected by ATP-binding cassette (ABC) efflux transporters functionally expressed placenta: P-glycoprotein (ABCB1), breast cancer resistance protein (ABCG2), multidrug resistance-associated 2 (ABCC2) 5 (ABCC5). In vitro transport assays revealed that substrate human ABCB1 ABCG2 but not ABCC2 or ABCC5. addition, experiments dually perfused rat term placenta confirmed interactions with placental Abcb1/Abcg2. contrast, uptake studies villous fragments did reveal any interaction suggesting large contribution passive diffusion and/or influx mechanisms net transfer.
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