ticagrelor and gallocatechol

This study aimed at exploring the potential mechanism of decreased in vivo exposure of the antiplatelet agent, ticagrelor and its active metabolite, AR-C124910XX, mediated by tea polyphenols, which was first revealed by our previous study, as well as predicting the in vivo drug-drug interaction (DDI) potential utilizing an in vitro to in vivo extrapolation (IVIVE) approach. The bidirectional transport and uptake kinetics of ticagrelor were determined using Caco-2 cells. Inhibition potency of major components of tea polyphenols, epigallocatechin gallate (EGCG) and epigallocatechin (EGC) were obtained from Caco-2 cells, human intestinal and hepatic microsomes (HIMs and HLMs) in vitro. A mean efflux ratio of 2.28 ± 0.38 and active uptake behavior of ticagrelor were observed in Caco-2 cell studies. Further investigation showed that the IC

Topics: Adenosine; Biological Transport; Caco-2 Cells; Catechin; Cell Line, Tumor; Drug Interactions; Humans; Intestinal Absorption; Kinetics; Microsomes, Liver; Models, Theoretical; Platelet Aggregation Inhibitors; Polyphenols; Purinergic P2Y Receptor Antagonists; Tea; Ticagrelor