Comparison of two hepatic uptake assay methods
Akito Takahashi, Ryota Takeuchi, Ryo Fujino, Kenta Hashizume, Shin-ichi Ninomiya
Drug Development Solutions Center, Drug Development Solutions Division, Sekisui Medical Co., Ltd. 2117 Muramatsu, Tokai, Ibaraki 319-1182, Japan
“Comparison of two hepatic uptake assay methods, plated and oil layer methods, using human and preclinical species cryopreserved hepatocytes”
The prediction of in vivo human hepatic clearance (CL) of drug from in vitro data is important for drug development. Primary Human cryopreserved hepatocytes are widely used as an in vitro tool for the prediction of in vivo CL since a variety of hepatic uptake transporters are expressing in them. The oil layer method is a current major hepatic uptake assay method. On the other hand, the plated method has come to be used to evaluate hepatic uptake recently. In this study, we compared the difference between the plated method and the oil layer method using human cryopreserved hepatocytes in order to show the usefulness of the plated method. Also, we examined whether or not the plated method is useful for the evaluation of species difference of hepatic uptake using preclinical species (monkey, dog, and rat) cryopreserved hepatocytes.