Medium throughput assays

MT-Direct vesicular transport assays: In a medium throughput mode, the direct vesicular transport studies have a modular set up. These assays have two basic and one optional module. The launch of the given modules depends on the success of the previous module.

The suggested modules are the following:

  • Module 1 - Assay Development: pilot experiments to determine feasibility
  • Module 2 - Detailed characterization of the transport: KM and Vmax
  • Module 3 - Optional module for characterizing potential drug-drug interactions

MT-Direct uptake transport assays are organized into the same modules as the direct vesicular transport assays.

Caco-2 : Screening for uni- and bi-directional permeability in polarized monolayers of human epithelial cells to assess intestinal absorption and/or map transporter interactions. Digoxin transport inhibition studies model P-gp mediated drug-drug interactions.

MDCKII cell lines transfected with both BCRP and OATPB model vectorial transport across hepatocytes as well as endothelial cells in the placenta. The single transfectants and the parental cell lines provide negative controls for the transport.

For more scientific background on monolayer assays please click here.

Further assays with MDCKII (MRP2, uptake transporters) single and double transfected cell lines and with LLC-PK1 transfected (MDR1 or ratMdr1b) cell monolayers are under development.

This page contains information about following topics: Digoxin assessment, Verapamil, Transporter drug-drug interaction, Transporter Oral bioavailability, BBB penetration, Transporter CNS.