ADME / TOX Screening

Permeability & Transporters

ADME / TOX Screening
IN THIS SECTION

Insights into compound permeability and interactions

Frontage offers FDA-recommended drug permeability and transporters assays to provide key insight into intestinal drug permeability and compound interaction with drug transporters.

The permeability of a drug candidate often referred to as its capability to penetrate across the human GI tract, is a key factor governing its oral absorption. The permeability of drugs and drug-like molecules across biological membranes is governed by processes that include passive diffusion, active uptake, active efflux, and receptor-mediated endocytosis. The potential for drug interaction with these proteins to affect both drug absorption and drug delivery to intracellular organelles may have significant implications for drug design.

Permeability Services at Frontage

  • Caco-2 Permeability
  • MDCK Permeability
  • MDCK-MDRI Permeability

The absorption of many compounds is also affected by transporters located on the cell membranes of various tissues in the body. For this reason, the FDA guidelines recommend the evaluation of the role of transporter proteins in the absorption process (transporter substrate), and possible interactions related to their functions (transporter inhibition & activation). This data shed light on potential drug-drug interactions (DDI).

Transporter Services at Frontage

  • P-gp & BCRP Inhibition and substrate assays
  • OATP1B1 and OATP1B3 inhibition and substrate assays