Permeability and Transporters

Insights into compound permeability and interactions

Permeability and Transporters

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 

Contact us to discuss your permeability studies. 

 

The permeability assay is required by the FDA for sponsors to be able to apply for an Investigational New Drug (IND).

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). 

Contact us to discuss your drug transporter studies. 

Transporter Services at Frontage

  • P-gp Assays 
  • Other Transporters: Frontage has developed both substrate and inhibition assays for BCRP and MRP2 transporters in Caco-2 cells. For BCRP, estrone-3-sulfate is used as a reference substrate and FTC as an inhibitor. For MRP2, vinblastine is used as a reference substrate and MRK-571 as an inhibitor. 

Webinar: Innovative Solutions for Investigating Drug-Induced Liver Injury. Screen your drug candidate’s inhibition of BSEP and/or MDR3 to assess DILI risk.