In vitro Drug Absorption and Transport
Understanding whether your compounds are permeability-limited
The absorption of orally administered drugs requires their movement across the intestinal epithelial barrier. Poor intestinal permeability leads to limited absorption. If a compound achieves 90% or greater oral absorption, it is considered highly permeable (for example, propranolol or metoprolol). Drugs that display 50% or less oral absorption are considered poorly permeable (for example, ranitidine and atenolol). Compounds with extremely poor permeability are likely to have limited in vivo absorption.
Intestinal epithelium permeability is a critical characteristic that determines the rate and extent of human absorption and ultimately affects the bioavailability of a drug candidate. Eurofins has recognized the need for robust and reliable permeability assays for rapid assessment of membrane permeability - assisting in rank-ordering compounds in terms of their absorption potential. P-glycoprotein (P-gp), an efflux transporter located in the intestine and blood-brain barrier among other tissues, counteracts the absorption of drugs. Eurofins also have permeability models to assess the ability of compounds to act as P-gp substrates.
By assessing your compounds' permeability in the early drug discovery stage, you'll be able to identify compounds which are more likely to pose challenges during preclinical and clinical development, saving time and effort later down the development process.
Available assays include: