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Caco-2 permeability, P-gp and BCRP assessment
Intestinal permeability of a drug is an important factor driving the fraction absorbed and can be evaluated using the Caco-2 monolayer transport assay. The Caco-2 cell model is one of the industry standards for investigating intestinal absorption, permeability and drug-drug-interactions (DDIs).
Membrane drug transporters, located in many barrier tissues in the body, may interact with drugs to affect absorption, distribution and elimination in vivo, and are the cause of clinically relevant DDIs.
Identification of the test article as a substrate or an inhibitor of transporters can explain clinically relevant altered exposures and toxicities of concomitantly administered drugs.
Regulators have guidance on identifying P-gp and BCRP as key transporters with potential clinical implications.
