Transporters are a family of proteins that play a major role in the active uptake and efflux of substances, including drugs, across cellular membranes. Given many drugs directly interact with transporter proteins, as substrates and/or inhibitors, transporters are often a rate limiting step in defining the ADME-PK and toxicity profiles for drugs.
In the drug discovery process, understanding potential compound interactions with transporters in the early stage of development is essential for selecting candidates with desirable drug metabolism and safety profiles. Eurofins Discovery provides extensive transporter and permeability testing services, state-of-the-art equipment, and scientific expertise in DMPK to support your specific needs.
The key transporters involved in drug absorption, excretion, and drug-drug interactions belong to the ABC (ATP binding cassette) and SLC (solute carrier) transporter families. ABC transporters, including members like P-glycoprotein (P-gp), MRP2, BSEP, and BCRP, play major roles in hepatobiliary and urinary excretion of drugs, intestinal absorption of drugs, and in blood brain barrier (BBB) penetration of drugs. The SLC transporters, including members like OATP1B1, OATP1B3, OAT1, OAT3, OCT1, OCT2, MATE1 and MATE2-K, play major roles in hepatic and renal uptake of drugs, as well as urinary excretion of drugs.
To test for compound interactions with the ABC and SLC transporters, as recommended by regulatory agencies (FDA, EMA and PMDA), we offer both substrate assessment and inhibition services in Caco-2, MDCK, HEK293, CHO, membrane vesicles, various transfected cells lines, and transporter knock-out and knock-in cells using probe substrates, inhibitors and testing parameters as recommended by the regulatory agencies. For more information on available transporter assays, please see our features section below.
