Transporters for drug absorption and disposition
Testing FDA and EMA recommended drug transporters
Drug transporters are essential in controlling the absorption and disposition of xenobiotics, including pharmaceuticals. As such, transporters play a key role in defining the clinical efficacy and safety of drugs.
ABC (ATP binding cassette) transporters, including members like P-gp and BCRP transporters, play major roles in hepatobiliary and urinary excretion of drugs from the blood to the lumen, intestinal absorption of drugs, and in brain blood barrier penetration of drugs. SLC (solute carrier) transporters, including members like OATP1B1 and OAT1, play major roles in hepatic and renal uptake, and urinary excretion.
Interaction with these efflux or uptake transporters can play a significant role in a drug's pharmacokinetic properties and, in turn, its efficacy and safety profile. Eurofins, through the expertise of Cerep and Panlabs, has developed robust in vitro transporter inhibition assays to assess potential drug-drug interactions prior to costly clinical assessment.
Advantages of Drug Transporter Screening:
Figure 1. Inhibition profiles of FDA and EMA recommended transporters
Inhibition of transport of fluorogenic substrates by transporter inhibitor reference compounds (% of control response)