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Transporter studies for ADME and therapeutic activity

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Transporters are membrane proteins that control the influx and efflux of essential nutrients, ions, neurotransmitters, cellular waste, environmental toxins, and other xenobiotics such as drugs. Drug transporters are composed of two major super families: ABC (ATP binding cassette) and SLC (solute carrier) transporters.

ABC transporters mediate unidirectional efflux and are primarily active transporters as they directly rely on ATP hydrolysis to pump their substrates across membranes. They 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 transporters mediate either drug uptake or efflux and can be facilitated transporters or secondary active transporters, which transport drugs using energy produced by transmembrane movement of other solutes in accordance with their concentration gradient. They play major roles in hepatic and renal uptake, and urinary excretion. Some SLC transporters, such as those for neurotransmitters, are also important drug targets themselves with clinical drugs treating various psychiatric disorders.

Transporters play a significant role in a drug's clinical efficacy and safety. Eurofins, through the expertise of Cerep and Panlabs, has developed robust transporter uptake and inhibition assays to allow quick and cost-effective screening of new molecular entities (NMEs) for their interactions with these transporters.

   

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Advantages of transporter screening with Eurofins:

  • Cell based assays to provide functional characterization of compound activity
  • Key drug transporters and neurotransmitter transporters are covered
  • Drug transporter assays meet regulatory requirements