PReadyPort - OATP2B1 BCRP

A NOVEL READY-TO-USE SYSTEM FOR IN VITRO NET TRANSPORT EVALUATION

Membrane transporters can be major determinants of the pharmacokinetic, safety and efficacy profiles of drugs. Monolayer assays using transfected MDCKII cells have been widely recognized tools, acknowledged by the ITC1, to study the interaction of drugs with cellular transporters.

OATP2B1 – Organic Anion Transporting Polypeptide 2B1 is present in the blood-brain-barrier, the liver, the intestine and the placenta; and BCRP – Breast Cancer Resistance Protein plays an important role in drug disposition and distribution, similar to P-gp.

PreadyPortTM-OATP2B1/BCRP Kits contain 24-insert integrated plates with differentiated MDCKII cells expressing OATP2B1/BCRP, as well as the parental cell line. It can be used to model the net transport events of important fluid compartment barriers in the organism. This system is suitable for performing both inhibition and substrate assessments.

FEATURES

 

  • Available on demand
  • Ready-to-use
  • User-friendly and easy-handling system
  • Adaptable to automation
  • Transporter experiments without in house cell propagation
  • Transporter experiments without in house cell line development or acquisition

REGULATORY REQUIREMENTS

  • OATPs are expressed on majority of the major absorptive membrane surfaces throughout the body.
  • OATPs play a major role in the influx of endogenous compounds as well as clinically important drugs.
  • OATPs impact in the absorption, distribution and excretion of pharmacologically active drugs throughout the body can lead to increased drug-drug interaction risk.
  • BCRP interaction can act as a barrier to absorption and distribution of drugs in intestinal epithelia and blood-brain barrier. BCRP also contributes to the biliary excretion of compounds. OATPs play a major role in the influx of endogenous compounds as well as clinically important drugs.
  • Inhibition of BCRP may lead to hepatotoxicity due to build-up of endogenous and xenobiotic compounds in the liver.
  • Several clinicaly relevant drug-drug interactions (DDIs) have been associated with BCRP.
APICAL BASOLATERAL OATPB2

CLINICAL IMPORTANCE

  • MRP2 confers resistance to diverse chemotypes
  • MRP2 is implicated in cancer drug resistance.
  • Specifically in the hepatocyte, MRP2 plays an active role in excretion of bilirubin.
  • MRP interactions have been identified as playing a part in a number of clinically relevant drug-drug interactions (DDIs) and conferring drug resistance.

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