A novel ready-to-use system for in vitro drug transporter evaluation

A NOVEL READY-TO-USE SYSTEM FOR IN VITRO DRUG TRANSPORTER EVALUATION

Membrane transporters can be major determinants of the pharmacokinetic, safety and efficacy profile of drugs.

Monolayer assays using transfected MDCKII-BRCP (ABCG2) cells have been widely recognized tools, acknowledged by the ITC1 , to study the interaction of drugs with the BCRP transporter.

This system is suitable for performing both inhibition and substrate assessments.

MDCKII-BCRP is often used to model the net transport events of important fluid compartment barriers in the organism that express BCRP at high level. BCRP transporter is present in the blood-brain-barrier, intestine, liver, kidney, testis and mammary tissue.

FEATURES

  • Differentiated MDCKII-BRCP barrier (11 days system)
  • Flexibility: the kit can be used up to 7 days after reception.
  • 24 insert-integrated plate format.
  • Up to 4 days of transportation and storage at room temperature in propietary shipping medium.
  • Shipping medium is easy to remove after liquefication at 37ºC
  • Sample Assay Protocol and Plate Layouts.
  • Available under a Limited Single-use License without extra charge.

BENEFITS

  • 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.

APPLICATIONS

  • BCRP substrates assessments (direct transport studies).
  • BCRP inhibition assessment (drug-drug interactions)
  • Models the net transport events of barriers like the human blood-brain-barrier and the intestine.
Apical - Basolateral

REGULATORY REQUIREMENTS

  • BCRP transporter has relevance to drug PK and interactions, for BBB and tumor penetration.
  • In vitro evaluation is required by the regulatory agencies FDA and EMA for all drug candidates prior to going to market.
  • Based on this data, decisions are made for the need for BCRP transporter – based clinical drug interaction trials.

CLINICAL IMPORTANCE

  • 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.
  • 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.

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