A NOVEL READY-TO-USE SYSTEM FOR IN VITRO DRUG TRANSPORTER 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. The MDCKII-MRP2 monolayer system is suitable for performing both substrate and inhibition assessments and is often used to model the net transport events of important fluid compartment barriers in the organism that express MRP2 at a high level, such as human intestinal epithelium, liver and kidney. Predyctive-MRP2 kits contain 24-insert integrated plates with differentiated MDCKII cells expressing MRP2, as well as the parental cell line. The innovative shipping medium preserves the properties of the barrier throughout transportation. The kit will allow researchers to perform MRP2 interaction studies on monolayer’s without bothering about cell-line licensing and culturing.
- Differentiated MDCKII-MRP2 barrier (13 day 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 proprietary shipping medium
- Shipping medium is easy to remove after liquefaction at 37 °C
- Sample Assay Protocol and Plate Layouts
- Available under a Limited Single-use License without extra charge
- Available on demand.
- 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.
- MRP2 substrates assessments (direct transport studies)
- MRP2 inhibition assessment (drug-drug interactions)
- Models the net transport events of barriers like the human intestinal epithelium, liver and kidney
- FDA and EMA state that, as the field of transporter protein science is rapid growing, additional transporters may be considered.
- Based on “knowledge of other drugs in the therapeutic class as the investigational drug” and that the “choice of transporters investigated should be based on scientific evidence”.
- 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.