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MDR1-MDCK permeability assay (P-glycoprotein substrate identification)

Understand the suitability of your compound for oral dosing or for use as a CNS therapeutic by using our MDR1-MDCK permeability assay to identify intestinal or CNS permeability, characterize P-gp substrates or investigate P-gp efflux.

MDR1-MDCK permeability is one of our portfolio of in vitro ADME screening services. Cyprotex deliver consistent, high quality data with cost-efficiency that comes from a highly automated approach.

 

Use of MDR1-MDCK permeability in the identification of P-gp substrates

  • MDR1-MDCK cells originate from transfection of Madin Darby canine kidney (MDCK) cells with the MDR1 gene, the gene encoding for the efflux protein, P-glycoprotein (P-gp)2.
  • The MDR1-MDCK permeability assay is a valuable tool for the identification and characterization of P-gp substrates and inhibitors.
  • Using MDR1-MDCK cells avoids the complexities of multiple transporters by focusing specifically on P-gp, one of the most well-recognized efflux transporters in many tissues including the brain, kidney and intestine.
  • MDR1-MDCK helps to gain a greater understanding of the mechanism of drug efflux, and highlights early potential issues with drug permeability.
  • MDR1-MDCK has been found to be a useful predictor of blood brain barrier permeability.
  MDR1-MDCK Permeability
‘All investigational drugs should be evaluated in vitro to determine whether they are a potential substrate of P-gp or BCRP.’
1FDA Draft Guidance for Industry - Drug Interaction Studies - Study Design, Data Analysis, Implications for Dosing, and Labeling Recommendations (February 2012).
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References

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11 Liu X et al. (2004) Drug Metab Dispos 32; 132-139.
12 Zhao YH et al. (2001) J Pharmaceut Sci 90; 749-784

1 Draft FDA Guidance for Industry - Drug Interaction Studies - Study Design, Data Analysis, Implications for Dosing, and Labeling Recommendations (February 2012).
2 Pastan I et al. (1988) Proc Natl Acad Sci USA 85; 4486-4490.
3 Wang O et al. (2005) Int J Pharmaceut 288; 349-359.
4 Di L et al. (2003) Eur J Med Chem 38; 223-232.
5 Seelig A et al. (1994) Proc Natl Acad Sci USA 91; 68-72.
6 Thomas RC et al. (1975) J Pharm Sci 64; 1360-6.
 

 
MDR1-MDCK permeability

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on 16th April 2014
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