in vitro PHARMACOLOGY 2011 CATALOG - Cerep

200 in vitro pharmacology 2011 catalog
❚ Cerep standard profiles
❚ P-gp mediated drug-drug interaction profile [14 assays]
FULL panel
Ref. P21
Q 4 weeks
MODULES
Module 1 Ref. P21-m1
Q 4 weeks
Module 2 Ref. P21-m2
Q 4 weeks
P-glycoprotein (P-gp) is an efflux pump located in the intestine and blood-brain barrier among
other tissues. Compounds that are substrates for P-gp may be secreted back into the lumen of
the intestine. Additionally, compounds may be inhibitors of P-gp, and interfere with the efflux
of concurrently administered drugs, resulting in potentially toxic levels and severe side effects.
Compounds that are P-gp substrates may or may not inhibit P-gp activity. Similarly, compounds
that are P-gp inhibitors may or may not be substrates for P-gp.
The FDA draft guidance for industry on drug interaction studies addresses study design and data
analysis for evaluating P-gp substrates and inhibitors. It recommends the bi-directional transport
assay as the definitive assay for identifying P-gp substrates and inhibitors since this measures
drug efflux in a more direct manner than other methods.
The P-gp-mediated drug-drug interaction profile is a set of assays designed to comply with
the FDA draft guidance recommendations.
The P-gp mediated drug-drug interaction profile contains 2 modules:
1 P-gp substrate evaluation (12 assays):
Step I assays are designed to assess a compound's non-specific binding and determine the
efflux ratio and linear flux range.
Step II assays are designed to confirm whether the efflux activity is related to P-gp by including
P-gp inhibitors and to evaluate the concentration dependence of the test compound.
2 P-gp inhibitor evaluation (2 assays):
Assays are designed to determine the IC 50 value of the test compound.
For list of assays included in standard profiles and updated information:
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New profile Profile/module changed as compared to 2010: please go to www.cerep.com Q Standard turnaround time