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Home > Products & Services > Pharmacology & ADME-Tox > Profiling > ADME-Tox

Cerep offers a range of over 130 assays (including 25 new assays) for rapid evaluation of the pharmaceutical properties and safety of drug discovery compounds:

Solution properties
Cerep has developed methods for the accurate and rapid assessment of the solubility, lipophilicity, chemical stability, protein binding and blood partitioning characteristics of chemical compounds.

In vitro drug absorption/ drug transport
Cerep has developed an efficient test to assess the intestinal permeability of compounds in both the absorptive and the secretory directions. The TC7 sub-clone of the Caco-2 cell line originally derived from the human intestine is used in this in vitro absorption model. Also available are Madin-Darby canine kidney cells (MDCKII) and MDCKII cells expressing the human MDRI gene (MDRI-MDCKII). Data obtained from the permeability tests can be used to:
      Predict drug absorption in human
      Identify potential substrates and/or inhibitors of efflux systems such as P-glycoprotein

In vitro drug metabolism
There is a significant advantage to obtaining metabolism data as early as possible in the drug discovery process. Hepatic metabolism is a primary determinant of pharmacokinetic behavior, and rapid first-pass metabolism is a major cause of low bioavailability. At Cerep, a variety of assay matrices including pooled liver microsomes, pooled liver S9 fraction, hepatocytes, recombinant cytochrome P450s and plasma are used for the metabolic assessment of hits, leads, and new pharmaceutical compounds. The results of the metabolism studies are useful in:
      Determining the initial rate at which compounds are metabolized
      Investigating the major pathways of drug metabolism
      Identifying probable metabolites
      Predicting in vivo pharmacokinetic properties
      Investigating the potential for drug-drug interactions

In vivo PK / Bioanalytical
Obtaining early stage pharmacokinetic data in the evaluation of new chemical entities is a prerequisite for successful animal pharmacology and toxicology studies. Cerep has developed pharmacokinetics assays in rats and mice. In addition, Cerep has also developed the in vivo blood-brain barrier assays in rats and mice to evaluate the brain penetration of compounds.
Cerep has developed three distinct assays – recovery, linearity, quantitative bioanalysis – to support in vivo pharmacokinetics studies. These assays are designed to ensure that reliable and useful data are ultimately obtained. In each case state-of-the-art HPLC-MS/MS instrumentation and optimized analytical methods allow for detection of picogram quantities of analyte in a biological matrix.

In order to be able to assess the potential toxicity of compounds as early as possible, Cerep has developed a set of in vitro tests which address:
      Drug-drug interactions
      Cardiac toxicity
      In vitro toxicity (high-content analysis, cytotoxicity)
      Genetic toxicity


Pharmacologie & ADME-Tox
Criblage à haut-débit (HTS)
Pharmacologie in vitro
Assay platforms
Global profiling services
Kinase assay platform
Functional GPCR platform
Binding assay platform
Custom assay development
BioPrint® services

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