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:
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:
In vitro toxicity (high-content analysis, cytotoxicity)