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

Cerep offers a range of over 175 assays (including 22 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, ionization constant, 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, human recombinant cytochrome P450s, UGTs, blood, 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/BBB - Bioanalytical support
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 pharmacokinetic assays in rats and mice. In addition, Cerep has also developed 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 pharmacokinetic 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.

Drug-drug interactions
It is not uncommon that a patient may be taking several drugs, simultaneously, for the treatment of one or more health related issues. A drug may affect or be affected by other co-administered drugs. Metabolism-based drug-drug interactions occur when a drug inhibits or induces the activity of a drug metabolizing enzyme, which catalyzes the metabolism of a concomitant drug. Metabolism-based drug-drug interactions (DDI) are one of the major factors that cause drug failures during drug development. Early stage screening of compounds for potential drug-drug interactions using in vitro techniques becomes necessary in order to decrease late stage compound attrition.
Cerep offers a range of assays to determine the metabolism of compounds and their potential for drug-drug interactions.
      High-throughput cocktail CYP inhibition
      CYP inhibition- recombinant CYPs or liver microsomes
      Time-dependent CYP inhibition
      CYP induction

Toxicity
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:
      Cardiac toxicity
      In vitro toxicity
      Genetic toxicity

Many assays are suitable for evaluating the ADME-Tox properties of compounds early in the drug discovery process while others are designed with the intent to meet regulatory requirements making them suitable for later stage development.


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