drug metabolism & pharmacokinetics

We understand you need to efficiently identify and focus your efforts on compounds that have the greatest likelihood of success. Our high throughput automated in vitro ADMET and in vivo pharmacokinetic/ADME screening services provide you key information to help prioritize and accelerate the drug discovery process from compound ranking to lead candidate selection.
Additional in-depth GLP in vitro and in vivo metabolism services are also available to complement the regulated toxicology and pharmacology investigations carried out further in the drug development process.
In Vitro ADMET
In vitro ADMET parameters are a set of factors that describe how a drug behaves in the human body and can be a major cause of drug failure. By focusing on in vitro ADMET data you can predict at an early stage which compounds not only possess good binding affinity for a specific target, but also pass the test for good bioavailability and safety. Our wide range of automated in vitro assays yields information in the areas of metabolism, toxicity, and physicochemical characteristics.
In vitro screening assays:
Aqueous solubility
Cytochrome P450 enzyme inhibition
Cytochrome P450 induction
Cytochrome P450 reaction phenotyping
Cell permeability and efflux assays (CaCo-2)
Cell proliferation and cytotoxicity
Drug-drug interaction
Enzyme assays
hERG inhibition
Melanin binding
Metabolic plasma and buffer stability
Metabolite profiling
Metabolite assessment and identification
Plasma protein binding

In Vivo Pharmacokinetic/ADME Screening
Whether you have one compound or a library of compounds requiring drug metabolism assessment, the skilled scientists at Charles River can design, conduct, and interpret the in vivo pharmacokinetic/ADME components of your program as part of our streamlined non-GLP screening services. Quick study initiation, multiple species, resident animal colonies with chronic surgical models included, and various dose regimens and administration routes plus bioanalytical support provide the necessary tools you need to rapidly identify and optimize potential drug candidates.
Available services:
Bioavailability
Biliary excretion
Mass balance
Tissue distribution
Placental transfer
Bioequivalence
Dose ranging
Linearity
Proportionality
Single, multiple, and cassette dosing
Metabolite profiling
Surgical models:
Vascular access ports
Chronic bile duct cannulation in nonrodent species
Intestinal cannulation
Portal vein cannulation
Cardiovascular telemetry

Laboratory support:
Formulation development
Research-grade assays