Understanding metabolic routes of clearance is a key aspect of investigating DMPK (drug metabolism and pharmacokinetic) properties of a prospective drug compound. In vitro ADME and DMPK studies can provide important information useful for designing further nonclinical and clinical studies.
In Vitro Drug Metabolism Studies for Preclinical Drug Development
Our Approach to Evaluating Drug Metabolism
It is important to identify the enzymes that significantly contribute to the metabolism of a drug candidate and to evaluate its potential to be a victim (a drug whose clearance is significantly impacted by the removal of one or more routes of elimination) in a drug-drug interaction (DDI). We perform various types of in vitro metabolism studies to evaluate the potential of your compound to be metabolized by hepatic and/or extrahepatic enzymes, assess the extent of metabolism (stability), and elucidate the metabolic pathways to provide support through discovery and development processes.
Drug Metabolism Services We Offer
Metabolic Stability assays measure intrinsic clearance and determine the extent to which a drug will be metabolized. Multiple test systems are available to cover all major enzymes and pathways.
Metabolite Identification/Profiling/Characterization assays identify the number, putative structure, and proposed biotransformation of metabolites produced as a result of interaction with drug-metabolizing enzymes at various sites of metabolism. In some cases these results can determine preliminary components of reaction phenotyping studies.
Reaction Phenotyping studies are required by regulatory authorities to identify enzymes responsible for the biotransformation of a compound. Compounds with a single route of elimination have a high victim potential; knowing how a drug candidate is eliminated by the human body is important in understanding the potential for drug-drug interactions.
Species Comparison uses data from certain definitive in vitro studies to help a sponsor choose a preclinical animal model that most closely resembles human in its metabolic profile. Additionally, comparing animal species to human data helps identify any human-specific metabolites– a very important step in preclinical drug safety testing.
Related Services: Drug Metabolism Screening & Metabolite Production
Discovery Plus™ Screening Suite presents medium-throughput alternatives to definitive in vitro studies through non-GLP, abbreviated versions of our definitive assays. This option is best used for lead optimization and comparison of multiple compounds or to yield preliminary data for definitive in vitro studies.
Metabolite Production Services: Once metabolites have been identified through radiolabeling or in vitro metabolism studies, we can set you up to screen and optimize and produce metabolites directly from drug candidates through a service offered by our friends at HepatoChem.