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In Vitro Metabolism

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About In Vitro Metabolism

In vitro assays are an essential component of the data package required in support of an investigational new drug. 

Data is utilized for nomination of your drug development candidate and developing pharmacokinetic (PK) models of your test article for prediction of human pharmacokinetics and assessment of potential drug-drug interactions (DDI).

Get a Fully Compliant, DDI Solution

The ability of a drug to cause potential drug-drug interactions (DDIs) are predicted from your in vitro data. In vitro study designs conducted at therapeutic drug concentrations will indicate whether a test article has the potential to cause DDI, allowing informed decisions to be made about the necessity of a clinical DDI study.

We have established robust test systems to define the drug candidate characteristics of Absorption, Distribution, Metabolism, and Elimination (ADME). 

In Vitro Metabolism Studies

Enzyme Induction Drugs may increase drug metabolizing enzyme (DME) expression and activity leading to undesired clinical effects or toxicity. Assess the potential of your test article to induce DME expression and activity of cytochrome P450 enzymes in human hepatocytes. Enzyme Inhibition Inhibition of cytochrome P450 enzymes may lead to drug-drug interactions. Assess the inhibitory potential of your drug by determining its effect on the metabolism of established probe substrates utilizing pooled human liver microsomes. Metabolic Stability Assess your drug metabolism using cross-species hepatic, renal (or gut) microsomes, hepatocytes or other matrix specific to your program. Compare and assess your compound’s metabolic rate across species to predict human PK. With state-of-the-art global mass spectometry capabilities, you can receive metabolic profiling and identification to better understand the clearance pathways for your drug. Protein Binding Determining your drug fraction unbound in plasma and its association with blood cell components is critical for assessing drug-drug interaction risks, determining the ideal analytical approach for pharmacokinetic blood sample analysis, and for establishing robust pharmacometic models. Utilize specific protein binding and blood cell partitioning methods to support your program. Reaction Phenotyping Identifying DME responsible for metabolizing your drug will highlight potential liabilities associated with clearance pathways. Utilize established tools such as chemical inhibitors and human recombinant enzymes to determine the role and extent of each DME in the metabolism of your drug. Transporter & Absorption Membrane drug transporters are a key component in understanding potential DDI associated with your drug. Potential drug-drug interactions may impact the ADME characteristics of your drug and lead to clinically relevant drug-drug interactions (DDIs). Identifying your drug as a substrate or an inhibitor of drug transporters will provide data to better understand and predict clinically relevant shifts in exposures associated with concomitantly drugs.

Regulatory Guidance Resources

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