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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).

YES.  You can leverage in vitro study options for your next
drug development program. 


Are you looking to incorporate more non-animal testing options into your drug development program?  Know that in vitro assays are an essential component of the data package required in support of an investigational new drug. Labcorp is ready to conduct these quick studies to help you assess the drug metabolism and pharmacokinetic (DMPK) aspects of your test article as well as potential drug-drug interactions. Let’s discuss your in vitro options today.  

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.

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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.

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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.

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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.

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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.

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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.

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Regulatory guidance resources

    FDA

    In Vitro Drug Interaction Studies - Cytochrome P450 Enzyme- and Transporter-Mediated Drug Interactions Guidance for Industry
    Center for Drug Evaluation and Research (CDER) 2020.

    EMA

    Guideline on the Investigation of Drug Interactions. 
    Committee for Human Medicinal Products (CHMP) Rev 1, 2015.

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