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Determine your drugs interaction with other drugs

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Metabolism-mediated drug-drug interactions (DDI) refer to simultaneously administered drugs that interfere with each other's absorption, distribution, metabolism, and elimination (ADME) by changing activities of drug metabolizing enzymes and/or drug transporters.

As an example, drug A may inhibit or induce activity of an enzyme(s) or transporter(s) directly or virtual of it being a substrate of these proteins.  As a consequence, another medicine, drug B, that is a substrate of those affected enzymes and transporters will have its PK profiles altered and vise versa.

DDI alters drug's pharmacokinetic (PK) profile and this change in concentration and duration profile may lead to either clinical ineffectiveness or adverse drug reaction in patients that can be severe or fatal. Both the FDA and EMA have issued guidances which recommends that all new drugs be investigated to understand their potential to interact with other drugs.

To address this need, Eurofins provides a wide range of assays to help our clients screen their compounds for drug-drug interactions. Early screening of DDI characteristics of a compound is critical in reducing late-stage failures.

   

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Available DDI Profiling Assays:

  • CYP- and UGT-reaction phenotyping
  • CYP inhibition (reversible and time-dependent) and CYP induction (mRNA level)
  • UGT inhibition
  • P-gp substrate
  • Transporter inhibition

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Figure 1. Investigating the potential for CYP Induction

In vitro CYP3A4 induction from hepatocytes from three donors was measured using 15 compounds with known in vivo or in vitro CYP induction potentials per University of Washington Drug-Drug Interaction Database.