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Recent Advances in Transporter Testing Strategies Enable Effective Identification of Potential Drug-Drug Interactions



October 17, 2017
11 am to 12 pm EDT

 

Sponsored by
Eurofins Pharma Discovery Services Logo

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Webinar Description:

Understanding the Absorption, Distribution, Metabolism, Excretion (ADME) and Pharmacokinetics (PK) properties of your compound(s) is essential for selecting candidates with desirable profiles for later stages of drug development. In the liver, the phase I (e.g. cytochrome P450’s) and phase II (e.g. GSTs and UGTs) metabolizing enzymes are responsible for the majority of drug metabolism that occurs in the body. Additionally, transporter proteins can play a significant role in the uptake and/or efflux of a drug in key organs of the body important for drug absorption, distribution, metabolism and excretion.

Many drugs interact with metabolizing enzymes and transporters, by inhibiting their enzymatic activity (e.g. CYP inhibition), through activation of nuclear receptors leading to induction of their gene expression (CYP induction) or being a substrate and/or inhibitor of transporter proteins. Drug-drug interactions (DDI) can occur when one drug affects the ADME and PK properties of another simultaneously administered drug(s) by altering the activities of drug metabolizing enzymes and/or drug transporters.

With an increase in both life expectancies and the number of patients who are simultaneously taking multiple medications to treat one or more conditions, the potential for clinically relevant DDIs is becoming an increasing concern for drug developers, regulatory agencies, and physicians. While the in vitro assessment of DDIs related to drug metabolizing enzymes, such as cytochromes P450 (CYPs), are well-established, in vitro assays to study DDIs related to drug transporters are still evolving.

Eurofins Pharma Discovery Services offers robust inhibition and substrate assays to allow quick and cost-effective screening of drug candidates for their interactions with the major drug transporters in the ABC (ATP-binding cassette) and SLC (solute-carrier) families. In this webinar we will discuss strategies and methods for assessing these transporter interactions and the benefits for including these studies in a drug development program. We will also discuss how drug transporter assays fit into a broader DDI profile which includes assays such as CYP inhibition, CYP induction, CYP phenotyping, UGT inhibition, and UGT phenotyping, all of which are recommended by regulatory agency guidance documents in the evaluation of new drug candidates for potential DDIs.

Learning Objectives:

  • Understand the significant role that metabolizing enzymes and transporter proteins play in the absorption, distribution, elimination and toxicity of drugs.
  • Gain greater insights into the important role transporters play in drug-drug interactions (DDI).
  • Become familiar with the in vitro assays recommended by regulatory agency guidance documents for assessing potential drug-drug interactions for new drug candidates.
  • Learn about the evolution of transporter testing and the variety of industry standard in vitro transporter assays and formats used to screen for potential drug-transporter interactions.

Speaker:

Kevin Kennedy Ph.D.

Principal Scientist, Director of ADME-PK

Eurofins Pharma Discovery Services

Dr. Kennedy has over 10 years of experience in ADME and Transporter applications, sample-preparation techniques and the development of LC/MS methodology for the analysis of small-molecule and peptide therapeutics. His expertise in the application of high-resolution mass spectrometry for the detection and characterization of drug metabolites and other analytes is important for the development and application of in vitro ADME and transporter assays. Dr. Kennedy holds a Ph.D. in Pharmaceutical Science from the Medical University of South Carolina and a B.Sc. in Biological Sciences from Cornell University. He is currently Principal Scientist and Group Leader for ADME services at Eurofins Pharma Discovery Services in St Charles, MO.



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