Comprehensive in vitro approach to evaluate transporter-mediated drug interactions in drug discovery

In this on-demand webinar, an assay strategy to assess transport-mediated drug interactions that complies with regulations is examined.

About this on-demand webinar

Transporters are membrane proteins that facilitate cross-membrane movement of ions or molecules, including endogenous or exogenous substances, such as toxins and drugs. They are expressed in different organs throughout the human body and control the access of endogenous and exogenous substances to various sites in the body. The interaction of investigational drugs with transporters may lead to clinically-relevant drug interactions with concomitant drugs. Therefore, in vitro evaluation of investigational drug and drug transporter interaction is an essential assessment.

Transporters that are involved in drug absorption, distribution and elimination belong to two categories: ATP Binding Cassette (ABC) transporters, such as P-gp and BCRP; and Solute Carrier (SLC) transporters, such as OATP1B1 and OATP1B3 (for hepatic clearance drugs), OAT1, OAT3, OCT2, MATE1 and MATE2-K (for renal clearance drugs). It is recommended by regulatory agencies that the potential of an investigational drug to be either an inhibitor (perpetrator) or a substrate (victim) of drug transporters is evaluated to determine the drug interaction profile of the investigational drug. All the above-mentioned transporters are recommended for the inhibition evaluation of investigational drugs. P-gp and BCRP are recommended for the substrate assessment of investigational drugs that are not highly permeable and highly soluble. OATP1B1 and OATP1B3 are recommended for substrate assessment of investigational drugs that are mainly cleared through hepatic metabolism or biliary secretion, or when the drug’s uptake into the liver is clinically important. OAT1, OAT3, OCT2, MATE1 and mAte2-k are recommended for substrate assessment of investigational drugs that are mainly cleared through kidneys.

In this on-demand webinar, a comprehensive in vitro approach to evaluating transport-mediated drug interactions in drug discovery is discussed. The assays that evaluate potential inhibition effects and the potential of drug transporter substrates of an investigational drug are introduced. The options of various assays that satisfy regulatory agencies’ recommendations of drug interactions are discussed.

Benefits of this on-demand session

  • Understand the regulatory recommendations on evaluating transporter-mediated drug interactions
  • Explore the comprehensive package of evaluating transporter-mediated drug interactions in drug discovery
  • Learn the detailed assay design and data interpretation of drug transporter inhibition and substrate assays.

Our speaker

Yong ZhaoYong Zhao, Principal Scientist and Study Director, Eurofins Discovery

Dr Zhao is a Principal Scientist and study director of ADME-Toxicology at Eurofins Discovery where he is responsible for all activities relating to the in vitro ADME-Toxicology services. He has over 15 years of industrial drug discovery experience. His main area of expertise is in vitro DDI (Drug-drug Interaction) assessment, high throughput in vitro toxicity assessment in early drug discovery, including assay development and validation.

Prior to joining Eurofins Cerep/Panlabs in 2004, Dr Zhao completed a postdoctoral fellowship at the Department of Pharmacology in the University of Washington. He obtained his PhD at the University of California, Riverside and his MS and BS from Nankai University in Tianjin, China.