MDR3cyte® is a fully-validated assay format that characterizes MDR3 inhibition by a test agent using primary hepatocytes in suspension. This platform is metabolically competent and retains biological functions. The assay involves in situ biosynthesis of deuterium (d9)-labeled PC, activation of MDR3 by bile salt micelles and LC-MS/MS determination of transported extracellular d9-PC. The profile of PCs produced using the MDR3cyte® assay platform and human hepatocyte more accurately reflects the profile found in natural human bile. MDR3 inhibition is associated with most DILI-concern drugs.
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Drug-induced liver injury (DILI) accounts for >50% acute liver failures, and is the leading cause of drug development failure, boxed warning and market withdrawal of approved drugs. Inhibition of BSEP and MDR3 is one of the underlying mechanisms for DILI. BSEP and MDR3 are the primary hepatic transporters responsible for exporting bile salts and phosphatidylcholine, respectively. In humans, inhibition of BSEP and/or MDR3 can result in serious liver injury. This presentation will discuss our patented platforms BSEPcyte® and MDR3cyte® using primary hepatocytes in suspension for higher throughput assessment of DILI potentials. In addition, a brief review of the critical transporter studies to inform DDI potentials will also be discussed. This presentation will benefit scientists wanting to learn more about DILI and/or those needing guidance on crucial transporter studies for better assessment of DDI potentials that is aligned with regulatory guidance.