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.