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Drug-induced liver injury (DILI) is a leading cause of drug failure due to poor translation between traditional preclinical animal models and human clinical outcome. More sophisticated human in vitro cell-based models with multiparametric endpoints are now being developed to improve DILI prediction.

In this review article, we focus on:

  • the evolution of the strategies adopted to improve human hepatotoxicity prediction in drug discovery
  • how companies are addressing translational challenges using human relevant cell-based models
  • a further insight into the key role of human exposure and hepatic drug uptake transporters (e.g., OATPs, OAT2)

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