The Importance of In Vitro ADME and Toxicity Studies in Drug Discovery and Development

Understanding the absorption, distribution, metabolism, excretion (ADME), and toxicity (ADME-Tox) of new drugs is a key element of drug discovery. These studies provide insights into the disposition of a pharmaceutical compound in the body, including its safety and efficacy.

Obtaining in vitro ADME-Tox data as early as possible in the drug discovery process has many advantages. For example, the results generated from ADME-Tox studies early in development provide valuable indicators as to whether a compound will have good bioavailability, helping to avoid costly clinical stage failures when drug candidate don’t meet ADME properties or show early signs of being toxic.

One of the key challenges with interpretation of ADME-Tox studies in pre-clinical drug development is identifying the appropriate models that can provide clinically relevant results. While animal models remain one of the most important tools in preclinical ADME-Tox studies, in vitro systems such as culturing primary human cells are becoming increasingly important for decision making in the drug development pipeline.

Below, we outline the use of primary cells, in particular liver cells, in ADME-Tox studies. You can also watch our webinar ‘Hepatocytes in the Drug Development Pipeline’ for more information.

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 1. Guo L, Dial S, Shi L, Branham W, Liu J, Fang J-L, Green B, Deng H, Kaput J, and Ning B. (2011) Similarities and differences in the expression of drug metabolizing enzymes between human hepatic cell lines and primary human hepat1. Guo L, Dial S, Shi L, Branham W, Liu J, Fang J-L, Green B, Deng H, Kaput J, and Ning B. (2011) Similarities and differences in the expression of drug metabolizing enzymes between human hepatic cell lines and primary human hepatocytes. Drug Metabolism and Disposition 39(3): 528-538.