eSeminar: Challenges in Assessing Mitochondrial Toxicities and Liabilities in Drug Discovery

14. 11. 2018

De-risk Your Drug Pipeline. Learn how Genentech is advancing the state of the art in mitochondrial liability assessment.
Early identification of compounds that induce mitochondrial toxicities is an important part of lead-optimization during drug discovery. While cell-based assays (e.g. glucose-galactose switch assay) are commonly employed in the discovery space, they suffer from both technical and sensitivity issues. As such, assays that measure drug-related effects on mitochondrial respiration have gained interest from industry due to their increased sensitivity. We will outline here the thresholding and other qualification measures we employ to the Agilent cell-based respiration assays and how this information, in addition to complementary data from respiration studies using isolated rat liver mitochondria, informs preclinical risk assessment.
In this webinar we will discuss:
The state of the science in mitochondrial toxicity assessment,
How Genentech employs these assays to support small-molecule lead optimization and issue mitigation, and
A cross-comparison of popular assays using a test set of commercial
drugs with known clinical toxicities.

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