Enhanced drug classification using machine learning with multiplexed cardiac contractility assays

Cardiac screening of newly discovered drugs remains a longstanding challenge for the pharmaceutical industry. While therapeutic efficacy and cardiotoxicity are evaluated through preclinical biochemical and animal testing, 90 % of lead compounds fail to meet safety and efficacy benchmarks during human clinical trials. A preclinical model more representative of the human cardiac response is needed; heart tissue engineered from human pluripotent stem cell derived cardiomyocytes offers such a platform. In this study, three functionally distinct and independently validated engineered cardiac tissue assays are exposed to increasing concentrations of known compounds representing 5 classes of mechanistic action, creating a robust electrophysiology and contractility dataset. Combining results from six individual models, the resulting ensemble algorithm can classify the mechanistic action of unknown compounds with 86.2 % predictive accuracy. This outperforms single-assay models and offers a strategy to enhance future clinical trial success aligned with the recent FDA Modernization Act 2.0.

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Publication Details

Journal
Pharmacological Research
Published
2024-10-11
DOI
https://doi.org/10.1016/j.phrs.2024.107459
Citations
2
Primary Topic
Computational Drug Discovery Methods
Type
article
Field-Weighted Citation Impact
0.72

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article

Enhanced drug classification using machine learning with multiplexed cardiac contractility assays

Erin G. Roberts, Kevin D. Costa, Andy O.T. Wong, Yuki Kurokawa et al.
2 citations
Pharmacological Research
Computational Drug Discovery Methods
0.72
article

Enhanced drug classification using machine learning with multiplexed cardiac contractility assays

Erin G. Roberts, Kevin D. Costa, Andy O.T. Wong, Yuki Kurokawa, Ronald A. Li, Reza Aghavali, E. Mak, Martin Y C Chan
article en
2 citations

Abstract

Cardiac screening of newly discovered drugs remains a longstanding challenge for the pharmaceutical industry. While therapeutic efficacy and cardiotoxicity are evaluated through preclinical biochemical and animal testing, 90 % of lead compounds fail to meet safety and efficacy benchmarks during human clinical trials. A preclinical model more representative of the human cardiac response is needed; heart tissue engineered from human pluripotent stem cell derived cardiomyocytes offers such a platform. In this study, three functionally distinct and independently validated engineered cardiac tissue assays are exposed to increasing concentrations of known compounds representing 5 classes of mechanistic action, creating a robust electrophysiology and contractility dataset. Combining results from six individual models, the resulting ensemble algorithm can classify the mechanistic action of unknown compounds with 86.2 % predictive accuracy. This outperforms single-assay models and offers a strategy to enhance future clinical trial success aligned with the recent FDA Modernization Act 2.0.

Pharmacological ResearchVol. 209
Novia University of Applied Sciences (FI), PTC (United States) (US), Boston De Novo Design (United States) (US), Micro Focus (United States) (US), Novelis (Canada) (CA), National Oilwell Varco (United States) (US)
Innovation and Technology Commission - Hong Kong
Openalex Percentile: Top 25%
Computational Drug Discovery Methods
0.72
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