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.
Authors
- Erin G. Roberts (ORCID: https://orcid.org/0000-0001-8985-8799)
- Kevin D. Costa (ORCID: https://orcid.org/0000-0003-4594-3742)
- Andy O.T. Wong
- Yuki Kurokawa (ORCID: https://orcid.org/0000-0001-5665-4829)
- Ronald A. Li
- Reza Aghavali
- E. Mak
- Martin Y C Chan
Institutions
- 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)
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
Funders
- Innovation and Technology Commission - Hong Kong