Anti-Arrhythmic Hit to Lead Refinement in a Dish using Patient-Derived iPSCs

In the United States, almost one million individuals are hospitalized every year for cardiac arrhythmias, making arrhythmias one of the top causes of healthcare expenditures with a direct cost of almost $50 billion annually. Almost 300,000 individuals die of sudden arrhythmic death syndrome every year.

Medicinal chemists at the Human BioMolecular Research Institute (HBRI), in San Diego, CA, and stem cell biologists at Stanford University, in Stanford, CA, and cardiovascular pharmacologists at UCLA in Los Angeles, CA and Columbia University, in New York City, NY, respectively, reported on reengineered mexiletine compounds that showed improved potency and decreased toxicity in addressing ventricular cardiac arrhythmia.

https://pubs.acs.org/doi/full/10.1021/acs.jmedchem.0c01545

Reengineering a drug guided by patient-derived hiPSC-cardiomyocytes

San Diego, California – September, 2020. Medicinal chemists at the Human BioMolecular Research Institute (HBRI), in San Diego, CA, and biologists at Sanford-Burnham-Prebys Medical Discovery Institute (SBPMDI), in San Diego, CA, and at Stanford University, Stanford, CA, Columbia University, New York, NY, and Northwestern University, Chicago, IL, respectively, have reported on improving an antiarrhythmic drug using patient-derived human induced pluripotent stem cell cardiomyocytes (hiPSC-CMs) in a high throughput manner in vitro. This may have importance for heart disease and other drug discovery efforts.

https://www.cell.com/cell-stem-cell/fulltext/S1934-5909(20)30399-4