The Journal of Medicinal Chemistry recently publishes an article titled, “Discovery of Nelutroctiv (CK-136), a Selective Cardiac Troponin Activator for the Treatment of Cardiovascular Diseases Associated with Reduced Cardiac Contractility”. Heart failure (HF) is a lifelong clinical syndrome and remains a major societal concern. Cardiac myosin activators constitute a new class of inotropes and are found to be a viable therapeutic approach for increasing myocardial contractility.
CK-136 is a small molecule cardiac troponin activator that is discovered under a previous joint research program between Cytokinetics and Amgen. It acts on the sarcomere and is designed to improve myocardial contractility by sensitizing cardiac troponin to calcium, increasing actin-myosin cross bridge formation during each cardiac cycle. CK-136 is developed as a potential treatment for heart failure (HF) with reduced ejection fraction (HFrEF) and other types of heart failure, and currently under phase 1 clinical investigation.