CK-3773274, or CK-274, is an investigational, novel, oral, small molecule cardiac myosin inhibitor discovered by company scientists independent of its collaborations, for the potential treatment of hypertrophic cardiomyopathies (HCM).
CK-274 was designed to reduce the hypercontractility associated with HCM. HCM causes the heart to thicken and stiffen, eventually limiting its ability to pump blood. This happens when myosin, a protein in the muscle responsible for converting chemical energy into the mechanical force that causes muscle contraction, is working too hard to grab or pull on actin, another protein within the sarcomere, resulting in hypercontractility, or too many hands pulling on the rope. CK-274 addresses this hypercontractility by blocking some myosins from pulling, resulting in less contraction, or fewer hands on the rope. In preclinical models, CK-274 reversed and reduced thickening and stiffening of the heart.
Preclinical data has shown potential for best-in-class safety and efficacy, and pharmacokinetic projections are consistent with once-daily dosing employing titration to an optimized personalized dose, suggesting ease of use and broad clinical utility.
CK-274 is currently the subject of a Phase 1 clinical trial. Results are expected in the second half of 2019.