Tirasemtiv

An activator of the fast skeletal troponin complex; selectively binds to purified fast skeletal troponin complex (Kd = 40 nM) over slow skeletal (Kd = 3,800 nM) and cardiac troponin complexes; slows the rate of calcium release from the fast skeletal troponin complex at 20 μM; increases the ATPase activity of isolated rabbit fast skeletal myofibrils at a fixed calcium concentration (EC50 = 390 nM); sensitizes skinned fast skeletal muscle fibers isolated from human and rabbit to calcium; increases in situ EDL muscle force and forelimb grip strength in a rat model of myasthenia gravis; increases forelimb grip strength, grid hang test performance, and rotarod performance in a mouse model of ALS at 10 mg/kg