rimacalib

Rimacalib (SMP-114) is an orally bioavailable small molecule inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII), with IC50 values ranging from approximately 1 μM for CaMKIIα to about 30 μM for CaMKIIγ. It has been investigated primarily as a disease-modifying anti-rheumatic drug (DMARD) in rheumatoid arthritis and malignant rheumatoid arthritis. Rimacalib acts by inhibiting CaMKII activity, which plays a central role in inflammatory signaling and cardiac calcium handling. In addition to its anti-inflammatory effects, rimacalib reduces sarcoplasmic reticulum (SR) calcium leak in cardiomyocytes and has shown potential to suppress arrhythmogenic events without impairing contractility or relaxation. Clinical development reached phase II trials for rheumatoid arthritis; however, these studies were terminated before completion[1][3][4][5][6][7][8].

Other names

rimacalib215174-50-8BZ76J3N815BZ-76J3N815BZ 76J3N815