RP4010

RP4010 is a novel first-in-class oral small molecule inhibitor targeting the calcium release-activated calcium (CRAC) channel pathway, specifically inhibiting store-operated calcium entry (SOCE) via blockade of the ORAI1 channel. By binding to and inhibiting CRAC channels, RP4010 prevents extracellular Ca2+ influx into cells, thereby suppressing downstream Ca2+-mediated signaling pathways. This inhibition leads to reduced activation of transcription factors such as NFAT and NF-κB, decreased cell proliferation through cell cycle arrest at G0/G1 phase, and impaired tumor growth in various cancer models including pancreatic ductal adenocarcinoma, esophageal squamous cell carcinoma (ESCC), gastrointestinal cancers, and acute myeloid leukemia. Preclinical studies have demonstrated that RP4010 can act synergistically with standard chemotherapeutic agents and has shown activity in both in vitro and in vivo cancer models[1][3][4][5][6].