RP3128

RP3128 is a novel, orally available small molecule modulator and inhibitor of the calcium release-activated calcium (CRAC) channel. It is being developed primarily for the treatment of autoimmune and inflammatory diseases, including asthma. The drug acts by inhibiting CRAC channels (notably Orai1), which play a key role in immune cell activation and inflammation. Preclinical studies have shown nanomolar potency in various models of inflammation, and first-in-human clinical trials demonstrated that RP3128 was well tolerated with no dose-limiting toxicities observed at single or multiple doses. Pharmacodynamic effects included reductions in plasma levels of pro-inflammatory cytokines such as tumor necrosis factor-alpha (TNFα) and interleukin-4 (IL-4). Chemically, it is described as a pyridyl-substituted benzamide[1][2][5][7].