Belnacasan is a prodrug of VRT-043198
, a caspase-1 inhibitor that was developed by Vertex. Pharmacological inhibition of caspase-1 is being investigated as a mechanism to reduce pro-inflammatory cytokine (predominantly IL-1β) production as a novel treatment of inflammatory diseases [1
]. Inhibition of caspase-1 is a small molecule strategy developed as an alternative to the use of anti-IL-1β neutralising antibodies, such as canakinumab
, or the dimeric fusion protein rilonacept
that acts as a IL-1 trap.