zamaporvint

Zamaporvint (RXC004) is a potent, selective, orally available small molecule inhibitor of the membrane-bound O-acyltransferase Porcupine (PORCN), an essential enzyme for Wnt ligand secretion and activation of the Wnt signaling pathway. By inhibiting PORCN, zamaporvint blocks both canonical and non-canonical Wnt signaling pathways implicated in cancer initiation, progression, immune evasion, and resistance to therapies such as immune checkpoint inhibitors. The drug has demonstrated dual mechanisms of action—directly inhibiting tumor cell growth in genetically defined cancers with upstream Wnt pathway alterations (such as RNF43 loss-of-function mutations or RSPO fusions) and enhancing anti-tumor immunity by reducing immunosuppressive cells within tumors. Zamaporvint is being developed primarily for genetically selected solid tumors including microsatellite stable metastatic colorectal cancer (MSS mCRC), biliary tract cancer, and pancreatic cancer[1][3][5][6].

Brand names

zamaporvint

Other names

porcupine inhibitor RXC004