ETC-159

ETC-159 is a potent, orally available small molecule inhibitor of the membrane-bound O-acyltransferase porcupine (PORCN), an enzyme essential for the palmitoleation and secretion of Wnt ligands. By inhibiting PORCN, ETC-159 blocks Wnt signaling—a pathway implicated in the growth and survival of various cancers, particularly those with aberrant Wnt activation such as colorectal cancer with R-spondin fusions, endometrial, ovarian, pancreatic cancers, and osteosarcoma. Preclinical studies have shown that ETC-159 reduces β-catenin activity and tumor vascularity while increasing tumor necrosis. Clinical trials have demonstrated its safety as monotherapy and in combination with pembrolizumab (an immune checkpoint inhibitor), showing preliminary clinical benefit in patients with advanced or metastatic solid tumors—especially microsatellite stable (MSS) populations[1][4][5][6].

Other names

ETC 1922159ETC1922159ETC-1922159