KY0135

KY0135 is an orally bioavailable small molecule inhibitor of Porcupine (PORCN), a membrane-bound O-acyltransferase essential for the palmitoylation and subsequent secretion of Wnt ligands. Developed by Jiangsu Kanion Pharmaceutical, KY0135 is designed to target the Wnt/β-catenin signaling pathway, which is frequently dysregulated in various malignancies and contributes to tumor growth, stemness, and immune evasion. By inhibiting PORCN, the drug prevents the maturation and release of Wnt proteins, thereby suppressing downstream signaling. KY0135 is currently being evaluated in Phase I clinical trials in China for the treatment of advanced or metastatic solid tumors, particularly those harboring Wnt/β-catenin pathway alterations, including gastric, colorectal, and pancreatic cancers.