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ETC-611

Development stage: Discontinued
Lead developer: Experimental Therapeutics Centre
Modality: Small Molecules
Administration: Oral

Overview

ETC-611 is an orally bioavailable small molecule inhibitor of Porcupine (PORCN), a multi-pass membrane-bound O-acyltransferase (MBOAT) located in the endoplasmic reticulum that is essential for the post-translational palmitoylation and secretion of Wnt ligands. By blocking PORCN, ETC-611 prevents the secretion of mature Wnt proteins, thereby suppressing the activation of the Wnt-beta-catenin signaling cascade and downstream pathways such as mTOR, GSK3, Akt, and PKC. Developed by the Experimental Therapeutics Centre (ETC) in Singapore, ETC-611 has demonstrated significant antitumor efficacy in preclinical models of Wnt-driven cancers, including orthotopic murine MMTV-Wnt1 breast cancer and human HPAF-II pancreatic cancer xenograft models.

Targets

PORCN (Porcupine protein)

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