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ETC-539

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

Overview

ETC-539 is a preclinical-stage small molecule inhibitor of Porcupine (PORCN), a membrane-bound O-acyltransferase (MBOAT) located in the endoplasmic reticulum that is essential for the post-translational palmitoylation and secretion of Wnt ligands. Developed by the Experimental Therapeutics Centre (ETC) in Singapore and Duke-NUS Medical School, ETC-539 targets the Wnt-beta-catenin signaling pathway, which is frequently aberrantly activated in various cancers. In preclinical studies, ETC-539 has demonstrated favorable oral pharmacokinetic properties and significant antitumor efficacy in mouse models of Wnt-driven cancers, including orthotopic murine MMTV-Wnt1 breast tumors and human HPAF-II pancreatic cancer xenografts.

Targets

PORCN (Porcupine protein)

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