ETS-003

ETS-003 is a potent, selective, and orally available small molecule inhibitor of the protein-protein interaction (PPI) between YAP/TAZ and TEAD transcription factors, developed by ETERN Biopharma. It specifically targets the Ω loop site of TEAD1, disrupting the Hippo signaling pathway which is frequently dysregulated in various cancers. By preventing the formation of the YAP/TAZ-TEAD complex, ETS-003 inhibits the transcription of genes that drive cell proliferation, survival, and tumor microenvironment remodeling. Preclinical data presented at AACR 2023 demonstrated broad anti-tumor activity across multiple solid tumor cell lines and significant efficacy in mesothelioma models. Furthermore, ETS-003 has shown potential in combination therapies with MAPK pathway inhibitors such as osimertinib, sotorasib, and MRTX1133.