TY-0584

TY-0584 is a potent, orally available small molecule inhibitor of the YAP/TEAD transcription factor complex, developed by TYK Medicines. It functions by targeting the palmitoylation of TEAD proteins, thereby disrupting the Hippo/YAP signaling pathway which is frequently hyperactivated in various cancers. Preclinical studies have demonstrated significant anti-tumor activity in models of malignant mesothelioma (particularly those with NF2 loss-of-function mutations) and head and neck cancer. Additionally, TY-0584 has shown synergistic effects when combined with third-generation EGFR inhibitors like TY-9591 in non-small cell lung cancer (NSCLC) models, potentially overcoming resistance to EGFR-targeted therapies. As of early 2023, the compound was in the IND-enabling stage of development.