IK930

IK930 is an orally bioavailable small molecule inhibitor of the Transcriptional Enhancer Associate Domain (TEAD) transcription factors, specifically designed to be selective for TEAD1. Developed by Ikena Oncology, it targets the Hippo signaling pathway by binding to the palmitate-binding pocket of TEAD, which prevents the interaction between TEAD and its transcriptional co-activators, YAP and TAZ. This disruption inhibits the expression of pro-proliferative and pro-survival genes that drive tumor growth in Hippo-pathway-altered cancers. IK930 was primarily evaluated in Phase 1 clinical trials for patients with advanced solid tumors harboring NF2 mutations or YAP/TAZ fusions, including mesothelioma, meningioma, and epithelioid hemangioendothelioma (EHE). Although it demonstrated a favorable safety profile with a lower incidence of kidney toxicity compared to pan-TEAD inhibitors, Ikena Oncology announced the discontinuation of the IK930 program in 2024 to prioritize other pipeline assets.