DioTree is developing first-in-class small-molecule inhibitors of DIO3, a novel therapeutic target in high-grade serous carcinoma
OUR TECHNOLOGY
Targeting DIO3 to restore thyroid-hormone signaling in cancer
DioTree is developing a novel class of small-molecule inhibitors targeting type 3 deiodinase (DIO3), an enzyme highly expressed in several aggressive cancers, including high-grade serous carcinoma (HGSC). DIO3 inactivates thyroid hormones within tumor cells, reducing intracellular T3 and supporting cellular programs associated with tumor growth, survival and distorted metabolism. Our proprietary DIO3 inhibitors are designed to block this process, restore intracellular T3 signaling and reactivate anti-cancer effects.
Protected by granted U.S. and European patents - US10,435,365 B2 | EP3119768B1
PRECLINICAL EFFICACY
Across multiple high-grade serous carcinoma mouse models, DIO3i demonstrated substantial antitumor activity. In the metastatic OVCAR8-LUC model, daily dosing at 50mg/kg achieved 100% tumor growth inhibition (TGI). Additional xenograft models similarly achieved significant tumor inhibition.
100% TGI in an OVCAR8-LUC ovarian cancer model, with longitudinal IVIS imaging
