Clinical-stage biopharmaceutical company Iterion Therapeutics reported on Wednesday that the first patient has been dosed at HonorHealth Research Institute in a phase 1/2 clinical trial evaluating tegavivint, a first-in-class, small molecule inhibitor of the Wnt/beta-catenin pathway, for the treatment of metastatic colorectal cancer (mCRC).

This expands Iterion's clinical development into mCRC, a disease with significant unmet need and limited progress in developing targeted therapies.

Tegavivint is a small-molecule inhibitor of TBL1, a transcriptional co-factor required for oncogenic beta-catenin signalling. By selectively disrupting the TBL1/beta-catenin transcriptional complex, tegavivint promotes degradation of nuclear beta-catenin and suppresses beta-catenin-dependent gene transcription, inhibiting Wnt-driven tumour growth while avoiding the dose-limiting toxicities historically associated with upstream Wnt inhibition.

Rahul Aras, PhD, president and CEO of Iterion Therapeutics, said: "The mCRC study builds on the encouraging clinical benefit we're observing in patients with advanced hepatocellular carcinoma, including partial responses and durable disease control in heavily pre-treated patients. The level of monotherapy activity observed with tegavivint in complex solid tumours is unprecedented for a Wnt/beta-catenin pathway inhibitor and we're excited to expand development into other hard-to-treat Wnt-driven cancers."