On April 13, 2026 Iterion Therapeutics reported that two abstracts featuring its first-in-class TBL1 inhibitor, tegavivint, will be presented at the 2026 American Association for Cancer Research (AACR) (Free AACR Whitepaper) Annual Meeting. Each will highlight the company’s approach to targeting the Wnt/β-catenin pathway, one of the most frequently dysregulated signaling programs in cancer.

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Despite its role in an estimated 25–30% of solid tumors, the Wnt/β-catenin pathway has historically proven difficult to target therapeutically. Earlier efforts focused on inhibiting upstream components of the pathway and were often limited by bone and gastrointestinal toxicities.

Tegavivint takes a differentiated approach by targeting TBL1, a transcriptional regulator required for β-catenin–mediated gene expression. By disrupting the TBL1–β-catenin transcriptional complex, tegavivint promotes degradation of nuclear β-catenin, inhibits oncogenic transcriptional programs driven by Wnt signaling, and has demonstrated potent anti-tumor activity in preclinical models and clinical studies.

"These data further support our strategy of targeting TBL1 as a novel approach to treating Wnt-driven cancers," said Rahul Aras, Ph.D., President and Chief Executive Officer of Iterion Therapeutics. "As clinical momentum builds in hepatocellular carcinoma and our program expands into colorectal cancer and pediatric osteosarcoma, we see the potential for tegavivint to play an important role across multiple cancers where Wnt signaling drives disease."

Iterion recently completed a Phase 1 study of tegavivint in patients with advanced hepatocellular carcinoma (HCC), where the therapy demonstrated encouraging clinical responses and durable disease control in heavily pre-treated patients, along with a favorable tolerability profile. Detailed results from the study are expected to be presented at a scientific conference later this year as the company prepares to advance tegavivint into Phase 2 development in HCC.

The two presentations highlight both the mechanistic basis of tegavivint’s activity and its emerging potential across multiple Wnt-driven cancers.

Building on a recently initiated Phase 1 clinical study in colorectal cancer, one presentation describes the activity of tegavivint in Wnt-driven colorectal cancer models, demonstrating potent anti-tumor activity in preclinical models characterized by activation of the Wnt/β-catenin pathway. These findings support the continued clinical development of tegavivint and exploration of combination strategies in colorectal and other cancers.

A second presentation further characterizes the mechanism of action of tegavivint and the characterization of TBL1 as a druggable therapeutic target within the Wnt/β-catenin pathway. The work highlights how targeting TBL1 can selectively disrupt β-catenin–dependent transcriptional activity and supports the broader potential of this approach across Wnt-driven cancers.

AACR Presentation Details

Poster 1: Tegavivint, a first-in-class TBL1 inhibitor demonstrates potent activity in WNT-driven colorectal cancers
Presenter: Stephen Horrigan, Ph.D., Chief Scientific Officer
Session Title: CL07.02 – Molecular Targeted Therapy
Abstract Number: 3900/6
Date / Time: Monday April 20th, 2026, 2:00-5:00pm
Location: Section 47
Poster 2: Tegavivint directly targets TBL1 to inhibit β-catenin nuclear oncogenic activity
Presenter: Aundrietta Duncan, Ph.D., Sr. Director of Translational Research and Non-Clinical Development
Session Title: ET05.01 – Mechanisms of Anticancer Drug Action
Abstract Number: 5669/15
Date / Time: Tuesday April 21st, 2:00-5:00pm
Location: Section 12

(Press release, Iterion Therapeutics, APR 13, 2026, View Source [SID1234664320])