Iterion Therapeutics Announces First Patient Dosed in Clinical Study of Tegavivint, a First-in-Class Wnt/β-Catenin Inhibitor, in Relapsed/Refractory Osteosarcoma

Tegavivint Is the First Wnt/β-Catenin Inhibitor to Demonstrate Tolerability and Monotherapy Clinical Activity in Complex Solid Tumors

Osteosarcoma Program Builds on Clinical Benefit observed in Lead Indication of Advanced Hepatocellular Carcinoma

HOUSTON, Feb. 10, 2026 /PRNewswire/ -- Iterion Therapeutics, a clinical-stage, biopharmaceutical company dedicated to revolutionizing the treatment of Wnt-driven cancers, today announced that the first patient has been dosed in a clinical study evaluating tegavivint, a first-in-class inhibitor of the Wnt/β-catenin pathway, in combination with gemcitabine for patients with relapsed or refractory osteosarcoma. The trial is sponsored by Emory University, conducted at the Aflac Cancer and Blood Disorders Center of Children's Healthcare of Atlanta and supported by funding from the Peach Bowl LegACy Fund, reflecting strong academic, clinical and philanthropic commitment to advancing new therapies for this rare pediatric cancer.

Osteosarcoma is the most common malignant bone tumor in children and adolescents, and outcomes following relapse remain poor. A growing body of research has shown that Wnt/β-catenin signaling is highly active in relapsed and metastatic osteosarcoma, where it is associated with tumor progression, treatment resistance, and metastasis.

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

"Tegavivint represents a novel approach to targeting one of the central biological drivers of osteosarcoma," said Rahul Aras, PhD, President and CEO of Iterion Therapeutics. "This first patient dosed marks an important clinical milestone for a program supported by extensive biological validation and reinforces the broader value of our Wnt/β-catenin platform."

Tegavivint has already demonstrated favorable tolerability, pharmacodynamic activity, and encouraging monotherapy clinical responses in Company-sponsored clinical trials in hepatocellular carcinoma and desmoid tumors, two diseases driven by aberrant Wnt/β-catenin signaling. In addition, a Children's Oncology Group (COG)-led study conducted through the National Cancer Institute has established the safety of tegavivint across a broad pediatric population, providing a strong foundation for advancement into disease-focused combination studies in osteosarcoma.

"Tegavivint is uniquely positioned for osteosarcoma because it targets a pathway that is consistently active in high-risk and relapsed disease," said Thomas Cash, MD, Principal Investigator of the study at the Aflac Cancer and Blood Disorders Center and Associate Professor of Pediatrics at Emory University. "Evaluating tegavivint in combination with gemcitabine allows us to build on a strong scientific foundation as we seek to improve outcomes for patients with limited treatment options."

Tegavivint has received both Orphan Drug Designation and Pediatric Rare Disease Designation from the U.S. Food and Drug Administration for the treatment of osteosarcoma.

About Iterion Therapeutics
Iterion Therapeutics is a clinical-stage oncology company developing first-in-class therapies that target cancers driven by aberrant Wnt/β-catenin signaling. The Company's lead asset, tegavivint, is the first and only small-molecule inhibitor of TBL1, a critical transcriptional regulator required for nuclear β-catenin stability and oncogenic gene expression. Tegavivint has demonstrated clinical tolerability, target engagement, and monotherapy activity in multiple complex solid tumors, including advanced hepatocellular carcinoma, positioning Iterion at the forefront of Wnt/β-catenin drug development.

Iterion is advancing a focused clinical strategy anchored by its lead program in hepatocellular carcinoma, with expansion into additional Wnt-driven cancers, including pediatric and rare oncology indications where Wnt/β-catenin signaling represents a validated disease driver. The Company has received $26 million in Product Development Awards from the Cancer Prevention and Research Institute of Texas (CPRIT) and continues to build a pipeline of differentiation-driven clinical opportunities around its proprietary Wnt/β-catenin platform. For more information on Iterion, please visit  www.iteriontherapeutics.com.

Investor Contact:
Laurence Watts
[email protected]

Media Contact:
Ryan Walker
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SOURCE Iterion Therapeutics