Iterion Therapeutics Announces Initiation of Phase 1 Clinical Trial to Study Tegavivint in Combination with Osimertinib in Epidermal Growth Factor Receptor-Positive Non-Small Cell Lung Cancer

HOUSTON, Dec. 9, 2021 /PRNewswire/ -- Iterion Therapeutics, Inc., a venture-backed, clinical-stage biotechnology company developing novel cancer therapeutics, today announced the initiation of a Phase 1 clinical trial to investigate tegavivint in a first-line combination study with osimertinib in previously untreated patients with metastatic epidermal growth factor receptor (EGFR)-positive Non-Small Cell Lung Cancer (NSCLC). Tegavivint is a potent and selective first-in-class small molecule inhibitor of Transducin beta-like Protein One (TBL1), a novel downstream target in the Wnt/beta-catenin signaling pathway. The trial (NCT04780568) is sponsored by The Ohio State University Comprehensive Cancer Center - Arthur G. James Cancer Hospital and Richard J. Solove Research Institute (OSUCCC - James), and led by Regan M. Memmott, M.D., Ph.D., an OSUCCC – James oncologist.

An important clinical challenge with EGFR-TKIs (tyrosine kinase inhibitors), including osimertinib, is that while such drugs are recommended as first line therapy in metastatic EGFR-positive NSCLC, this class of drugs enriches for "drug-tolerant persister cells" (DPCs), resulting in the eventual development of resistance. Researchers at OSUCCC - James determined that enrichment of DPC's by osimertinib is driven by activation of beta-catenin, and further demonstrated that administration of tegavivint in combination with osimertinib prevented osimertinib-induced enrichment of DPCs. Use of this combination also showed deeper anti-tumor responses and prolonged overall survival in mouse models of EGFR-mutant NSCLC.¹

"For the estimated 15-30% of patients in the U.S. who have EGFR-positive NSCLC, treatment with EGFR-TKIs, such as osimertinib, has been shown to be very effective, but unfortunately patients will relapse as a result of their tumors eventually developing resistance," said Dr. Memmott, principal investigator for the study. "Research conducted at OSUCCC – James suggests that combining tegavivint with osimertinib could curtail the osimertinib-induced drug-tolerant persister cells from developing due to tegavivint's ability to act as a beta-catenin inhibitor via TBL1 inhibition.  This new Phase 1 clinical trial evaluates osimertinib in combination with tegavivint as a potential first-line treatment for EGFR-positive NSCLC, which is exciting in a disease that is the No. 1 cause of cancer-related death in the United States."

"We are excited to collaborate with OSUCCC and the National Cancer Institute to initiate this Phase 1 first-line study of tegavivint in combination with osimertinib in previously untreated patients with metastatic EGFR-mutant NSCLC," said Rahul Aras, Ph.D., CEO of Iterion. "NSCLC is the most common type of lung cancer, accounting for 85% of all lung cancer diagnoses, according to the American Society of Clinical Oncology (ASCO). This trial has the potential to help this enormous patient population and to further demonstrate tegavivint's unique mechanism of action of TBL1 inhibition, thereby disrupting the oncogenic activity of beta-catenin. Tegavivint has already demonstrated safety in desmoid tumor patients and is currently being investigated in additional clinical trials as a potential treatment for acute myeloid leukemia and solid and hematologic pediatric tumors."

This Phase 1 clinical trial is funded by Pelotonia, a Columbus-based organization that has raised more than $236 million for cancer research conducted at the OSUCCC – James, and the V Foundation.

About Ohio State University Comprehensive Cancer Center - Arthur G. James Cancer Hospital and Richard J. Solove Research Institute (OSUCCC - James)
OSUCCC is one of 51 National Cancer Institute (NCI)-designated Comprehensive Cancer Centers and one of only a few centers funded by the NCI to conduct both Phase 1 and Phase 2 clinical trials on novel anticancer drugs sponsored by the NCI. The James at Brain and Spine Hospital has been ranked one of the top cancer hospitals in the nation by U.S. News & World Report and has achieved Magnet® designation, the highest honor an organization can receive for quality patient care and professional nursing practice.

About Iterion Therapeutics
Iterion Therapeutics is a venture-backed, clinical stage biotechnology company developing novel cancer therapeutics. The company's lead product, tegavivint, is a potent and selective small molecule that binds to TBL1 in the nucleus inhibiting nuclear beta-catenin signaling and oncogenic activity. Research demonstrating potent anti-tumor activity in a broad range of pre-clinical models indicate that tegavivint has the potential for clinical utility in multiple cancer types. Currently, tegavivint is the subject of three separate clinical trials: a Phase 1 clinical trial sponsored by MD Anderson Cancer Center in patients with relapsed or refractory acute myeloid leukemia (AML); a Phase 1/2 clinical trial sponsored by Children's Oncology Group Pediatric Early Phase Clinical Trials Network in pediatric patients with sarcomas, lymphomas and other solid tumors, excluding central nervous system (CNS) tumors; and a Phase 1 clinical trial sponsored by Ohio State University Comprehensive Cancer Center in EGRF-positive non-small cell lung cancer (NSCLC). Data from a prior Phase 1/2a clinical trial of tegavivint in patients with progressive desmoid tumors demonstrated safety and preliminary clinical efficacy. Iterion is the recipient of an up to $15.9 million Product Development Award from the Cancer Prevention and Research Institute of Texas (CPRIT). For more information on Iterion, please visit https://iteriontherapeutics.com.

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SOURCE Iterion Therapeutics