On June 1, 2022 Iterion Therapeutics, Inc., a venture-backed, clinical-stage biotechnology company developing novel cancer therapeutics, reported that results from a Phase 1 study of tegavivint in patients with desmoid tumors will be featured in a poster presentation and discussion session at the 2022 American Society of Clinical Oncology (ASCO) (Free ASCO Whitepaper) Annual Meeting (ASCO 2022) (Press release, Iterion Therapeutics, JUN 1, 2022, View Source [SID1234615391]). ASCO (Free ASCO Whitepaper) 2022 is being held June 3-7, 2022, in Chicago, Illinois.
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Tegavivint is a potent and selective first-in-class small molecule inhibitor of Transducin Beta-like Protein One (TBL1), a novel downstream co-factor in the Wnt/beta-catenin signaling pathway. Increased expression of beta-catenin and TBL1 are associated with metastasis and poor prognosis in a broad range of tumor types. Tegavivint’s targeting of TBL1 prevents TBL1/beta-catenin complex formation, specifically inhibiting beta-catenin’s oncogenic transcriptional activity without disrupting key cell membrane functions that have been linked to toxicity common to other drugs in this pathway.
The poster, titled, "Results of a phase I dose escalation study of a tegavivint (BC2059), a first-in-class TBL1 inhibitor for patients with progressive, unresectable desmoid tumors," will be presented on Sunday, June 5, 2022, at 11:30 a.m., CDT, during the Sarcoma session (poster number 428; abstract number 11523) by Lee D. Cranmer, M.D., Ph.D., F.A.C.P., principal investigator of the trial. The poster details results from the Phase 1 trial in adult patients with progressive, unresectable desmoid tumors. The primary objectives of the study were to evaluate safety and to determine the maximum tolerated dose (MTD), the recommended Phase 2 dose (RP2D), and exploratory efficacy. No dose-limiting toxicities were observed and a maximum tolerated dose (MTD) was not determined. Treatment related adverse events were mostly Grade 1-2 with none resulting in treatment discontinuation. The RP2D was declared at 5 mg/kg based on pharmacologically relevant plasma concentrations and preliminary efficacy. Responses were observed at all dose levels with an overall response rate of 25% at the RP2D. Additionally, the 9 month progression free survival rate was 79% among those treated at the RP2D. Overall, these data demonstrated that tegavivint is well tolerated, does not appear to have the toxicity historically associated with WNT inhibition, and has promising clinical activity.
"The data presented at ASCO (Free ASCO Whitepaper) complements research presented earlier this year at AACR (Free AACR Whitepaper), which cumulatively demonstrate the safety, tolerability and clinical activity of tegavivint in the treatment of desmoid tumors," said Rahul Aras, PhD, CEO of Iterion. "We are particularly excited to present these results at ASCO (Free ASCO Whitepaper), the world’s preeminent oncology conference, because the data also serve to highlight the potential of our ongoing tegavivint programs in AML, non-small cell lung cancer, and pediatric solid tumors. These cancer indications, like desmoid tumors, are associated with nuclear beta-catenin overexpression, which has historically been considered undruggable. We believe tegavivint’s unique mechanism of action provides an opportunity to selectively disrupt the interaction of beta-catenin and TBL1, which in turn, allows for the specific degradation of nuclear beta-catenin without impacting key cell membrane functions that have been linked to previously reported toxicity."