tegavivint (BC2059) / Iterion Therap, Apollomics - LARVOL DELTA

Iterion Therapeutics Announces Promising Phase 1b Data for Tegavivint in Combination with Osimertinib in First-Line EGFR-Mutated Non-Small Cell Lung Cancer (PRNewswire) - "Amongst all evaluable patients treated, the Overall Response Rate (ORR) was 79%, with complete responses (CR) observed in 3 of 19 patients (16%), including a CR in the one patient enrolled whose lung cancer harbored a Wnt-pathway activating mutation (WPAM); In the doses escalation portion of the study, the median progression free survival (mPFS) for all evaluable patients was 19.9 months and median overall survival (mOS) was 48.8 months, only 6 events have occurred; Preliminary results suggest combination of osimertinib and tegavivint has the potential to improve the depth and durability of response through targeting drug-tolerant persister (DTP) cells and may be better tolerated than current FDA-approved combinations."

P1 data • Non Small Cell Lung Cancer

OSU-20298: Osimertinib and Tegavivint as First-Line Therapy for the Treatment of Metastatic EGFR-Mutant Non-small Cell Lung Cancer (clinicaltrials.gov) - P1 | N=25 | Recruiting | Sponsor: Ohio State University Comprehensive Cancer Center | Active, not recruiting ➔ Recruiting

Enrollment open • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

Tegavivint, a downstream Wnt/β-catenin inhibitor: Dose-finding results from a phase 1/2 trial in advanced hepatocellular carcinoma (aHCC). (ASCO 2026) - P1/2 | "Tegavivint is the first Wnt/β-catenin inhibitor to demonstrate monotherapy clinical activity and a manageable safety profile in heavily pretreated aHCC pts with WPMs. Observed partial responses, durable disease control, and on-target PD effects in 2L and 3L pts support further development of tegavivint as a monotherapy or in combination with other treatments for this population."

Metastases • P1/2 data • Hepatocellular Cancer • Hepatology • Musculoskeletal Pain • Oncology • Solid Tumor • AFP • CTNNB1

A Phase Ib Study of Osimertinib and Tegavivint as First-Line Therapy in Patients with Metastatic EGFR-Mutant Non-Small Cell Lung Cancer (NSCLC) (IASLC-WCLC 2024) - P1 | "Once the dose escalation phase of this trial is complete, the dose expansion phase will include a total of 12 patients at the RP2D to further assess clinical outcomes, including response rate, progression free survival, duration of response, and overall survival. Correlative studies include PK analysis, the evaluation of pharmacodynamic markers of β-catenin pathway activity, assessment of the clearance of EGFR-mutant ctDNA, and CT tumor volumetric studies."

Clinical • Metastases • P1 data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

OSU-20298: Osimertinib and Tegavivint as First-Line Therapy for the Treatment of Metastatic EGFR-Mutant Non-small Cell Lung Cancer (clinicaltrials.gov) - P1 | N=24 | Active, not recruiting | Sponsor: Ohio State University Comprehensive Cancer Center | Recruiting ➔ Active, not recruiting | Trial primary completion date: Jul 2026 ➔ Dec 2026

Enrollment closed • Trial primary completion date • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

Daneng Li, MD, on Tegavivint in Advanced HCC (THE ASCO POST) - "Daneng Li, MD...discusses dose-finding results from a phase I/II trial of tegavivint, a downstream Wnt/β-catenin inhibitor, in patients with advanced hepatocellular carcinoma (HCC) (Abstract 4015). "

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Iterion Therapeutics Reports First Clinical Validation of Tegavivint as a Targeted Therapy for Wnt-Driven Advanced HCC in Oral Presentation at 2026 ASCO Annual Meeting (PRNewswire) - "A total of 40 patients were enrolled....Clinical activity among efficacy-evaluable patients treated with tegavivint at the recommended dose range was observed primarily in patients with WPAM+ tumors: Tegavivint produced tumor shrinkage in approximately 40% of evaluable patients with WPAM+ tumors and achieved a 72% disease control rate (DCR); no tumor shrinkage was observed in patients without WPAMs. In second- and third-line patients with WPAM+ tumors, tegavivint achieved a 22% overall response rate (ORR), an 89% DCR and a median progression-free survival (mPFS) of 8 months."

P1/2 data • Hepatocellular Cancer

A phase Ib study of osimertinib and tegavivint as first-line therapy in patients with metastatic EGFR-mutated non–small cell lung cancer (NSCLC). (ASCO 2026) - P1 | "NCT04780568 showed that the combination of osimertinib and tegavivint was safe and tolerable as first-line therapy in patients with metastatic EGFR-mutated NSCLC. This novel combination has the potential to improve the depth and durability of response to EGFR TKIs, without significantly increasing toxicity, by targeting drug-tolerant persistence."

Clinical • Metastases • P1 data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

A phase 1b study of tegavivint, a TBL1 inhibitor, with gemcitabine in patients with relapsed or refractory osteosarcoma (TIGER). (ASCO 2026) - P1 | "Tumor tissue will be analyzed for TBL1 and Wnt/β-catenin signaling (sequencing and protein expression). Clinical trial information: NCT07144254."

Clinical • P1 data • CNS Disorders • Endocrine Disorders • Orthopedics • Osteosarcoma • Sarcoma • Solid Tumor • CTCs

City of Hope Researchers to Share New Immunotherapy and Precision Medicine Insights Across Cancer Types at ASCO 2026 (City of Hope)

Clinical data • Castration-Resistant Prostate Cancer • Hepatocellular Cancer • Large B Cell Lymphoma • Pancreatic Cancer • Renal Cell Carcinoma

Iterion Therapeutics Announces Oral Presentation of Phase 1/2 Tegavivint Data in Advanced Hepatocellular Carcinoma at the 2026 ASCO Annual Meeting (PRNewswire) - "Two additional investigator-sponsored trial posters featuring tegavivint clinical studies in EGFR-mutated NSCLC and pediatric osteosarcoma will also be presented...Headlining Iterion's presence is a rapid oral abstract session presenting Phase 1/2 dose-finding data in advanced hepatocellular carcinoma (HCC), which is the third-leading cause of cancer death globally and an area where treatment options remain limited."

P1 data • P1/2 data • Hepatocellular Cancer • Non Small Cell Lung Cancer • Osteosarcoma

Tegavivint directly targets TBL1 to inhibit b-catenin nuclear oncogenic activity (AACR 2026) - "Similar to tegavivint, these series bind directly to TBL1, disrupt the β-catenin/TBL1 interaction, inhibit β-catenin dependent transcription, and promote nuclear β-catenin degradation. These findings establish the oncogenic driver gene TBL1 as a novel, druggable target in the WNT/ β- catenin signaling pathway and highlight tegavivint as a differentiated therapeutic strategy for Wnt-driven cancers."

Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • TBL1XR1

Tegavivint, a first-in-class TBL1 inhibitor demonstrates potent activity in WNT-driven colorectal cancers (AACR 2026) - "Tegavivint demonstrated synergistic activity when combined with VEGF-TKIs and pan-RAS inhibitors, while combination with other Wnt-inhibitors yielded no added activity.Conclusion. These findings underscore the translational promise of Tegavivint as a therapeutic strategy in colorectal cancer, supporting its advancement toward clinical development to improve outcomes in WNT-driven disease subsets."

Colorectal Cancer • Hepatocellular Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ANXA5 • APC

Phase 1/2 trial of the TBL1 inhibitor, tegavivint, in advanced hepatocellular carcinoma (aHCC) (AACR 2025) - P1/2 | "In these early cohorts, weekly tegavivint appears tolerable and demonstrates preliminary efficacy in aHCC."

Metastases • P1/2 data • Hepatocellular Cancer • Oncology • Solid Tumor • AFP • AXIN1

Inhibition of TBL1 and β-catenin interaction sensitizes acute lymphoblastic leukemia to chemotherapy (AACR 2024) - "We hypothesize that interrupting the binding of TBL1 to β-catenin abrogates leukemia cell survival and test if tegavivint sensitizes these cells to chemotherapeutic agents such as VDL (Vincristine, Dexamethasone, L-asparaginase) as part of preclinical evaluation of tegavivint in T- and B-cell ALL. Four T-ALL cell lines one patient-derived T-ALL case, B-ALL cell lines and eight patient-derived B-ALL cases were used in vitro. Our preliminary data shows that T-ALL and B-ALL are sensitive to TBL1-β-catenin inhibition using tegavivint as a monotherapy. Tegavivint can also sensitize T-ALL and B-ALL to chemotherapy (VDL). As our data supports our hypothesis that TBL-1-β-catenin inhibition is a new target in ALL therapy, further studies are in progress to preclinically evaluate this approach for clinical care."

IO biomarker • Acute Lymphocytic Leukemia • B Acute Lymphoblastic Leukemia • Hematological Malignancies • Leukemia • Oncology • T Acute Lymphoblastic Leukemia • T-cell Acute Lymphoblastic Lymphoma • ANXA5 • CTNNB1

Iterion Presents New Data on First-in-Class TBL1 Inhibitor Tegavivint, Targeting Wnt-Driven Cancers at AACR Annual Meeting (PRNewswire) - "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."

Preclinical • Colorectal Cancer

Iterion Therapeutics Expands Clinical Development of Tegavivint, a First-in-Class Wnt/β-Catenin Inhibitor, into Colorectal Cancer with First Patient Dosed (PRNewswire)

Trial status • Colorectal Cancer

Safety and Efficacy of Tegavivint in Patients With Metastatic Colorectal Carcinoma (clinicaltrials.gov) - P1/2 | N=126 | Recruiting | Sponsor: HonorHealth Research Institute

New P1/2 trial • Colorectal Cancer • Oncology • Solid Tumor • BRAF

Tegavivint With Gemcitabine in Patients With Relapsed or Refractory Osteosarcoma (clinicaltrials.gov) - P1 | N=24 | Recruiting | Sponsor: Emory University | Not yet recruiting ➔ Recruiting

Enrollment open • Oncology • Osteosarcoma • Sarcoma • Solid Tumor

Tegavivint for Treating Patients With Relapsed or Refractory Large B-Cell Lymphoma (clinicaltrials.gov) - P1 | N=18 | Recruiting | Sponsor: Lapo Alinari | Trial completion date: Mar 2027 ➔ Mar 2028 | Trial primary completion date: Mar 2027 ➔ Mar 2028

Trial completion date • Trial primary completion date • B Cell Lymphoma • B Cell Non-Hodgkin Lymphoma • Diffuse Large B Cell Lymphoma • Hematological Malignancies • High-grade B-cell lymphoma • Indolent Lymphoma • Large B Cell Lymphoma • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • BCL2 • BCL6 • MYC

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

Trial status • Osteosarcoma

Tegavivint for the Treatment of Relapsed or Refractory Leukemia (clinicaltrials.gov) - P1 | N=9 | Active, not recruiting | Sponsor: M.D. Anderson Cancer Center | Trial completion date: Dec 2025 ➔ Feb 2027 | Trial primary completion date: Dec 2025 ➔ Feb 2027

Trial completion date • Trial primary completion date • Acute Myelogenous Leukemia • Hematological Malignancies • Leukemia • Oncology

Tegavivint With Gemcitabine in Patients With Relapsed or Refractory Osteosarcoma (clinicaltrials.gov) - P1 | N=24 | Not yet recruiting | Sponsor: Emory University | Initiation date: Oct 2025 ➔ Jan 2026

Trial initiation date • Oncology • Osteosarcoma • Sarcoma • Solid Tumor

OSU-20298: Osimertinib and Tegavivint as First-Line Therapy for the Treatment of Metastatic EGFR-Mutant Non-small Cell Lung Cancer (clinicaltrials.gov) - P1 | N=24 | Recruiting | Sponsor: Ohio State University Comprehensive Cancer Center | Trial primary completion date: Jul 2025 ➔ Jul 2026

Trial primary completion date • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Actionable Findings from an Unbiased Drug Screen for Novel Single Agent and Combination Therapies Against AML with Mecom Re-Arrangement (ASH 2023) - "This was consistent with previous reports that BET inhibitors (e.g., OTX015, mivebresib or ABBV-075 and JQ1) are effective against 3q26.2-r AML cell lines, patient-derived (PD) AML cells and PDX models...In follow-up experiments, XIAP/cIAPs inhibitors birinapant (10-1000 nM) or SM-164 (30-1000 nM), chosen based on the MIPE screen outcomes, induced significantly more dose-dependent apoptosis in 3q26.2-r versus the other AML cell lines...Treatment with the dual mTOR/PIK3CA inhibitor NVP-BGT226 (1-30 nM) or navitoclax or Bcl-xL-specific BH3 mimetic A-1155463 also exerted lethality and synergistically induced apoptosis with mivebresib in AML cells with inv3/t(3; 3)...Co-treatment with birinapant and tegavivint also synergistically induced apoptosis in 3q26.2-r AML cells...Additionally, compared to each drug or vehicle control, co-treatment with birinapant and the BETi OTX015 (30 mg/kg/day, by oral gavage) was more effective in reducing AML burden in the xenograft model...."

Combination therapy • Acute Myelogenous Leukemia • Oncology • BCL2L1 • BRD4 • CASP3 • CDK4 • CTNNB1 • GATA2 • HEXIM1 • MCL1 • MECOM • MYC • PIK3CA • SF3B1 • XIAP