Clinical Trials

Multiple clinical trials evaluate tegatrabetan (BC2059) across several advanced oncological indications, including unresectable desmoid tumors, relapsed or refractory leukemias, advanced hepatocellular carcinoma, and metastatic EGFR-mutant non-small cell lung carcinoma. Sponsored by industry and academic institutions, including Iterion Therapeutics, M.D. Anderson Cancer Center, and Ohio State University Comprehensive Cancer Center, these Phase 1 and Phase 1/2 protocols range from active recruitment to completed status.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04874480 ACTIVE_NOT_RECRUITING
Recurrent Leukemia; Refractory Leukemia
M.D. Anderson Cancer Center
 2021-09-27 PHASE1
NCT04780568 ACTIVE_NOT_RECRUITING
Metastatic Lung Non-Small Cell Carcinoma; Stage IV Lung Cancer AJCC v8; Stage IVA Lung Cancer AJCC v8; Stage IVB Lung Cancer AJCC v8
Ohio State University Comprehensive Cancer Center
 2022-01-18 PHASE1
NCT05797805 RECRUITING
Advanced Hepatocellular Carcinoma
Iterion Therapeutics
 2023-09-13 PHASE1; PHASE2
NCT05797805 Recruiting
Advanced Hepatocellular Carcinoma
Iterion Therapeutics
 2023-09-13 Phase 1|Phase 2
NCT03459469 COMPLETED
Desmoid Tumor
Iterion Therapeutics
 2018-07-15 PHASE1
NCT03459469 Completed
Desmoid Tumor
Iterion Therapeutics
 2018-07-15 Phase 1

(data from https://clinicaltrials.gov, updated on 2026-08-25)

Check the Tegatrabetan (BC-2059) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Tegatrabetan acts as a β-catenin antagonist by disrupting the binding interaction between β-catenin and the scaffold protein transducin β-like 1 (TBL1), thereby promoting proteasomal degradation and decreasing nuclear accumulation of β-catenin. This inhibition suppresses β-catenin-mediated transcription and oncogenic proliferation, providing potential therapeutic utility in β-catenin-driven malignancies such as advanced hepatocellular carcinoma, desmoid tumors, relapsed leukemias, and non-small cell lung cancer.

Appendix RUO and cGMP Quality Standards

Quality Dimension RUO (Research Use Only) cGMP (Current Good Manufacturing Practice)
Clinical Applicability Prohibited in human clinical trials or medical diagnostics. Mandatory for human clinical trials (Phase I–III) and therapies.
Regulatory Status Non-regulated grade; exempt from drug manufacturing laws. Legally enforced by health authorities (e.g., FDA, EMA, NMPA).
Facility Environment Unclassified analytical or research laboratories. Validated Cleanrooms (ISO Class 5–8) with continuous monitoring.
Quality Control Basic purity and activity testing. Rigorous safety release testing (Sterility, Endotoxin, Mycoplasma).
Process Validation Basic equipment calibration; no process validation required. Full qualification (IQ/OQ/PQ) and complete batch records.
Quality Assurance Vendor self-declared without required formal QMS. Mandatory QA/QC unit, Change Control, CAPA, and vendor audits.
Regulatory Impact High risk of IND rejection if used as a critical raw material. Required for IND/NDA filings, supported by Drug Master Files (DMF).

Footnotes

Regulatory Note: Governed by FDA (21 CFR Parts 210/211/312), EMA (EudraLex Vol 4), ICH Guidelines (E6/Q7/Q9/Q10), and compendial standards (USP <71>/<85>/<1043>).

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Note: Technical data last updated: Sep 1, 2026.