Overview

NCI Definition [1]:
A small molecule inhibitor of the Wnt/beta-catenin pathway with potential antineoplastic activity. Upon intravenous administration, tegavivint binds to transducin beta-like protein 1 (TBL1) and disrupts the binding of beta-catenin to TBL1. This promotes beta-catenin degradation, attenuates nuclear and cytoplasmic levels of beta-catenin, and reduces transcriptional activity of transcription factor 4 (TCF4) and expression of its target genes, cyclin D1, c-Myc and survivin. The Wnt/beta-catenin signaling pathway regulates cell morphology, motility, and proliferation; aberrant regulation of this pathway leads to neoplastic proliferation. Beta-catenin is frequently mutated in various tumors.

Tegavivint has been investigated in 3 clinical trials, of which 3 are open and 0 are closed. Of the trials investigating tegavivint, 3 are phase 1 (3 open).

EGFR A763_Y764insFQEA, EGFR Exon 19 Deletion, and EGFR Exon 19 Insertion are the most frequent biomarker inclusion criteria for tegavivint clinical trials.

Acute myeloid leukemia, desmoid-type fibromatosis, and non-small cell lung carcinoma are the most common diseases being investigated in tegavivint clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Tegavivint
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating tegavivint and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
tegavivint, tegavivint, bc2059, bc 2059, tegatrabetan, bc-2059, 9,10-anthracenedione, 2,7-bis(((3r,5s)-3,5-dimethyl-1-piperidinyl)sulfonyl)-, 9,10-dioxime, rel-
Drug Target(s) [2]:
CTNNB1
NCIT ID [1]:
C155885

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.