Overview

NCI Definition [1]:
An orally bioavailable, binaphthol-sulfonamide-based inhibitor of signal transducer and activator of transcription 3 (STAT3), with potential antineoplastic activity. Upon oral administration, the STAT3 inhibitor C-188-9 specifically targets and binds to the phosphotyrosyl peptide binding site within the Src homology 2 (SH2) domain of STAT3. This inhibits the Janus kinase (JAK)-mediated tyrosine phosphorylation and activation of STAT3. This impedes nuclear translocation of STAT3, prevents STAT3 binding to responsive gene promoters and blocks STAT3-mediated regulation of gene expression. STAT3 regulates the transcription of genes involved in several cellular functions. STAT3 is constitutively activated in a variety of human cancers and plays a key role in neoplastic transformation, uncontrolled tumor cell proliferation, resistance to apoptosis, metastasis, immune evasion, tumor angiogenesis, epithelial-mesenchymal transition (EMT) and the Warburg effect.

Tti-101 has been investigated in 1 clinical trial, of which 1 is open and 0 are closed. Of the trial investigating tti-101, 1 is phase 1 (1 open).

Malignant solid tumor is the most common disease being investigated in tti-101 clinical trials [2].

Drug Details

Synonyms [2]:
tti101, tti 101, stat3 inhibitor xiii, tat3 inhibitor tti-101, stat3 inhibitor c188-9, c188-9
Drug Target(s) [2]:
STAT3
NCIT ID [1]:
C151932

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.