TARGETING STAT3 TO PREVENT COLORECTAL CANCER SECONDARY TO INFLAMMATORY BOWEL DISEASE

NIH RePORTER · NIH · N01 · $932,948 · view on reporter.nih.gov ↗

Abstract

Signal transducer and activator of transcription 3 (STAT3) is one of the seven members of a family of transcription factors that regulates cell proliferation, differentiation, apoptosis, and the immune response. There is increasing evidence that STAT3 contributes to the development of both inflammatory bowel disease (IBD) and colorectal cancer (CRC). For example, a multitude of cytokines found to be elevated in the plasma and tissue of patients with IBD are known to activate STAT3 and/or its downstream targets; and mice with increased pro-inflammatory and anti-apoptotic STAT3 activity show accelerated development of intestinal tumors compared to wildtype mice when treated with azoxymethane (AOM) and dextran sulfate sodium (DSS). Thus, inhibiting STAT3 may prevent CRC in individuals diagnosed with IBD (e.g. ulcerative colitis or Crohn’s disease) who have a 20- to 30-fold greater chance than the general population of developing CRC and a worse outcome following diagnosis. The STAT3 inhibitor TTI-101, developed by Dr. David Tweardy and colleagues and licensed to Tvardi Therapeutics, binds to the SH2 domain of STAT3 with high affinity and inhibits the protein’s dimerization and phosphorylation. It does not target other tyrosine kinases, provides excellent plasma exposure following oral administration, and produces no detectable toxicity when administered for a period of 28 days in rats and dogs. It is currently being evaluated in a Phase I clinical trial in patients with advanced cancers (https://clinicaltrials.gov/show/NCT03195699). The purpose of this Task Order is to evaluate TTI-101 for the prevention of CRC associated with IBD.

Key facts

NIH application ID
10491413
Project number
75N91019D00021-0-759102100002-1
Recipient
UNIVERSITY OF TX MD ANDERSON CAN CTR
Principal Investigator
POWELL BROWN
Activity code
N01
Funding institute
NIH
Fiscal year
2021
Award amount
$932,948
Award type
Project period
2021-09-16 → 2023-09-15