Technology ID
TAB-3505

Discovery of an imidazo[1,2-a]pyridines with Anticancer Properties

E-Numbers
E-151-2020-0
Lead Inventor
Thomas, Craig
Lead IC
NCATS
Co-Inventors
Hoyt, Scott
Walker, Morgan
Sutter, Patrick
Jiang, Jiankang
Finocchio, Chris
Starczynowski, Daniel
ICs
NCATS
Applications
Therapeutics
Research Materials
Therapeutic Areas
Oncology
This technology includes a series of imidazo[1,2-a]pyridines with potent inhibition of FLT3, which retains potent binding and activity against FLT3 tyrosine kinase domain and gatekeeper mutations. This chemotype exhibits superior anti-leukemic activity against the common clinically-relevant FLT3-mutant acute myeloid leukemia (AML) in vitro and in vivo. Tyrosine kinase domain mutations are a common cause of acquired resistance to FLT3 inhibitors used to treat FLT3-mutant AML. This invention builds upon an earlier IP position with new analogs.
Commercial Applications
If successful in human clinical trials, these agents could be used to treat a variety of hematological diseases, including but not limited to AML, myelodysplastic syndrome, diffuse large B-cell lymphoma, and other blood cancers.

Competitive Advantages
These agents have activity versus mutations in the acquired resistance space and versus non-IRAK inhibitors in the adaptive resistance space.
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