Technology ID
TAB-3586
Discovery of imidazo[1,2-b]pyridazines with Anticancer Properties
E-Numbers
E-044-2016-0
Lead Inventor
Thomas, Craig (NCATS)
Co-Inventors
Hoyt, Scott (NCATS)
Sutter, Patrick (Baylor University)
Finocchio, Chris (NCATS)
Starczynowski, Daniel (Cincinnati Children's Hospital Medical Center)
Tawa, Gregory (NCATS)
Applications
Therapeutics
Research Materials
Therapeutic Areas
Oncology
Lead IC
NCATS
ICs
NCATS
This technology includes a series of imidazo[1,2-b]pyridazines that display potent inhibition of FLT3, as well as 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.
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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