Technology ID
TAB-3556
Mutant IDH1 Inhibitors for Cancer Treatment
E-Numbers
E-243-2014-0
Lead Inventor
Boxer, Matthew (NCATS)
Co-Inventors
Rohde, Jason (NCATS)
Pragani, Rajan (NCATS)
Liu, Li (NCATS)
Davis, Mindy (NCATS)
Brimacombe, Kyle (NCATS)
Shen, Min (NCATS)
Simeonov, Anton (NCATS)
Urban, Daniel (NCATS)
Jadhav, Ajit (NCATS)
Wang, Xiaodong (University of North Carolina, Chapel Hill)
McIver, Andrew (University of North Carolina, Chapel Hill)
Karavadhi, Surendra (NCATS)
Applications
Therapeutics
Therapeutic Areas
Oncology
Lead IC
NCATS
ICs
NCATS
This technology includes a novel chemotype against mutant (R 132H) isocitrate dehydrogenase 1 (IDH1) enzyme to be utilized as an anticancer therapy. We have progressed the structure activity relationship (SAR) and optimized the compound to be low nanomolar inhibitor of the enzyme with low nanomolar inhibition of the target in cells. These compounds lower 2-hydroxyglutarate, which has been termed an 'oncometabolite' and is common in a subset of cancers including glioma, cholangiocarcinoma, chondrosarcoma and acute myeloid leukemia.
Commercial Applications
These IDH1 inhibitors would be used to treat cancers in which mutated IDH1 has been discovered.
Competitive Advantages
Wide variety of cancers which harbor IDH1 mutations, with potential for large market share.
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