Technology Bundle ID
TAB-3556

Mutant IDH1 Inhibitors for Cancer Treatment

Applications
Linked ID
E-243-2014-0
Lead Inventors
Matthew Boxer (NCATS)
Co-Inventors
Ajit Jadhav (NCATS)
Andrew McIver (University of North Carolina Chapel Hill)
Anton Simeonov (NCATS)
Daniel Urban (NCATS)
Jason Rohde (NCATS)
Kyle Brimacombe (NCATS)
Li Liu (NCATS)
Min Shen (NCATS)
Mindy Davis (NCATS)
Rajan Pragani (NCATS)
Surendra Karavadhi (NCATS)
Xiaodong Wang (University of North Carolina Chapel Hill)
ICs
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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