Thursday, August 8, 2013
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Aurora kinase A (AURKA;
In vitro and mouse studies suggest furanopyrimidine-based
dual AURKA and AURKB inhibitors could help treat cancer. In in vitro
assays, the lead furanopyrimidine selectively inhibited AURKA and AURKB at
nanomolar IC50 values. In a mouse xenograft model for human
colorectal cancer, the lead compound decreased tumor growth compared with
vehicle without causing toxicity. Next steps could include testing the lead
compound in animal models for other cancers.
Pharmaceutical Co. Ltd.'s alisertib
a second-generation AURKA inhibitor, is in Phase III testing to treat T cell
lymphoma and Phase II testing or earlier for other cancers.
an inhibitor of AURKA and multiple tyrosine kinases, is in Phase II
testing to treat sarcoma, breast cancer and ovarian cancer and Phase I
testing for other cancers.
Pharmaceuticals Inc.'s AT9283,
a small molecule inhibitor of AURKA, AURKB, Janus
tyrosine kinase 3 (FLT3;
T315I, is in Phase II testing to treat multiple myeloma (MM)
and Phase I testing for other cancers.
Published online Aug. 8, 2013
Patent and licensing status
Shiao, H.-Y. et al. J.
Med. Chem.; published online June 28, 2013;
Contact: Hsing-Pang Hsieh, National Health Research
Institutes, Zhunan, Taiwan
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