This week in therapeutics




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Mammalian target of rapamycin complex 1
(mTORC1); mTORC2

An SAR study suggests dual-specificity inhibitors of mTORC1 and mTORC2 could help treat cancer. In vitro lead optimization studies identified benzoxazepine-based compounds that were nanomolar inhibitors of both mTORC1 and mTORC2 but not of phosphoinositide 3-kinase (PI3K). In a mouse xenograft model, the lead compound, XL388, decreased tumor growth compared with vehicle control. Next steps could include further optimization or IND-enabling studies.
Exelixis Inc.'s XL388 is in preclinical development for cancer indications.
Takeda Pharmaceutical Co. Ltd.'s INK128, an inhibitor of mTORC1 and mTORC2, is in Phase I testing for various cancers.

SciBX 6(9); doi:10.1038/scibx.2013.213
Published online March 7, 2013

Patented by Exelixis; available for partnering or licensing

Takeuchi, C.S. et al. J. Med. Chem.; published online Feb. 8, 2013;
Contact: James W. Leahy, University of South Florida, Tampa, Fla.
Contact: Byung Gyu Kim,
Asan Institute for Life Science,
Seoul, South Korea