This week in therapeutics

Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Cancer

Cancer

Mdm2 p53 binding protein homolog (MDM2; HDM2); p53

In vitro and mouse studies identified MI-888 as an inhibitor of MDM2-p53 protein-protein interactions that could help treat cancer. In the in vitro binding studies, MI-888 showed subnanomolar binding affinity for MDM2. In a mouse xenograft model for human osteosarcoma, MI-888 caused complete tumor regression, whereas vehicle did not. Mice remained tumor free for at least 64 days after the last dose of
MI-888. Next steps include testing and optimizing
MI-888 for use in multiple tumor types.
Ascenta Therapeutics Inc. and Sanofi have MI-773, a related small molecule inhibitor of p53-MDM2 protein-protein interactions, in Phase I testing to treat cancer.

SciBX 6(21); doi:10.1038/scibx.2013.515
Published online May 30, 2013

Patent applications filed; licensed to Ascenta and sublicensed to Sanofi

Zhao, Y. et al. J. Am. Chem. Soc.; published online May 3, 2013;
doi:10.1021/ja3125417
Contact: Shaomeng Wang, University of Michigan, Ann Arbor, Mich.
e-mail:

shaomeng@umich.edu