Dual PI3K-mTOR inhibitors

Context

The phosphoinositide-3 kinase (PI3K) and mTOR signaling pathway is an important target for the treatment of several cancers. Mutations in the genes encoding the PI3K, Akt and mTOR kinases result in a dysregulation of the pathway that promotes the development of tumors, such as breast and colon cancer. This deregulation is also associated with increased chemo resistance and a poor prognosis. Only inhibition of both PI3K and mTOR can completely block the abnormally-activated pathway.

Technology

A large family of 100 small chemical molecules able to target both PI3K and mTOR and block the resulting signaling pathway. - High specificity - High selectivity - Tested on a large panel of tumor cells in vitro - Low toxicity in vivo - Proof-of-concept in a mouse model of colorectal cancer - Large chemical synthesis know-how

Benefits

• Dual inhibition of PI3K and mTOR
• Synergy in efficacy and complementary therapeutics to current cytotoxic and targeted therapies.