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ULK kinase inhibition for cancers caused by RAS/RAF mutations

DCC-3116 in an investigational, orally administered, potent, and highly selective switch-control inhibitor of the ULK kinase that was discovered using our proprietary drug discovery platform. DCC-3116 is designed to inhibit autophagy, a key tumor survival mechanism in cancer cells, by inhibiting the ULK 1/2 kinases, which have been shown to be the initiating factors that activate autophagy. DCC-3116 in combination with RAS/MAP kinase signaling pathway inhibition has the potential to change the treatment of RAS/RAF cancers.

Cancers caused by RAS/RAF mutations are the most common activating mutations of all cancers and represent a significant unmet medical need. The RAS mutation activates signaling through the MAPK (RAF-MEK-ERK) pathway and the autophagy pathway. MAPK inhibitors have not been successful thus far as single agents for the treatment of cancers caused by RAS mutations.