On April 7, 2014 Deciphera Pharmaceuticals reported the initiation of a Phase 1 clinical trial of its pan-RAF inhibitor LY3009120 (DP-4978), under development in collaboration with Eli Lilly (Press release Deciphera Pharmaceuticals, APR 7, 2014, View Source [SID:1234500371]). The Phase 1 trial will evaluate the safety, tolerability and initial efficacy of LY3009120 in cancer patients. Data demonstrating the preclinical activity of LY3009120 in cancer were recently presented at the New Drugs on the Horizon plenary session at the American Association for Cancer Research (AACR) (Free AACR Whitepaper) national meeting, held April 5-9, 2014 in San Diego. LY3009120 emerged from a collaboration between Eli Lilly and Deciphera Pharmaceuticals, LLC. Deciphera received a $6 million development milestone for initiation of Phase 1 studies.
LY3009120 is a small molecule kinase inhibitor that has been shown to inhibit known characterized RAF isoforms, and potentially blocks proliferation in both BRAF and RAS mutant cancer cells. LY3009120 broadly blocks signaling of cellular RAF homo/heterodimers including CRAF containing dimers, thus minimizing paradoxical pathway activation and resistance mechanisms associated with selective BRAF inhibitors. Such paradoxical pathway stimulation is associated with side effects of these selective B-RAF inhibiting drugs, including cutaneous squamous cell carcinoma and other hyperplasias. As a pan-RAF inhibitor, LY3009120 blocks aberrant cancer signaling through RAS protein mutations, known to be prevalent in approximately 30% of all human cancers.
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