Cerecor (CERC) Announces Publication of Data Regarding Human Brain Receptor Occupancy of CERC-501

December 11, 2015 9:18 AM EST

Cerecor Inc. (NASDAQ: CERC) today announced the publication of data regarding the human brain receptor occupancy of CERC-501, formerly known as LY2456302. In this study of healthy volunteers, CERC-501 demonstrated reproducible penetration of the blood-brain barrier and target engagement, as shown through PET (positron emission tomography) imaging. CERC-501 is a potent and selective oral kappa opioid receptor, or KOR, antagonist being developed to treat depression and substance use disorders, such as alcohol, nicotine and/or illicit drug dependence.

The study ‘Receptor Occupancy of the Kappa Opioid Antagonist LY2456302 Measured with PET and the Novel Radiotracer 11C-LY2795050 was conducted by researchers at the Yale University School of Medicine and Eli Lilly and Company and published in the December issue of the Journal of Pharmacology and Experimental Therapeutics (JPET).

“Kappa opioid receptor antagonists are an exciting new class of compounds that hold the promise to treat a broad range of mood and substance use disorders,” commented Dr. Blake Paterson, CEO of Cerecor. “This study demonstrated that CERC-501 gets to where it is needed in the brain to be effective and that a single dose of 10 mg of CERC-501 almost completely saturated kappa receptors in the brain at 2.5 hours post dose, supporting the exploration of doses between 4 and 25 mg in efficacy clinical trials. We wish to acknowledge the excellent scientific and collaborative effort put forth by our Lilly and Yale colleagues. We expect to initiate a Phase 2 proof-of-concept study of CERC-501 in heavy smokers in the near future with top-line data expected before the end of 2016.”

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