CERC-501

CERC-501 (formerly LY2456302) is a potent and highly selective small molecule antagonist of the kappa opioid receptor (KOR). Originally discovered by Eli Lilly and subsequently licensed to Cerecor, the compound is designed to modulate the dynorphin/KOR system, which is implicated in the biology of stress, mood, and reward. By blocking KOR signaling, CERC-501 aims to mitigate the dysphoric effects of stress that often trigger drug-seeking behavior and relapse. In collaboration with Yale University and with NIH funding, CERC-501 has been investigated in Phase 2 human laboratory models to evaluate its efficacy in reducing stress-precipitated smoking lapses and withdrawal symptoms in individuals with tobacco use disorder. It has also been explored as an adjunctive treatment for major depressive disorder and for other substance use disorders such as cocaine addiction.

Other names

(S)-3-fluoro-4-(4-((2-(3,5-dimethylphenyl)pyrrolidin-1-yl)methyl)phenoxy)benzamide