Aticaprant
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| Other names | JNJ-67953964; CERC-501; LY-2456302 |
| Routes of administration | By mouth |
| Pharmacokinetic data | |
| Bioavailability | 25% |
| Elimination half-life | 30–40 hours |
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| Chemical and physical data | |
| Formula | C26H27FN2O2 |
| Molar mass | 418.512 g·mol−1 |
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Aticaprant, also known by its developmental codes JNJ-67953964, CERC-501, and LY-2456302, is a κ-opioid receptor (KOR) antagonist which was under development for the treatment of major depressive disorder and other conditions. Aticaprant is taken by mouth.
Side effects of aticaprant include itching, among others. Aticaprant acts as a selective antagonist of the KOR, the biological target of the endogenous opioid peptide dynorphin. The medication has decent selectivity for the KOR over the μ-opioid receptor (MOR) and other targets, a relatively long half-life of 30 to 40 hours, and readily crosses the blood–brain barrier to produce central effects.
Aticaprant was originally developed by Eli Lilly, was under development by Cerecor for a time, and is now under development by Janssen Pharmaceuticals. As of July 2022, it is in phase III clinical trials for major depressive disorder. In March 2025, Johnson & Johnson discontinued development of aticaprant for major depressive disorder due to lack of effectiveness in phase III trials.
Aticaprant was also under development for the treatment of alcoholism, cocaine use disorder, and nicotine withdrawal, but development for these indications was discontinued as well.