Major Depression Drug: aticaprant CAS 1174130-61-0

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Author : sarms4muscle
Update time : 2024-04-28 15:39:15
Drug name: aticaprant

R&D code: JNJ 67953964, LY2456302, CERC501
CAS: 1174130-61-0
Indication: Severe depression
Original Research Company: Johnson
Aticaprant was originally developed by Eli Lilly and Company under the code name LY-2456302. It first appeared in the scientific literature in 2010.

In February 2015, Cerecor announced that it had acquired development and commercialization rights to LY-2456302 (new development code CERC-501) from Eli Lilly and Company.
A Phase II study in heavy smokers was initiated in early 2016 in which Aticaprant failed to meet the primary endpoint of nicotine withdrawal.
In August 2017, Cerecor announced the assignment of its patents to Janssen Pharmaceuticals (Janssen).
Stage of development: phase 3

Aticaprant has a 25% oral bioavailability, which is good. After administration, it is quickly absorbed and takes one to two hours to reach its maximal concentration. In healthy persons, its elimination half-life lasts between thirty and forty hours. Atiprane levels in the blood rise in direct proportion to dosage. After taking the medication once daily for six to eight days, steady-state concentrations are attained. It has been demonstrated that aticaprant can repeatedly cross the blood-brain barrier.

It is undergoing Phase III clinical studies for major depressive disorder as of July 2022. The effectiveness of this medication, like that of other kappa opioid antagonists presently being studied in clinical settings for the treatment of major depressive disorder, may be impacted by counter-compensatory activation of pro-inflammatory cytokines in central nervous system microglia. Although development for these indications has been halted, ativaparant is also being developed for the treatment of alcoholism, cocaine use problems, and smoking cessation.