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.
