Icalcaprant + itraconazole

Icalcaprant + itraconazole is an experimental combination of two small molecule drugs, administered together for clinical research purposes. - **Icalcaprant** is a selective antagonist of the kappa opioid receptor, under development for the treatment of neuropsychiatric disorders such as bipolar I/II disorder and opioid-related disorders. It blocks kappa opioid receptor (KOR) signaling, and is being developed as a potential antidepressant and drug withdrawal therapy by Cerevel Therapeutics, now part of AbbVie. - **Itraconazole** is a triazole antifungal agent that inhibits fungal cytochrome P450–dependent enzyme 14α-demethylase, impairing ergosterol synthesis, and is clinically used to treat systemic and superficial fungal infections. This drug combination is not approved for therapeutic use; rather, it has been investigated in Phase 1 drug-drug interaction studies to assess the effect of itraconazole, a strong CYP3A inhibitor, on the pharmacokinetics, safety, and tolerability of a single dose of icalcaprant in healthy participants.