JNJ-54166060 is a potent and selective P2X7 receptor antagonist, with IC50 values of 4 nM, 115 nM, and 72 nM for the human, rat, and mouse P2X7 receptors, respectively [1].

JNJ-54166060 demonstrates significant effectiveness across various animal models, with high oral bioavailability observed in rats (55%), dogs (>100%), and monkeys (54%), alongside considerable maximum plasma concentrations (C max) of 375 ng/mL, 1249 ng/mL, and 389 ng/mL, respectively, following a 5 mg/kg oral dose. Intravenously administered at 1 mg/kg, the compound showed low to moderate clearance rates, resulting in terminal elimination half-lives of 1.7 hours in rats, 11.9 hours in dogs, and 4.2 hours in monkeys. These pharmacokinetic parameters indicate the compound's potent and durable presence in systemic circulation across different species, underscoring its potential for further therapeutic development.