JNJ-54166060 is a potent and selective antagonist of P2X7 receptor, with IC 50 s of 4/115/72 nM for human/rat/mouse P2X7 receptor, respectively [1].

JNJ-54166060 shows high oral bioavailability (rat 55%, dog >100%, monkey 54 %) and C max (rat 375, dog 1249, monkey 389 ng/mL) following oral administration (rat 5 and, dog 5 mg/kg, monkey 5 mg/kg) [1]. JNJ-54166060 exhibits terminal elimination half-lives (rat 1.7 and, dog 11.9 h, monkey 4.2 h) due to low-moderate clearance (30, 5.5, and 14 mL/min/kg respectively) following intravenous administration (rat 1.0 and, dog 1.0 mg/kg, monkey 1.0 mg/kg) [1]. Animal Model: Sprague-Dawley rats [1] Dosage: 1 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis) Administration: Intravenous administration and oral administration Result: Oral bioavailability (55%), C max (375 ng/mL), T 1/2 (1.7 h). Animal Model: Beagle dogs [1] Dosage: 1 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis) Administration: Intravenous administration and oral administration Result: Oral bioavailability (>100%), C max (1249 ng/mL), T 1/2 (11.9 h). Animal Model: Cynomolgus monkeys [1] Dosage: 1 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis) Administration: Intravenous administration and oral administration Result: Oral bioavailability (54%), C max (389 ng/mL), T 1/2 (4.2 h).