A clinical study was conducted to evaluate the safety and efficacy of the H4 antagonist, JNJ 39758979 [(R)-4-(3-amino-pyrrolidin-1-yl)-6-isopropyl-pyrimidin-2-ylamine], on histamine-induced pruritus in healthy subjects (n = 23). A single oral dose of 600 mg of JNJ 39758979, 10 mg of cetirizine, or placebo was administered in a randomized, three-period, double-blind, crossover study. A histamine challenge was administered on day −1 and at 2 and 6 hours postdose on day 1 of each treatment period. The primary efficacy endpoint was area under the curve of pruritus score 0–10 minutes posthistamine challenge. Compared with placebo, the reduction of the pruritus score was significant for JNJ 39758979 at 2 hours and for cetirizine at 6 hours. JNJ 39758979 did not demonstrate a significant decrease in wheal or flare reaction, although a significant reduction was achieved with cetirizine. Adverse events reported in more than one patient with JNJ 39758979 were headache (9%) and nausea (13%). In conclusion, JNJ 39758979 was effective in inhibiting histamine-induced pruritus in healthy subjects.
See article at J Pharmacol Exp Ther 2014, 350:181–187.
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