RO5101576 is a potent LTB4 receptor antagonist with activity to inhibit LTB4-induced calcium mobilization and chemotaxis of human neutrophils. RO5101576 significantly attenuated LTB4-induced pulmonary eosinophilia in guinea pigs. RO5101576 inhibited allergen- and ozone-induced pulmonary neutrophilia in nonhuman primates with efficacy comparable to that of budesonide. RO5101576 had no effect on LPS-induced neutrophilia in guinea pigs and cigarette smoke-induced neutrophilia in mice and rats. RO5101576 performed well in toxicology studies and was well tolerated.
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