Selectins, a family of adhesion molecules, play a key role in the activation and extravasation of leukocytes in inflammatory diseases, like COPD. We investigated the effect of repeated inhalations of the pan-selectin antagonist Bimosiamose on ozone-induced airway inflammation in healthy volunteers. In a double-blind, placebo-controlled, randomised, cross-over study the effect of a 4-days treatment with 10 mg of Bimosiamose bid inhaled by a breath actuated nebuliser (AKITA2 APIXNEB®) on cellular and non-cellular composition of induced sputum after inhalation of ozone (250 ppb) for three hours was evaluated. 18 subjects were randomised and completed the study. All treatments were safe and well tolerated. Bimosiamose, compared to placebo treatment, reduced numbers of sputum neutrophils by 40% (p=0.068) and lymphocytes by 65% (p=0.004). Sputum concentration of interleukin-8 and MMP-9 was diminished by 35% (p=0,004) and 46% (p=0,022), respectively. Inhalation of Bimosiamose showed a broad and favourable significant effect on ozone-induced airway inflammation in healthy subjects. Further studies have to proof and translate this anti-inflammatory effect of Bimosiamose into a clinical benefit in patients with COPD.