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BIIL 260 BS is a potent, selective, and orally active antagonist of the leukotriene B4 (LTB4) receptor 1 (BLT1). Developed by Boehringer Ingelheim, it was investigated for the treatment of inflammatory conditions such as chronic obstructive pulmonary disease (COPD), asthma, and rheumatoid arthritis. BIIL 260 BS acts by competitively inhibiting the binding of LTB4 to its high-affinity receptor BLT1, thereby preventing LTB4-induced chemotaxis and activation of neutrophils. Notably, BIIL 260 BS is the active metabolite of the prodrug amelubant (BIIL 284). While it demonstrated significant anti-inflammatory activity in preclinical models and early clinical studies, its development was eventually discontinued.
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