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BIO-1211 is a highly selective and orally active small molecule inhibitor of the integrin α4β1 (also known as Very Late Antigen-4 or VLA-4). It exhibits high affinity for α4β1 with an IC50 of approximately 4 nM and demonstrates about 200-fold selectivity for the activated form of this integrin over related targets such as α4β7[1][4][5]. Integrin α4β1 plays a critical role in leukocyte recruitment, activation, inhibition of apoptosis, and mediator release during inflammatory responses. By antagonizing this target, BIO-1211 inhibits processes such as eosinophil chemotaxis and neutrophil adhesion—key steps in allergic inflammation and asthma pathophysiology[5][9]. Preclinical studies have shown that administration of BIO-1211 reduces airway inflammation and bronchoconstriction in animal models. Clinically, it has been investigated up to Phase 2 trials for asthma by companies including Biogen and Merck Sharp & Dohme[2].
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