Brensocatib CAS# 1802148-05-5

Brensocatib is a selective, orally active inhibitor of dipeptidyl peptidase-1 (DPP1), the enzyme responsible for activating neutrophil serine proteases. In preclinical biochemical assays, it inhibited DPP1 with subnanomolar potency (Ki ~0.5–1 nM) and reduced activation of neutrophil elastase, proteinase-3, and cathepsin G in human precursor cells. In murine lung-inflammation models, brensocatib decreased neutrophil elastase activity by >70% and significantly reduced airway damage and inflammatory cytokines. In toxicology studies across species, it showed good oral exposure, dose-dependent pharmacodynamic effects, and acceptable safety margins, supporting its advancement for neutrophil-driven inflammatory diseases.