Berotralstat CAS# 1809010-50-1 催乳药

Berotralstat (BCX7353) is a potent, selective, orally bioavailable small-molecule inhibitor of plasma kallikrein. In preclinical assays, it showed nanomolar potency (Ki ~1.0 nM) and effectively blocked kallikrein-mediated cleavage of high-molecular-weight kininogen, thereby reducing bradykinin generation. In animal models, berotralstat inhibited kallikrein activity in a dose-dependent manner and reduced vascular leakage associated with bradykinin overproduction. Pharmacokinetic studies in rodents and primates demonstrated favorable oral bioavailability (>40%) and sustained plasma concentrations supportive of once-daily dosing. These findings confirmed its potential to prevent hereditary angioedema (HAE) attacks and justified its progression into clinical development.