TEI-8362 (TEI 8362) is a potent, selective inhibitor of human neutrophil elastase (HNE) with Ki value of 1.38 nM and IC50 of 1.9 nM.
TEI-8362 showed 1000-fold selectivity for HNE versus chymotrypsin, and 100 fold versus trypsin.
TEI-8362 (0.03, 0.10 and 0.30 mg/kg, intratracheal administration) inhibited acute lung haemorrhage in a dose-dependent manner on HNE-induced lung haemorrhage in hamsters with an ED50 of 45 ug/kg.
TEI-8362 (0.1, 1.0 and 10.0 mg/ kg, intratracheal administration) also inhibited acute lung haemorrhage and attenuated the increase in elastase-like activity in a dose-dependent manner in LPS and FMLP-induced acute lung injury in hamsters with an ED50 of 0.56 mg/kg.
