Lodelaben is a human neutrophil elastase inhibitor with an IC50 of 0.5 μM and a Ki of 1.5 μM.

Elastase:(ki)1.5 μM , Elastase:0.5 μM

Results indicate that the inhibition of human neutrophil elastase (HNE) by Lodelaben is non-competetive.?Lodelaben is not inhibitory at 10 μM with the synthetic substrates or at 5 μM vith Azocoll.?Pseudomonas aeruginosa elastase, a metallo-protease is not inhibited by Lodelaben.?Cathepsin G activity, however, is inhibited by Lodelaben, with an IC50 of approximately 2.5 μM, with Azocoll as substrate[1].

The mean pulmonary artery pressures in both the saline/vehicle and saline/Lodelaben groups were comparable, at 16.4±1.1 and 17.4±0.9 mm Hg, respectively. However, the mean pressure significantly increased in the monocrotaline/vehicle group to 27.5±0.8 mm Hg. Notably, Lodelaben treatment in monocrotaline-administered rats markedly reduced the pressure to 21.00±1.6 mm Hg (p<0.05). In terms of vascular muscularization at the alveolar wall level, saline-treated rats, regardless of Lodelaben administration, demonstrated minimal muscularization (1.9±1.4% and 0.4±0.4%, respectively). Conversely, Lodelaben administration in monocrotaline-treated rats significantly lowered the percentage of muscularized alveolar wall arteries to 10.0±3.6%[2], indicating a protective effect of Lodelaben against monocrotaline-induced vascular alterations.