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Inflammation Research (2023) 72:1709–1717 https://doi.org/10.1007/s00011-023-01774-4 ORIGINAL RESEARCH PAPER Inflammation Research BI 1291583: a novel selective inhibitor of cathepsin C with superior in vivo profile for the treatment of bronchiectasis Stefan Kreideweiss1 · ...
In vivo inhibition of NE and NSP proteinase 3 (PR3) in bronchoalveolar lavage fluid (BALF) neutrophils after lipopolysaccharide (LPS) challenge and distribution of BI 1291583 was determined in a mouse model.Results BI 1291583 bound human CatC in a covalent, reversible manner, selectively and fully...
BI 1291583 bound human CatC in a covalent, reversible manner, selectively and fully inhibiting CatC enzymatic activity. This inhibition translated to concentration-dependent inhibition of NE activation in U937 cells and dose-dependent, almost-complete inhibition of NE and PR3 activity in BALF neutrophils...
Due to these promising phase I results, a multinational phase II program of BI 1291583 in adults with bronchiectasis is ongoing (Airleaf [NCT05238675], Clairafly [NCT05865886], and Clairleaf [NCT05846230]). 展开 关键词: LEUCOCYTE elastase DEATH rate ITRACONAZOLE DISEASE progression BRONCHIECTASIS ...
Here, we present the phase I characterization of the novel CatC inhibitor, BI 1291583. Five phase I trials of BI 1291583 in healthy subjects are ... P Badorrek,C Diefenbach,H Kgler,... - 《Cts Clinical & Translational Science》 被引量: 0发表: 2024年 The preclinical and phase 1 devel...
Preclinical and phase 1 study results indicate that BI 1291583 is a reversible, highly potent and highly selective CatC inhibitor that markedly inhibits ac... James D Chalmers,Philipp Badorrek,Claudia Diefenbach,... - ERJ Open Research 被引量: 0发表: 2024年 Regioselective synthesis of N-contain...