Definition
Sivelestat is a low molecular weight synthetic inhibitor of human neutrophil elastase (NE) (neutrophil elastase and cancer), which was produced by Ono Pharmaceutical Company Co., Ltd., in 1991 as ONO-5046, N-[2-{4-(2,2-dimethylpropionyloxy) phenylsulfonylamino}-benzoyl]aminoacetic acid (MW. 434.47). The structure is illustrated in Fig. 1. This is a potent, specific, and intravenously active NE inhibitor and it is widely used to treat patients with lung injury diagnosed as SIRS (systemic inflammatory response syndrome) in Japan at a dose of 0.2 mg/kg/h for 14 days.
Structure of sivelestat, ONO-5046, N-[2-{4-(2,2-dimethylpropionyloxy) phenylsulfonylamino}-benzoyl] aminoacetic acid (MW. 434.47)
This is a preview of subscription content, log in via an institution to check access.
Access this chapter
Tax calculation will be finalised at checkout
Purchases are for personal use only
References
DiCamillo SJ, Carreras I, Panchenko MV et al (2002) Elastase-released epidermal growth factor recruits epidermal growth factor receptor and extracellular signal-regulated kinases to down-regulate tropoelastin mRNA in lung fibroblasts. J Biol Chem 277:18938–18946
Kawabata K, Suzuki M, Sugitani M et al (1991) ONO-5046, a novel inhibitor of human neutrophil elastase. Biochem Biophys Res Commun 177:814–820
Matsuzaki K, Hiramatsu Y, Homma S et al (2005) Sivelestat reduces inflammatory mediators and preserves neutrophil deformability during simulated extracorporeal circulation. Ann Thorac Surg 80:611–617
Tamakuma S, Ogawa M, Aikawa N et al (2004) Relationship between neutrophil elastase and acute lung injury in humans. Pulm Pharmacol Ther 17:271–279
Wada Y, Yoshida K, Hihara J et al (2006) Sivelestat, a specific neutrophil elastase inhibitor, suppresses the growth of gastric carcinoma cells by preventing the release of transforming growth factor-alpha. Cancer Sci 97:1037–1043
Author information
Authors and Affiliations
Corresponding author
Editor information
Editors and Affiliations
Rights and permissions
Copyright information
© 2015 Springer International Publishing Switzerland
About this entry
Cite this entry
Yoshida, K. (2015). Sivelestat. In: Schwab, M. (eds) Encyclopedia of Cancer. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-662-46875-3_5332
Download citation
DOI: https://doi.org/10.1007/978-3-662-46875-3_5332
Published:
Publisher Name: Springer, Berlin, Heidelberg
Print ISBN: 978-3-662-46874-6
Online ISBN: 978-3-662-46875-3
eBook Packages: Biomedical and Life SciencesReference Module Biomedical and Life Sciences