Sivelestat Explained

Sivelestat (INN, research name ONO 5046, marketed as Elaspol) is an inhibitor of human neutrophil elastase.^[1]

It is used in the treatment of acute respiratory failure^[2] and preliminary studies show it may also improve neuropathic pain.^[3]

Synthesis

Sivelestat is synthesised as follows:^[4]

Notes and References

1. Kawabata K, Suzuki M, Sugitani M, Imaki K, Toda M, Miyamoto T . ONO-5046, a novel inhibitor of human neutrophil elastase . Biochemical and Biophysical Research Communications . 177 . 2 . 814–820 . June 1991 . 2049103 . 10.1016/0006-291X(91)91862-7 .
2. Imokawa S, Mori K, Harada M, Sagisaka S, Sano T, Uchiyama H, Yasuda K, Ukita T, Fujisawa T, Suda T, Chida K . 6 . [Acute respiratory failure due to pneumocystis pneumonia successfully treated with combined use of sivelestat sodium hydrate] . Japanese . Nihon Kokyuki Gakkai Zasshi = the Journal of the Japanese Respiratory Society . 46 . 6 . 461–465 . June 2008 . 18592991 . vanc .
3. Weyer AD, Stucky CL . Repurposing a leukocyte elastase inhibitor for neuropathic pain . Nature Medicine . 21 . 5 . 429–430 . May 2015 . 25951529 . 10.1038/nm.3861 . 10240018 .
4. US . 5017610 . Derivatives of p-substituted phenyl ester of pivalic acid . Imaki K, Arai Y, Okegawa T . Ono Pharmaceutical Co Ltd . 21 May 1991 .