Nafamostat
Chemical compound
From Wikipedia, the free encyclopedia
Nafamostat mesylate (INN), a synthetic serine protease inhibitor, is a short-acting anticoagulant,[1] and it is also used for the treatment of pancreatitis. It also has some potential antiviral and anti-cancer properties.[2] Nafamostat is a fast-acting proteolytic inhibitor and used during hemodialysis to prevent the proteolysis of fibrinogen into fibrin.[3] The mechanism of action of nafamostat is as a slow tight-binding substrate, trapping the target protein in the acyl-enzyme intermediate form, resulting in apparent observed inhibition.[4][5]
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- In general: ℞ (Prescription only)
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| AHFS/Drugs.com | International Drug Names |
| Routes of administration | IV |
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| Formula | C19H17N5O2 |
| Molar mass | 347.378 g·mol−1 |
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It inhibits a large number of Lys/Arg specific serine proteinases, and is also a tryptase inhibitor, which is implicated in leaking blood vessels which is symptomatic of dengue hemorrhagic fever and of end-stage dengue shock syndrome.[6] It is available in a generic form already used for the treatment of certain bleeding complications in some countries, there are risks of severe complications such as: agranulocytosis, hyperkalemia, and anaphylaxis which must be weighed in non-emergency care.[7] In some countries, it used as a treatment for pancreatitis and pancreatic cancer.[citation needed]
This drug has been identified as a potential therapy for COVID-19,[8][9] with clinical trials in Japan possibly set to begin in March 2020.[10] With evidence that nafamostat is a potent anti-viral inhibitor in lung cells, a second round of clinical trials in Korea has begun with 10 hospitals participating.[11] Multiple Phase 2/3[12][13][14] and Phase 3[15][16] clinical trials for COVID-19 in different countries are ongoing.
It has also been reported to target tubulin, favorizing its polymerization.[17]
