Nafamostat

Source: Wikipedia, the free encyclopedia.
Nafamostat mesylate
Clinical data
AHFS/Drugs.comInternational Drug Names
Routes of
administration
IV
ATC code
  • none
Legal status
Legal status
  • In general: ℞ (Prescription only)
Identifiers
  • 6-[amino(imino)methyl]-2-naphthyl 4-{[amino(imino)methyl]amino}benzoate
JSmol)
  • N=C(N)c1ccc2cc(OC(=O)c3ccc(N=C(N)N)cc3)ccc2c1
  • InChI=1S/C19H17N5O2/c20-17(21)14-2-1-13-10-16(8-5-12(13)9-14)26-18(25)11-3-6-15(7-4-11)24-19(22)23/h1-10H,(H3,20,21)(H4,22,23,24) ☒N
  • Key:MQQNFDZXWVTQEH-UHFFFAOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Nafamostat mesylate (

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]

It inhibits a large number of Lys/Arg specific serine proteinases, and is also a

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] with clinical trials in Japan possibly set to begin in March 2020.[9] 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.[10] Multiple Phase 2/3[11][12][13] and Phase 3[14][15] clinical trials for COVID-19 in different countries are ongoing.

References

  1. S2CID 22631056
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  7. ^ "Nafamostat". PubChem. U.S. National Library of Medicine. Retrieved 17 June 2020.
  8. PMID 32020029
    .
  9. . Retrieved 24 March 2020.
  10. ^ "Korean researchers find drug that is more effective in treating COVID-19 than remdesivir". Pharmafile. 15 May 2020. Retrieved 2020-06-17.
  11. ^ Clinical trial number NCT04473053 for "Rapid Experimental Medicine for COVID-19" at ClinicalTrials.gov
  12. ^ Clinical trial number NCT04352400 for "Efficacy of Nafamostat in Covid-19 Patients (RACONA Study)" at ClinicalTrials.gov
  13. ^ Clinical trial number NCT04418128 for "Clinical Efficacy of Nafamostat Mesylate for COVID-19 Pneumonia" at ClinicalTrials.gov
  14. ^ Clinical trial number NCT04483960 for "Australasian COVID-19 Trial (ASCOT) ADAptive Platform Trial" at ClinicalTrials.gov
  15. ^ Clinical trial number NCT04390594 for "Efficacy and Safety Evaluation of Treatment Regimens in Adult COVID-19 Patients in Senegal" at ClinicalTrials.gov