Nafamostat

Nafamostat mesylate
Clinical data
AHFS/Drugs.com	International Drug Names
Routes of; administration	IV
ATC code	none;
Legal status
Legal status	In general: ℞ (Prescription only);
Identifiers
	IUPAC name 6-[amino(imino)methyl]-2-naphthyl 4-{[amino(imino)methyl]amino}benzoate;
CAS Number	81525-10-2 ;
PubChem CID	4413;
IUPHAR/BPS	4262;
ChemSpider	4260 ;
UNII	Y25LQ0H97D;
KEGG	D01670 ;
CompTox Dashboard (EPA)	DTXSID0048420 ;
Chemical and physical data
Formula	C19H17N5O2
Molar mass	347.378 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1=CC(=CC=C1C(=O)OC2=CC3=C(C=C2)C=C(C=C3)C(=N)N)N=C(N)N;
	InChI 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) ; Key:MQQNFDZXWVTQEH-UHFFFAOYSA-N ;
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Nafamostat mesylate (INN), a synthetic serine protease inhibitor, it is a short-acting anticoagulant,[1] and 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]

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. 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.[4] In some countries, it used as a treatment for pancreatitis and pancreatic cancer.

This drug has been identified as a potential therapy for COVID-19,[5] with clinical trials in Japan possibly set to begin in March 2020.[6] 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.[7]

References

Al-Horani RA, Desai UR (November 2014). "Recent advances on plasmin inhibitors for the treatment of fibrinolysis-related disorders". Medicinal Research Reviews. 34 (6): 1168–216. doi:10.1002/med.21315. PMID 24659483.
Chen X, Xu Z, Zeng S, Wang X, Liu W, Qian L, et al. (2019). "The Molecular Aspect of Antitumor Effects of Protease Inhibitor Nafamostat Mesylate and Its Role in Potential Clinical Applications". Frontiers in Oncology. 9: 852. doi:10.3389/fonc.2019.00852. PMC 6733886. PMID 31552177.
Sadahiro T, Yuzawa H, Kimura T, Oguchi M, Morito T, Mizushima S, Hirose Y (2018). "Current Practices in Acute Blood Purification Therapy in Japan and Topics for Further Study". Contributions to Nephrology. 196: 209–214. doi:10.1159/000485724. PMID 30041229.
PubChem. "Nafamostat". pubchem.ncbi.nlm.nih.gov. Retrieved 2020-06-17.
Wang M, Cao R, Zhang L, Yang X, Liu J, Xu M, et al. (March 2020). "Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitro". Cell Research. 30 (3): 269–271. doi:10.1038/s41422-020-0282-0. PMC 7054408. PMID 32020029.
"Japanese researchers to test blood thinner for coronavirus treatment". The Japan Times Online. 2020-03-19. ISSN 0447-5763. Retrieved 2020-03-24.
Ltd, John Wiley & Sons; The Atrium, Southern Gate; Chichester; PO19 8SQ; Tel : 01243 779777; Fax : 01243 770421. "Korean researchers find drug that is more effective in treating COVID-19 than remdesivir | Pharmafile". www.pharmafile.com. Retrieved 2020-06-17.

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[pmid24659483-1] Al-Horani RA, Desai UR (November 2014). "Recent advances on plasmin inhibitors for the treatment of fibrinolysis-related disorders". Medicinal Research Reviews. 34 (6): 1168–216. doi:10.1002/med.21315. PMID 24659483.

[pmid31552177-2] Chen X, Xu Z, Zeng S, Wang X, Liu W, Qian L, et al. (2019). "The Molecular Aspect of Antitumor Effects of Protease Inhibitor Nafamostat Mesylate and Its Role in Potential Clinical Applications". Frontiers in Oncology. 9: 852. doi:10.3389/fonc.2019.00852. PMC 6733886. PMID 31552177.

[pmid30041229-3] Sadahiro T, Yuzawa H, Kimura T, Oguchi M, Morito T, Mizushima S, Hirose Y (2018). "Current Practices in Acute Blood Purification Therapy in Japan and Topics for Further Study". Contributions to Nephrology. 196: 209–214. doi:10.1159/000485724. PMID 30041229.

[4] PubChem. "Nafamostat". pubchem.ncbi.nlm.nih.gov. Retrieved 2020-06-17.

[pmid32020029-5] Wang M, Cao R, Zhang L, Yang X, Liu J, Xu M, et al. (March 2020). "Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitro". Cell Research. 30 (3): 269–271. doi:10.1038/s41422-020-0282-0. PMC 7054408. PMID 32020029.

[6] "Japanese researchers to test blood thinner for coronavirus treatment". The Japan Times Online. 2020-03-19. ISSN 0447-5763. Retrieved 2020-03-24.

[7] Ltd, John Wiley & Sons; The Atrium, Southern Gate; Chichester; PO19 8SQ; Tel : 01243 779777; Fax : 01243 770421. "Korean researchers find drug that is more effective in treating COVID-19 than remdesivir | Pharmafile". www.pharmafile.com. Retrieved 2020-06-17.