Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMOSJD0)

• Drug Name: Sivelestat sodium hydrate Drug Info
• Synonyms: sivelestat sodium hydrate; Sivelestat sodium tetrahydrate; 201677-61-4; Elaspol; Sodium sivelestat; EI546 sodium; UNII-737RR8Y409; Sivelestat (sodium tetrahydrate); LY544349 sodium; Sivelestat sodium [USAN]; Sivelestat sodium (USAN); 737RR8Y409; DSSTox_CID_26727; DSSTox_RID_81857; DSSTox_GSID_46727; sodium 2-[[2-[[4-(2,2-dimethylpropanoyloxy)phenyl]sulfonylamino]benzoyl]amino]acetate tetrahydrate; LY544349 Sodium Hydrate; Elaspol (TN); CAS-201677-61-4; NCGC00167577-01; AC1L4KMF; Sivelestat sodium hydrate (JAN); Sodium 2-[[2-[[4-(2,2-dimethylpropanoyloxy)phenyl]sulfonylamino]benzoyl]amino]acetate tetrahydrate; Sodium ((2-(((4-((2,2-dimethylpropanoyl)oxy)phenyl)sulfonyl)amino)benzoyl)amino)acetate tetrahydrate; Glycine, N-(2-(((4-(2,2-dimethyl-1-oxopropoxy)phenyl)sulfonyl)amino)benzoyl)-, monosodium salt, tetrahydrate

Indication

Disease Entry	ICD 11	Status	REF
Acute lung injury	NB32.3	Phase 4	[1]
Community-acquired pneumonia	CA40.Z	Phase 2	[2]

• Cross-matching ID:
  PubChem CID: 23663985
  ChEBI ID: CHEBI:32133
  CAS Number: CAS 201677-61-4
  TTD Drug ID: DMOSJD0

Molecule-Related Drug Atlas

Drug(s) Targeting Serine protease unspecific (SP)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Nafamostat	DMU1XOD	Pancreatitis	DC31-DC34	Approved	[4]
Gabexate	DMU9D2F	Pancreatitis	DC31-DC34	Approved	[4]
Aprotinin	DM0QD4W	Bleeding disorder	GA20-GA21	Approved	[5]
Camostat	DMQ7UL8	Cystic fibrosis	CA25	Phase 2	[6]
VT-111a	DMY9ZGN	Acute coronary syndrome	BA41	Phase 2	[7]
Sepimostat mesylate	DMRBYH8	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 3	[8]
VT-111	DMOY15R	Graft rejection in heart transplantation	NE84	Preclinical	[9]
NPI-1999	DMH1YL8	Thrombosis	DB61-GB90	Terminated	[10]
SDZ-MTH-958	DMKCXBJ	Artery stenosis	BD52	Terminated	[11]

Drug(s) Targeting Neutrophil elastase (NE)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Epigallocatechin gallate	DMCGWBJ	Hepatic fibrosis	DB93.0	Phase 3	[12]
Sivelestat	DM6BZCV	Crohn disease	DD70	Phase 3	[13]
Tiprelestat	DM1SB94	Myocardial infarction	BA41-BA43	Phase 2	[14]
AZD9668	DMB87M3	Bronchiectasis	CA24	Phase 2	[15]
L-694,458	DMA0DSJ	Cystic fibrosis	CA25	Phase 2	[16]
BAY 85-8501	DMCPUKG	Bronchiectasis	CA24	Phase 2	[17]
DX-890	DMBFZET	Acute lung injury	NB32.3	Phase 2	[3]
POL-6014	DM9B68S	Cystic fibrosis	CA25	Phase 1	[18]
AZD-9819	DMWYHXG	Chronic obstructive pulmonary disease	CA22	Phase 1	[19]
BI 1323495	DMAUKTS	Chronic obstructive pulmonary disease	CA22	Phase 1	[20]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Neutrophil elastase (NE)	TTPLTSQ	ELNE_HUMAN	Inhibitor	[3]
Serine protease unspecific (SP)	TTEMV5X	NOUNIPROTAC	Inhibitor	[2]

References

• [1] Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.
• [2] Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91.
• [3] Emerging therapies for treatment of acute lung injury and acute respiratory distress syndrome. Expert Opin Emerg Drugs. 2007 Sep;12(3):461-77.
• [4] Tryptase-positive mast cells correlate with angiogenesis in early breast cancer patients. Int J Oncol. 2009 Jul;35(1):115-20.
• [5] Randomized controlled trials of aprotinin in cardiac surgery: could clinical equipoise have stopped the bleeding Clin Trials. 2005;2(3):218-29; discussion 229-32.
• [6] Camostat mesilate inhibits prostasin activity and reduces blood pressure and renal injury in salt-sensitive hypertension. J Hypertens. 2009 Jan;27(1):181-9.
• [7] Viral Serpin Therapeutics: From Concept to Clinic. Methods Enzymol. 2011; 499: 301-329.
• [8] Effect of FUT-187, oral serine protease inhibitor, on inflammation in the gastric remnant. Gan To Kagaku Ryoho. 1996 Dec;23(14):1971-9.
• [9] New developments in immunosuppressive therapy for heart transplantation. Expert Opin Emerg Drugs. 2009 Mar;14(1):1-21.
• [10] US patent application no. 2005,0096,323, Diketopiperazine derivatives to inhibit thrombin.
• [11] Thrombin inhibition in an ex vivo model of porcine heart xenograft hyperacute rejection. Transplantation. 1996 Mar 27;61(6):862-8.
• [12] Evaluation of human neutrophil elastase inhibitory effect of iridoid glycosides from Hedyotis diffusa. Bioorg Med Chem Lett. 2010 Jan 15;20(2):513-5.
• [13] Neutrophil elastase inhibitor (sivelestat) reduces the levels of inflammatory mediators by inhibiting NF-kB. Inflamm Res. 2009 Apr;58(4):198-203.
• [14] Company report (Proteo Biotech AG)
• [15] Clinical pipeline report, company report or official report of AstraZeneca (2009).
• [16] Neutrophil elastase inhibitors as treatment for COPD. Expert Opin Investig Drugs. 2002 Jul;11(7):965-80.
• [17] Freezing the Bioactive Conformation to Boost Potency: The Identification of BAY 5-8501, a Selective and Potent Inhibitor of Human Neutrophil Elastase for Pulmonary Diseases. ChemMedChem. 2015 Jul;10(7):1163-73.
• [18] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2358).
• [19] Lipid Peroxide-Mediated Oxidative Rearrangement of the Pyrazinone Carboxamide Core of Neutrophil Elastase Inhibitor AZD9819 in Blood Plasma Samples. Drug Metab Dispos. 2015 Oct;43(10):1441-9.
• [20] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2023. Adis Insight