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

General Information of Drug (ID: DM9SLUK)

• Drug Name: PMID22595175C4g Drug Info
• Synonyms: GTPL8626; BDBM50384111

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 66561876
  TTD Drug ID: DM9SLUK

Molecule-Related Drug Atlas

Drug(s) Targeting Leukocyte proteinase-3 (PRTN3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tiprelestat	DM1SB94	Myocardial infarction	BA41-BA43	Phase 2	[2]
Combined PR1/WT1 vaccine	DMGCTX5	Myeloid leukaemia	2B33.1	Phase 2	[3]

Drug(s) Targeting Neutrophil elastase (NE)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sivelestat sodium hydrate	DMOSJD0	Acute lung injury	NB32.3	Phase 4	[4]
Epigallocatechin gallate	DMCGWBJ	Hepatic fibrosis	DB93.0	Phase 3	[5]
Sivelestat	DM6BZCV	Crohn disease	DD70	Phase 3	[6]
Tiprelestat	DM1SB94	Myocardial infarction	BA41-BA43	Phase 2	[2]
AZD9668	DMB87M3	Bronchiectasis	CA24	Phase 2	[7]
L-694,458	DMA0DSJ	Cystic fibrosis	CA25	Phase 2	[8]
BAY 85-8501	DMCPUKG	Bronchiectasis	CA24	Phase 2	[9]
DX-890	DMBFZET	Acute lung injury	NB32.3	Phase 2	[4]
POL-6014	DM9B68S	Cystic fibrosis	CA25	Phase 1	[10]
AZD-9819	DMWYHXG	Chronic obstructive pulmonary disease	CA22	Phase 1	[11]

Drug(s) Targeting Cathepsin G (CTSG)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
JNJ-10311795	DM7OTQS	Chronic obstructive pulmonary disease	CA22	Phase 2	[12]
Peptide analog 59	DMZAMNX	N. A.	N. A.	Patented	[13]
Peptide analog 61	DM45JMT	N. A.	N. A.	Patented	[13]
Peptide analog 55	DMVLP8H	N. A.	N. A.	Patented	[13]
Peptide analog 60	DMMSTNA	N. A.	N. A.	Patented	[13]
Peptide analog 70	DMN43Q5	N. A.	N. A.	Patented	[13]
Peptide analog 56	DMBCFJU	N. A.	N. A.	Patented	[13]
Peptide analog 57	DM6IQWE	N. A.	N. A.	Patented	[13]
Peptide analog 58	DM7X62M	N. A.	N. A.	Patented	[13]
Peptide analog 62	DM28NK0	N. A.	N. A.	Patented	[13]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Cathepsin G (CTSG)	TTQAJF1	CATG_HUMAN	Inhibitor	[1]
Leukocyte proteinase-3 (PRTN3)	TT5MLC4	PRTN3_HUMAN	Inhibitor	[1]
Neutrophil elastase (NE)	TTPLTSQ	ELNE_HUMAN	Inhibitor	[1]

References

• [1] N-Acyl and N-sulfonyloxazolidine-2,4-diones are pseudo-irreversible inhibitors of serine proteases. Bioorg Med Chem Lett. 2012 Jun 15;22(12):3993-7.
• [2] Company report (Proteo Biotech AG)
• [3] Leukemia-associated antigen-specific T-cell responses following combined PR1 and WT1 peptide vaccination in patients with myeloid malignancies. Blood. 2008 Jan 1;111(1):236-42.
• [4] Emerging therapies for treatment of acute lung injury and acute respiratory distress syndrome. Expert Opin Emerg Drugs. 2007 Sep;12(3):461-77.
• [5] Evaluation of human neutrophil elastase inhibitory effect of iridoid glycosides from Hedyotis diffusa. Bioorg Med Chem Lett. 2010 Jan 15;20(2):513-5.
• [6] Neutrophil elastase inhibitor (sivelestat) reduces the levels of inflammatory mediators by inhibiting NF-kB. Inflamm Res. 2009 Apr;58(4):198-203.
• [7] Clinical pipeline report, company report or official report of AstraZeneca (2009).
• [8] Neutrophil elastase inhibitors as treatment for COPD. Expert Opin Investig Drugs. 2002 Jul;11(7):965-80.
• [9] 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.
• [10] 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).
• [11] 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.
• [12] Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase. J Med Chem. 2007 Apr 19;50(8):1727-30.
• [13] Neutrophil elastase inhibitors: a patent review and potential applications for inflammatory lung diseases (2010 - 2014).Expert Opin Ther Pat. 2015;25(10):1145-58.