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

General Information of Drug (ID: DMK6GAU)

• Drug Name: PMID24556381C10f Drug Info
• Synonyms: GTPL8602; NSC748516; BDBM50449286; NSC-748516

Indication

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

• Cross-matching ID:
  PubChem CID: 54613196
  TTD Drug ID: DMK6GAU

Molecule-Related Drug Atlas

Drug(s) Targeting Bile-salt-activated lipase (CEL)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Bucelipase alfa	DM50SNX	Exocrine pancreatic insufficiency	DC35.1	Phase 3	[2]
Taurocholic Acid	DM2LZ8F	Type-2 diabetes	5A11	Phase 1/2	[3]
CVT-1	DMPWZCI	Hypercholesterolaemia	5C80.0	Terminated	[4]
PMID24556381C10l	DMOH45T	Discovery agent	N.A.	Investigative	[1]
TgBSSL	DMBFX7S	Pancreatic malfunction	DC30-DC3Z	Investigative	[5]

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	[6]
Epigallocatechin gallate	DMCGWBJ	Hepatic fibrosis	DB93.0	Phase 3	[7]
Sivelestat	DM6BZCV	Crohn disease	DD70	Phase 3	[8]
Tiprelestat	DM1SB94	Myocardial infarction	BA41-BA43	Phase 2	[9]
AZD9668	DMB87M3	Bronchiectasis	CA24	Phase 2	[10]
L-694,458	DMA0DSJ	Cystic fibrosis	CA25	Phase 2	[11]
BAY 85-8501	DMCPUKG	Bronchiectasis	CA24	Phase 2	[12]
DX-890	DMBFZET	Acute lung injury	NB32.3	Phase 2	[6]
POL-6014	DM9B68S	Cystic fibrosis	CA25	Phase 1	[13]
AZD-9819	DMWYHXG	Chronic obstructive pulmonary disease	CA22	Phase 1	[14]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Bile-salt-activated lipase (CEL)	TTTRNQW	CEL_HUMAN	Inhibitor	[1]
Neutrophil elastase (NE)	TTPLTSQ	ELNE_HUMAN	Inhibitor	[1]

References

• [1] Synthesis and evaluation of 2-(1H-indol-3-yl)-4-phenylquinolines as inhibitors of cholesterol esterase. Bioorg Med Chem Lett. 2014 Mar 15;24(6):1545-9.
• [2] ClinicalTrials.gov (NCT00743483) Efficacy of Bucelipase Alfa (BSSL) in Patients With Cystic Fibrosis and Pancreatic Insufficiency. U.S. National Institutes of Health.
• [3] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [4] Lack of effect of cholesterol esterase inhibitor CVT-1 on cholesterol absorption and LDL cholesterol in humans. Cardiovasc Drugs Ther. 1999 Sep;13(5):449-54.
• [5] 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: 2872).
• [6] Emerging therapies for treatment of acute lung injury and acute respiratory distress syndrome. Expert Opin Emerg Drugs. 2007 Sep;12(3):461-77.
• [7] Evaluation of human neutrophil elastase inhibitory effect of iridoid glycosides from Hedyotis diffusa. Bioorg Med Chem Lett. 2010 Jan 15;20(2):513-5.
• [8] Neutrophil elastase inhibitor (sivelestat) reduces the levels of inflammatory mediators by inhibiting NF-kB. Inflamm Res. 2009 Apr;58(4):198-203.
• [9] Company report (Proteo Biotech AG)
• [10] Clinical pipeline report, company report or official report of AstraZeneca (2009).
• [11] Neutrophil elastase inhibitors as treatment for COPD. Expert Opin Investig Drugs. 2002 Jul;11(7):965-80.
• [12] 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.
• [13] 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).
• [14] 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.