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

General Information of Drug (ID: DM1SB94)

• Drug Name: Tiprelestat Drug Info
• Synonyms: Elafin; Recombinant leukocyte elastase/proteinase-3 inhibitor (iv, inflammation), Proteo Biotech

Indication

Disease Entry	ICD 11	Status	REF
Myocardial infarction	BA41-BA43	Phase 2	[1]

• Cross-matching ID:
  PubChem CID: 44201346
  CAS Number: CAS 820211-82-3
  TTD Drug ID: DM1SB94

Molecule-Related Drug Atlas

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Combined PR1/WT1 vaccine	DMGCTX5	Myeloid leukaemia	2B33.1	Phase 2	[3]
PMID22595175C4g	DM9SLUK	Discovery agent	N.A.	Investigative	[4]

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	[5]
Epigallocatechin gallate	DMCGWBJ	Hepatic fibrosis	DB93.0	Phase 3	[6]
Sivelestat	DM6BZCV	Crohn disease	DD70	Phase 3	[7]
AZD9668	DMB87M3	Bronchiectasis	CA24	Phase 2	[8]
L-694,458	DMA0DSJ	Cystic fibrosis	CA25	Phase 2	[9]
BAY 85-8501	DMCPUKG	Bronchiectasis	CA24	Phase 2	[10]
DX-890	DMBFZET	Acute lung injury	NB32.3	Phase 2	[5]
POL-6014	DM9B68S	Cystic fibrosis	CA25	Phase 1	[11]
AZD-9819	DMWYHXG	Chronic obstructive pulmonary disease	CA22	Phase 1	[12]
BI 1323495	DMAUKTS	Chronic obstructive pulmonary disease	CA22	Phase 1	[13]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Leukocyte proteinase-3 (PRTN3)	TT5MLC4	PRTN3_HUMAN	Modulator	[2]
Neutrophil elastase (NE)	TTPLTSQ	ELNE_HUMAN	Modulator	[2]

References

• [1] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021706)
• [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] 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.
• [5] Emerging therapies for treatment of acute lung injury and acute respiratory distress syndrome. Expert Opin Emerg Drugs. 2007 Sep;12(3):461-77.
• [6] Evaluation of human neutrophil elastase inhibitory effect of iridoid glycosides from Hedyotis diffusa. Bioorg Med Chem Lett. 2010 Jan 15;20(2):513-5.
• [7] Neutrophil elastase inhibitor (sivelestat) reduces the levels of inflammatory mediators by inhibiting NF-kB. Inflamm Res. 2009 Apr;58(4):198-203.
• [8] Clinical pipeline report, company report or official report of AstraZeneca (2009).
• [9] Neutrophil elastase inhibitors as treatment for COPD. Expert Opin Investig Drugs. 2002 Jul;11(7):965-80.
• [10] 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.
• [11] 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).
• [12] 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.
• [13] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2023. Adis Insight