General Information of DTT (ID: TTPLTSQ)

DTT Name Neutrophil elastase (NE) DTT Info
Gene Name ELANE

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Discontinued Drug(s)
Approved Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Investigative Drug(s)
1 Approved Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sivelestat sodium hydrate DMOSJD0 Acute lung injury NB32.3 Phase 4 [1]
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10 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Epigallocatechin gallate DMCGWBJ Hepatic fibrosis DB93.0 Phase 3 [2]
Sivelestat DM6BZCV Crohn disease DD70 Phase 3 [3]
AZD9668 DMB87M3 Bronchiectasis CA24 Phase 2 [4]
BAY 85-8501 DMCPUKG Bronchiectasis CA24 Phase 2 [5]
DX-890 DMBFZET Acute lung injury NB32.3 Phase 2 [1]
L-694,458 DMA0DSJ Cystic fibrosis CA25 Phase 2 [6]
Tiprelestat DM1SB94 Myocardial infarction BA41-BA43 Phase 2 [7]
AZD-9819 DMWYHXG Chronic obstructive pulmonary disease CA22 Phase 1 [8]
BI 1323495 DMAUKTS Chronic obstructive pulmonary disease CA22 Phase 1 [9]
POL-6014 DM9B68S Cystic fibrosis CA25 Phase 1 [10]
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⏷ Show the Full List of 10 Clinical Trial Drug(s)
33 Patented Agent(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
2-pyrazinone derivative 1 DMWXUS4 N. A. N. A. Patented [11]
2-pyrazinone derivative 2 DMLEH4U N. A. N. A. Patented [11]
2-pyrazinone derivative 3 DME5WLD N. A. N. A. Patented [11]
2-pyrazinone derivative 4 DMJRHS4 N. A. N. A. Patented [11]
2-pyrazinone derivative 5 DMBIRMA N. A. N. A. Patented [11]
2-pyrazinone derivative 6 DMHIEBN N. A. N. A. Patented [11]
2-pyrazinone derivative 7 DMTG6X9 N. A. N. A. Patented [11]
4-pyridone derivative 1 DMMBUGK N. A. N. A. Patented [11]
4-pyridone derivative 2 DMS1O0G N. A. N. A. Patented [11]
Dihydropyrimidinone derivative 1 DMA25XH N. A. N. A. Patented [11]
Dihydropyrimidinone derivative 2 DM5Y13R N. A. N. A. Patented [11]
Hypersulfated disaccharide compound 1 DMMFI5G N. A. N. A. Patented [11]
Peptide analog 55 DMVLP8H N. A. N. A. Patented [11]
Peptide analog 56 DMBCFJU N. A. N. A. Patented [11]
Peptide analog 57 DM6IQWE N. A. N. A. Patented [11]
Peptide analog 58 DM7X62M N. A. N. A. Patented [11]
Peptide analog 59 DMZAMNX N. A. N. A. Patented [11]
Peptide analog 60 DMMSTNA N. A. N. A. Patented [11]
Peptide analog 61 DM45JMT N. A. N. A. Patented [11]
Peptide analog 62 DM28NK0 N. A. N. A. Patented [11]
Peptide analog 63 DMGC7NW N. A. N. A. Patented [11]
Peptide analog 64 DM1G2J5 N. A. N. A. Patented [11]
Peptide analog 65 DMAJLM1 N. A. N. A. Patented [11]
Peptide analog 66 DMW502M N. A. N. A. Patented [11]
Peptide analog 67 DMJ8QTX N. A. N. A. Patented [11]
Peptide analog 68 DMFG2KT N. A. N. A. Patented [11]
Peptide analog 69 DM2OXW3 N. A. N. A. Patented [11]
Peptide analog 70 DMN43Q5 N. A. N. A. Patented [11]
Pyrimidine derivative 34 DM4192V N. A. N. A. Patented [11]
Pyrimidinone derivative 4 DMDQNKW N. A. N. A. Patented [11]
Tetra-hydro-pyrrolopyrimidinedione derivative 1 DMM06K5 N. A. N. A. Patented [11]
Tetra-hydro-triazolopyrimidine derivative 2 DMI6VG9 N. A. N. A. Patented [12]
Uracil derivative 1 DM5SX8T N. A. N. A. Patented [11]
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⏷ Show the Full List of 33 Patented Agent(s)
14 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
MR-889 DMYQZBT Phlegmy cough SA80-SA8Z Discontinued in Phase 3 [6]
CE-1037 DM746L8 Chronic obstructive pulmonary disease CA22 Discontinued in Phase 2 [6]
Dermolastin DM6WSU2 Atopic dermatitis EA80 Discontinued in Phase 2 [13]
FK-706 DM524J3 Pulmonary emphysema CA21.Z Discontinued in Phase 2 [6]
ZD-8321 DMBSXPJ Acute lung injury NB32.3 Discontinued in Phase 2 [6]
AE-3763 DMRSEZD Chronic obstructive pulmonary disease CA22 Discontinued in Phase 1 [6]
AZD-6553 DMQZCET Chronic obstructive pulmonary disease CA22 Discontinued in Phase 1 [14]
FR167653 DM69OR8 Chronic obstructive pulmonary disease CA22 Discontinued in Phase 1 [6]
GW-311616 DM62T1C N. A. N. A. Discontinued in Phase 1 [6]
ZD-0892 DM82V1D Chronic obstructive pulmonary disease CA22 Discontinued in Phase 1 [6]
FR-901277 DM6PFVD N. A. N. A. Terminated [15]
FR-901451 DM2FNPO N. A. N. A. Terminated [15]
Mdl 101,146 DMRSOBG Inflammation 1A00-CA43.1 Terminated [16]
SR-26831 DM1GKTS Rheumatoid arthritis FA20 Terminated [17]
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⏷ Show the Full List of 14 Discontinued Drug(s)
47 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
(1H-pyrazol-1-yl)(o-tolyl)methanone DMACN68 Discovery agent N.A. Investigative [18]
(3,4-dichlorophenyl)(1H-pyrazol-1-yl)methanone DMNVDLI Discovery agent N.A. Investigative [18]
(3-nitro-1H-pyrazol-1-yl)(p-tolyl)methanone DMT9FZD Discovery agent N.A. Investigative [18]
(3-nitro-1H-pyrazol-1-yl)(phenyl)methanone DMD4Z6H Discovery agent N.A. Investigative [18]
(4-bromo-1H-pyrazol-1-yl)(m-tolyl)methanone DMS9125 Discovery agent N.A. Investigative [18]
(4-bromo-1H-pyrazol-1-yl)(o-tolyl)methanone DM5QDK9 Discovery agent N.A. Investigative [18]
(4-bromo-1H-pyrazol-1-yl)(p-tolyl)methanone DM31OSD Discovery agent N.A. Investigative [18]
(4-chloro-1H-pyrazol-1-yl)(o-tolyl)methanone DM4MAZ1 Discovery agent N.A. Investigative [18]
(4-nitro-1H-pyrazol-1-yl)(o-tolyl)methanone DMBPL3J Discovery agent N.A. Investigative [18]
(4-nitro-1H-pyrazol-1-yl)(phenyl)methanone DMIDUO9 Discovery agent N.A. Investigative [18]
1-(3,3-Dimethyl-2-oxo-butyl)-1H-indole-2,3-dione DMNZYWR Discovery agent N.A. Investigative [19]
1-benzoyl-N-phenyl-1H-pyrazole-3-carboxamide DMG5MNZ Discovery agent N.A. Investigative [18]
1-benzyl-3,3-diethylazetidine-2,4-dione DMPTMKU Discovery agent N.A. Investigative [20]
1-benzyl-3,3-dimethylazetidine-2,4-dione DMW59XA Discovery agent N.A. Investigative [20]
2-methylbut-3-yn-2-yl 4-methoxybenzoate DMKB2P8 Discovery agent N.A. Investigative [18]
3,3-Diethyl-1-(pyridin-3-yl)azetidine-2,4-dione DMWFD5C Discovery agent N.A. Investigative [20]
3,3-Diethyl-1-o-tolylazetidine-2,4-dione DMY8S94 Discovery agent N.A. Investigative [20]
3,3-diethyl-1-phenylazetidine-2,4-dione DMCFJIP Discovery agent N.A. Investigative [20]
3,4-dichloroisocoumarin DMOZCDK Discovery agent N.A. Investigative [21]
3-Benzyl-3-ethyl-1-phenylazetidine-2,4-dione DMDAO28 Discovery agent N.A. Investigative [20]
3-Benzyl-3-methyl-1-phenylazetidine-2,4-dione DMHINWF Discovery agent N.A. Investigative [20]
3-butyl-3-ethyl-1-phenylazetidine-2,4-dione DMOGZUK Discovery agent N.A. Investigative [20]
3-Decanoyl-4-hydroxy-6-nonyl-pyran-2-one DMLQJ64 Discovery agent N.A. Investigative [22]
3-Ethyl-3-isobutyl-1-phenylazetidine-2,4-dione DMB8Q7T Discovery agent N.A. Investigative [20]
4-Hydroxy-3-nonanoyl-6-octyl-pyran-2-one DMDEMV8 Discovery agent N.A. Investigative [22]
4-methoxy-N'-(2-phenylacetyl)benzohydrazide DMF079L Discovery agent N.A. Investigative [18]
6-Heptyl-4-hydroxy-3-octanoyl-pyran-2-one DMF3W15 Discovery agent N.A. Investigative [22]
Ac-Ala-Pro-Val-(2-benzoxazole) DMJ3C20 Discovery agent N.A. Investigative [23]
ADC-7828 DM19KY6 Chronic obstructive pulmonary disease CA22 Investigative [10]
AX-9657 DMKCT0M Pulmonary disease 1B10-1F85 Investigative [10]
Bornyl (3,4,5-trihydroxy)-cinnamate DMR70ZO Discovery agent N.A. Investigative [24]
Cbz-Val-Pro-Val-(2-benzoxazole) DM6TYRA Discovery agent N.A. Investigative [23]
DD7 DMV0JQG Acute respiratory distress syndrome CB00 Investigative [25]
E-6-O-p-methoxycinnamoyl scandoside methyl ester DM7ROJI Discovery agent N.A. Investigative [2]
ED1 DM5QS17 Acute respiratory distress syndrome CB00 Investigative [25]
ED45 DMX32JY Acute respiratory distress syndrome CB00 Investigative [25]
Fucose DMAHMSV N. A. N. A. Investigative [16]
ICI 200,355 DMLPZ3N Discovery agent N.A. Investigative [26]
ICI 200,880 DM0PQ37 Discovery agent N.A. Investigative [6]
L-658,758 DMY0IQ6 Discovery agent N.A. Investigative [27]
N,N-bis(cyanomethyl)-3,4-dimethoxybenzamide DMBQ0TY Discovery agent N.A. Investigative [18]
PMID22595175C4g DM9SLUK Discovery agent N.A. Investigative [28]
PMID24556381C10f DMK6GAU Discovery agent N.A. Investigative [29]
PMID24556381C10l DMOH45T Discovery agent N.A. Investigative [29]
TEI-8362 DMBNYJW Discovery agent N.A. Investigative [6]
WIN-63395 DMNM50K Discovery agent N.A. Investigative [30]
ZK-814048 DMCBV5F Discovery agent N.A. Investigative [31]
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⏷ Show the Full List of 47 Investigative Drug(s)
Molecule Interaction Atlas

References

1 Emerging therapies for treatment of acute lung injury and acute respiratory distress syndrome. Expert Opin Emerg Drugs. 2007 Sep;12(3):461-77.
2 Evaluation of human neutrophil elastase inhibitory effect of iridoid glycosides from Hedyotis diffusa. Bioorg Med Chem Lett. 2010 Jan 15;20(2):513-5.
3 Neutrophil elastase inhibitor (sivelestat) reduces the levels of inflammatory mediators by inhibiting NF-kB. Inflamm Res. 2009 Apr;58(4):198-203.
4 Clinical pipeline report, company report or official report of AstraZeneca (2009).
5 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.
6 Neutrophil elastase inhibitors as treatment for COPD. Expert Opin Investig Drugs. 2002 Jul;11(7):965-80.
7 Company report (Proteo Biotech AG)
8 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.
9 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2023. Adis Insight
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 Neutrophil elastase inhibitors: a patent review and potential applications for inflammatory lung diseases (2010 - 2014).Expert Opin Ther Pat. 2015;25(10):1145-58.
12 Serine protease inhibitors to treat inflammation: a patent review (2011-2016).Expert Opin Ther Pat. 2018 Feb;28(2):93-110.
13 Arriva-ProMetic recombinant alpha 1-antitrypsin (rAAT) moves into the clinic for dermatology applications. ProMetic Life Sciences. 2009.
14 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032703)
15 Resisting degradation by human elastase: commonality of design features shared by 'canonical' plant and bacterial macrocyclic protease inhibitor sc... Bioorg Med Chem. 2007 Jul 1;15(13):4618-28.
16 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
17 Biochemical and pharmacological activities of SR 26831, a potent and selective elastase inhibitor. J Pharmacol Exp Ther. 1992 Feb;260(2):809-16.
18 N-benzoylpyrazoles are novel small-molecule inhibitors of human neutrophil elastase. J Med Chem. 2007 Oct 4;50(20):4928-38.
19 Parallel synthesis of isatin-based serine protease inhibitors. Bioorg Med Chem Lett. 2000 Nov 20;10(22):2501-4.
20 4-Oxo-beta-lactams (azetidine-2,4-diones) are potent and selective inhibitors of human leukocyte elastase. J Med Chem. 2010 Jan 14;53(1):241-53.
21 Cathepsin A is the major hydrolase catalyzing the intracellular hydrolysis of the antiretroviral nucleotide phosphonoamidate prodrugs GS-7340 and G... Antimicrob Agents Chemother. 2007 Feb;51(2):543-50.
22 Inhibition of human sputum elastase by substituted 2-pyrones. J Med Chem. 1987 Jun;30(6):1017-23.
23 Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality. Bioorg Med Chem. 2008 Feb 15;16(4):1562-95.
24 Bornyl (3,4,5-trihydroxy)-cinnamate--an optimized human neutrophil elastase inhibitor designed by free energy calculations. Bioorg Med Chem. 2008 Mar 1;16(5):2385-90.
25 Therapeutic applications of aptamers. Expert Opin Investig Drugs. 2008 Jan;17(1):43-60.
26 Role of neutrophil elastase in hypersecretion in asthma. Eur Respir J. 1999 Jan;13(1):190-6.
27 Neutrophil elastase promotes lung microvascular injury and proteolysis of endothelial cadherins. Am J Physiol. 1998 Aug;275(2 Pt 2):H385-92.
28 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.
29 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.
30 A comparative SAR and computer modeling study of benzisothiazolone, mechanism-based inhibitors with porcine pancreatic and human leukocyte elastase, Bioorg. Med. Chem. Lett. 6(24):2941-2946 (1996).
31 Thiophene-anthranilamides as highly potent and orally available factor Xa inhibitors. J Med Chem. 2007 Jun 28;50(13):2967-80.