General Information of Drug (ID: DM6WSU2)

Drug Name
Dermolastin Drug Info
Synonyms Dermolastin
Indication
Disease Entry ICD 11 Status REF
Atopic dermatitis EA80 Discontinued in Phase 2 [1]
Cross-matching ID
PubChem CID
188403
TTD Drug ID
DM6WSU2

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Clinical Trial Drug(s)
Investigative Drug(s)
Approved Drug(s)
Discontinued Drug(s)
Patented Agent(s)
Drug(s) Targeting Tissue kallikrein (KLK2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Avoralstat DM5YHU2 Hereditary angioedema 4A00.14 Phase 2/3 [3]
VDA-1102 DMAJ85O Actinic keratosis EK90.0 Phase 2 [4]
JNJ-69086420 DM6VR13 Prostate cancer 2C82.0 Phase 1 [5]
JNJ-78278343 DM27FAN Prostate cancer 2C82.0 Phase 1 [6]
JNJ-75229414 DMV6XBC Prostate cancer 2C82.0 Phase 1 [7]
DM-107 DMRYQVJ Atopic dermatitis EA80 Investigative [8]
hK2p01 derivative KLK2 inhibitor DME13RQ Discovery agent N.A. Investigative [9]
⏷ Show the Full List of 7 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Bortezomib DMNO38U Leukemia Approved [10]
MELAGATRAN DM4W8RE N. A. N. A. Phase 3 [11]
Ulinastatin DMIQCFG Premature labour JB00 Phase 3 [12]
Alpha-1 antitrypsin DM5EFXZ Coagulation defect 3B10.0 Phase 2 [13]
RWJ-56423 DM6BIHE Asthma CA23 Discontinued in Phase 1 [14]
Patamostat DM6HBQJ Hypotension BA20-BA21 Terminated [13]
BMY-44621 DM8R3N0 N. A. N. A. Terminated [15]
Grassystatin a DM1PWX2 Discovery agent N.A. Investigative [16]
2-(2-Hydroxy-phenyl)-1H-indole-5-carboxamidine DM3UMYD Discovery agent N.A. Investigative [17]
4-(4-Benzyloxy-3-methoxy-benzylamino)-benzamidine DME3PUT Discovery agent N.A. Investigative [18]
⏷ Show the Full List of 10 Drug(s)
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 [19]
Epigallocatechin gallate DMCGWBJ Hepatic fibrosis DB93.0 Phase 3 [20]
Sivelestat DM6BZCV Crohn disease DD70 Phase 3 [21]
Tiprelestat DM1SB94 Myocardial infarction BA41-BA43 Phase 2 [22]
AZD9668 DMB87M3 Bronchiectasis CA24 Phase 2 [23]
L-694,458 DMA0DSJ Cystic fibrosis CA25 Phase 2 [24]
BAY 85-8501 DMCPUKG Bronchiectasis CA24 Phase 2 [25]
DX-890 DMBFZET Acute lung injury NB32.3 Phase 2 [19]
POL-6014 DM9B68S Cystic fibrosis CA25 Phase 1 [26]
AZD-9819 DMWYHXG Chronic obstructive pulmonary disease CA22 Phase 1 [27]
⏷ Show the Full List of 10 Drug(s)
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 [28]
Peptide analog 59 DMZAMNX N. A. N. A. Patented [29]
Peptide analog 61 DM45JMT N. A. N. A. Patented [29]
Peptide analog 55 DMVLP8H N. A. N. A. Patented [29]
Peptide analog 60 DMMSTNA N. A. N. A. Patented [29]
Peptide analog 70 DMN43Q5 N. A. N. A. Patented [29]
Peptide analog 56 DMBCFJU N. A. N. A. Patented [29]
Peptide analog 57 DM6IQWE N. A. N. A. Patented [29]
Peptide analog 58 DM7X62M N. A. N. A. Patented [29]
Peptide analog 62 DM28NK0 N. A. N. A. Patented [29]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Coagulation factor IIa (F2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Argatroban DMFI46A Thrombosis DB61-GB90 Approved [30]
Pyridoxal Phosphate DMO2K0J Malnutrition 5B50-5B71 Approved [31]
Bivalirudin DMECRX1 Thrombocytopenia 3B64 Approved [32]
Ximelegatran DMU8ANS Myocardial infarction BA41-BA43 Approved [33]
Dabigatran DMDI6R4 Stroke 8B20 Approved [34]
Desirudin Recombinant DM2BTFN Coagulation defect 3B10.0 Approved [35]
Human prothrombin complex concentrate DMPHVQ1 Bleeding disorder GA20-GA21 Approved [36]
Lepirudin DM1I3D5 Thrombocytopenia 3B64 Approved [37]
Anisindione DM2C48U Coagulation defect 3B10.0 Approved [38]
ATryn antithrombin DM79Y2T Multiple sclerosis 8A40 Approved [39]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Cathepsin G (CTSG) TTQAJF1 CATG_HUMAN Inhibitor [2]
Cationic trypsinogen (PRSS1) TT2WR1T TRY1_HUMAN Inhibitor [2]
Coagulation factor IIa (F2) TT6L509 THRB_HUMAN Inhibitor [2]
Neutrophil elastase (NE) TTPLTSQ ELNE_HUMAN Inhibitor [2]
Tissue kallikrein (KLK2) TTJLNAW KLK2_HUMAN Inhibitor [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 800018071)
2 Arriva-ProMetic recombinant alpha 1-antitrypsin (rAAT) moves into the clinic for dermatology applications. ProMetic Life Sciences. 2009.
3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4 Clinical pipeline report, company report or official report of Vidac Pharma.
5 ClinicalTrials.gov (NCT04644770) A Study of JNJ-69086420, an Actinium-225-Labeled Antibody Targeting Human Kallikrein-2 (hK2) for Advanced Prostate Cancer. U.S. National Institutes of Health.
6 ClinicalTrials.gov (NCT04898634) A Phase 1 Study of JNJ-78278343, a T-Cell-Redirecting Agent Targeting Human Kallikrein 2 (KLK2), for Advanced Prostate Cancer. U.S.National Institutes of Health.
7 ClinicalTrials.gov (NCT05022849) A Phase 1, Dose Escalation Study of JNJ-75229414, a Chimeric Antigen Receptor T Cell (CAR-T) Therapy Directed Against KLK2 for Metastatic Castration-Resistant Prostate Cancer. U.S.National Institutes of Health.
8 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: 2372).
9 Novel peptide inhibitors of human kallikrein 2. J Biol Chem. 2006 May 5;281(18):12555-60.
10 Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin. J Med Chem. 1995 Apr 28;38(9):1511-22.
11 Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety. Bioorg Med Chem Lett. 2006 May 15;16(10):2641-7.
12 Intravenous administration of ulinastatin (human urinary trypsin inhibitor) in severe sepsis: a multicenter randomized controlled study. Intensive Care Med. 2014 Jun;40(6):830-8.
13 US patent application no. 2012,0251,516, PHARMACEUTICAL COMPOSITION FOR TREATING CANCER COMPRISING TRYPSINOGEN AND/OR CHYMOTRYPSINOGEN AND AN ACTIVE AGENT SELECTED FROM A SELENIUM COMPOUND, A VANILLOID COMPOUND AND A CYTOPLASMIC GLYCOLYSIS REDUCTION AGENT.
14 Inhibitors of serine proteases as potential therapeutic agents: the road from thrombin to tryptase to cathepsin G. J Med Chem. 2004 Feb 12;47(4):769-87.
15 Design and synthesis of conformationally constrained arginal thrombin inhibitors, Bioorg. Med. Chem. Lett. 7(17):2205-2210 (1997).
16 Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. J Med Chem. 2009 Sep 24;52(18):5732-47.
17 Development of serine protease inhibitors displaying a multicentered short (<2.3 A) hydrogen bond binding mode: inhibitors of urokinase-type plasmi... J Med Chem. 2001 Aug 16;44(17):2753-71.
18 Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors. Bioorg Med Chem Lett. 2005 Feb 1;15(3):817-22.
19 Emerging therapies for treatment of acute lung injury and acute respiratory distress syndrome. Expert Opin Emerg Drugs. 2007 Sep;12(3):461-77.
20 Evaluation of human neutrophil elastase inhibitory effect of iridoid glycosides from Hedyotis diffusa. Bioorg Med Chem Lett. 2010 Jan 15;20(2):513-5.
21 Neutrophil elastase inhibitor (sivelestat) reduces the levels of inflammatory mediators by inhibiting NF-kB. Inflamm Res. 2009 Apr;58(4):198-203.
22 Company report (Proteo Biotech AG)
23 Clinical pipeline report, company report or official report of AstraZeneca (2009).
24 Neutrophil elastase inhibitors as treatment for COPD. Expert Opin Investig Drugs. 2002 Jul;11(7):965-80.
25 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.
26 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).
27 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.
28 Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase. J Med Chem. 2007 Apr 19;50(8):1727-30.
29 Neutrophil elastase inhibitors: a patent review and potential applications for inflammatory lung diseases (2010 - 2014).Expert Opin Ther Pat. 2015;25(10):1145-58.
30 Studies on the different modes of action of the anticoagulant protease inhibitors DX-9065a and Argatroban. I. Effects on thrombin generation. J Biol Chem. 2002 Dec 27;277(52):50439-44.
31 New antithrombotic drugs (excluding plasminogen activators. Arch Mal Coeur Vaiss. 2001 Nov;94(11 Suppl):1225-32.
32 New anticoagulants. Am Heart J. 2001 Aug;142(2 Suppl):S3-8.
33 Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90.
34 Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
35 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
36 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: 2362).
37 Recombinant hirudin (lepirudin) as anticoagulant in intensive care patients treated with continuous hemodialysis. Kidney Int Suppl. 1999 Nov;(72):S46-50.
38 Anticoagulation with anisindione in a patient with a warfarin-induced skin eruption. Pharmacotherapy. 2003 Apr;23(4):533-6.
39 Antithrombin III Utilization in a Large Teaching Hospital. P T. 2013 December; 38(12): 764-767, 779.