Drug Information

Drug General Information
Drug ID
D0B9EH
Former ID
DCL000019
Drug Name
Dermolastin
Drug Type
Small molecular drug
Indication Atopic dermatitis [ICD9: 691.8, 692.9; ICD10:L00-L99] Discontinued in Phase 2 [547642]
Company
Arriva Pharma
Structure
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2D MOL

3D MOL
Formula
C27H31NOS2
Canonical SMILES
CCN(CC=CC#CC(C)(C)C)CC1=CC(=CC=C1)OCC2=CC(=CS2)C3=CSC=C<br />3
InChI
1S/C27H31NOS2/c1-5-28(14-8-6-7-13-27(2,3)4)18-22-10-9-11-25(16-22)29-19-26-17-24(21-31-26)23-12-15-30-20-23/h6,8-12,15-17,20-21H,5,14,18-19H2,1-4H3/b8-6+
InChIKey
KIRGLCXNEVICOG-SOFGYWHQSA-N
PubChem Compound ID
6443223
PubChem Substance ID
11969045, 12014524, 14808557, 29217603, 43035751, 53466659, 57369379, 103197210, 103941282, 114567706, 134338732, 134340267, 135167254, 135650692, 163621011, 163686342, 172919320, 185974820, 234856456, 234856459, 252480125
Target and Pathway
Target(s) Leukocyte elastase Target Info Inhibitor [536190], [536840], [537435], [551533]
Cathepsin G Target Info Inhibitor [536190], [536840], [537435], [551533]
Tissue kallikrein Target Info Inhibitor [536190], [536840], [537435], [551533]
Trypsin Target Info Inhibitor [536190], [536840], [537435], [551533]
Coagulation factor IIa Target Info Inhibitor [536190], [536840], [537435], [551533]
KEGG Pathway Transcriptional misregulation in cancer
Systemic lupus erythematosushsa04080:Neuroactive ligand-receptor interaction
Lysosome
Renin-angiotensin system
Amoebiasis
Systemic lupus erythematosushsa04961:Endocrine and other factor-regulated calcium reabsorptionhsa04080:Neuroactive ligand-receptor interaction
Pancreatic secretion
Protein digestion and absorption
Influenza Ahsa04080:Neuroactive ligand-receptor interaction
Complement and coagulation cascades
Regulation of actin cytoskeleton
NetPath Pathway IL2 Signaling PathwayNetPath_11:TCR Signaling Pathway
PANTHER Pathway Blood coagulation
Pathway Interaction Database Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling
C-MYB transcription factor networkupa_upar_pathway:Urokinase-type plasminogen activator (uPA) and uPAR-mediated signalingar_pathway:Coregulation of Androgen receptor activity
Regulation of Androgen receptor activitythrombin_pathway:Thrombin/protease-activated receptor (PAR) pathway
Angiopoietin receptor Tie2-mediated signaling
FOXA2 and FOXA3 transcription factor networks
PAR4-mediated thrombin signaling events
Syndecan-4-mediated signaling events
PAR1-mediated thrombin signaling events
PathWhiz Pathway Vitamin K Metabolism
Coagulation
Reactome Collagen degradation
Degradation of the extracellular matrix
Activation of Matrix MetalloproteinasesR-HSA-1474228:Degradation of the extracellular matrix
Activation of Matrix Metalloproteinases
Metabolism of Angiotensinogen to Angiotensins
Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs)R-HSA-1592389:Activation of Matrix Metalloproteinases
Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs)
Activated PKN1 stimulates transcription of AR (androgen receptor) regulated genes KLK2 and KLK3R-HSA-1592389:Activation of Matrix Metalloproteinases
Cobalamin (Cbl, vitamin B12) transport and metabolismR-HSA-140837:Intrinsic Pathway of Fibrin Clot Formation
Common Pathway of Fibrin Clot Formation
Gamma-carboxylation of protein precursors
Transport of gamma-carboxylated protein precursors from the endoplasmic reticulum to the Golgi apparatus
Removal of aminoterminal propeptides from gamma-carboxylated proteins
Cell surface interactions at the vascular wall
Peptide ligand-binding receptors
G alpha (q) signalling events
Thrombin signalling through proteinase activated receptors (PARs)
WikiPathways Hair Follicle Development: Cytodifferentiation (Part 3 of 3)
Human Complement System
Degradation of collagenWP554:ACE Inhibitor Pathway
Regulation of Insulin-like Growth Factor (IGF) Transport and Uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs)WP2263:Prostate CancerWP2769:Activation of Matrix MetalloproteinasesWP558:Complement and Coagulation Cascades
Regulation of Actin Cytoskeleton
IL1 and megakaryotyces in obesity
Regulation of Insulin-like Growth Factor (IGF) Transport and Uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs)
PTM: gamma carboxylation, hypusine formation and arylsulfatase activation
Blood Clotting Cascade
Gastrin-CREB signalling pathway via PKC and MAPK
Thrombin signalling through proteinase activated receptors (PARs)
Platelet Aggregation (Plug Formation)
GPCR ligand binding
GPCR downstream signaling
Formation of Fibrin Clot (Clotting Cascade)
Cell surface interactions at the vascular wall
Folate Metabolism
Vitamin B12 Metabolism
Selenium Micronutrient Network
References
Ref 547642Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018071)
Ref 536190rAAt (inhaled) Arriva/Hyland Immuno. Curr Opin Mol Ther. 2006 Feb;8(1):76-82.
Ref 536840Bioreactor strategies for improving production yield and functionality of a recombinant human protein in transgenic tobacco cell cultures. Biotechnol Bioeng. 2009 Feb 1;102(2):508-20.
Ref 537435Optimization of the bioprocessing conditions for scale-up of transient production of a heterologous protein in plants using a chemically inducible viral amplicon expression system. Biotechnol Prog. 2009 May-Jun;25(3):722-34.
Ref 551533Arriva-ProMetic recombinant alpha 1-antitrypsin (rAAT) moves into the clinic for dermatology applications. ProMetic Life Sciences. 2009.

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