Drug General Information
Drug ID
D0HG5M
Former ID
DIB000974
Drug Name
Apratastat
Synonyms
TMI-005; TMI-1; Dual TACE/MMP-13 inhibitors (inflammation), Wyeth; Dual TACE/MMP-13 inhibitors (rheumatoid arthritis), Wyeth; Dual TACE/MMP-13 inhibitors, Wyeth-Ayerst
Drug Type
Small molecular drug
Indication Rheumatoid arthritis [ICD9: 710-719, 714; ICD10:M05-M06] Phase 2 [521616], [541616]
Company
Wyeth Research
Structure
Download
2D MOL

3D MOL

Formula
C17H22N2O6S2
InChI
InChI=1S/C17H22N2O6S2/c1-17(2)15(16(21)18-22)19(9-12-26-17)27(23,24)14-7-5-13(6-8-14)25-11-4-3-10-20/h5-8,15,20,22H,9-12H2,1-2H3,(H,18,21)/t15-/m0/s1
InChIKey
MAVDNGWEBZTACC-HNNXBMFYSA-N
PubChem Compound ID
PubChem Substance ID
Target and Pathway
Target(s) Collagenase 3 Target Info Modulator [528532], [536688]
ADAM 17 Target Info Modulator [528532], [536688]
KEGG Pathway Notch signaling pathway
Alzheimer's disease
Epithelial cell signaling in Helicobacter pylori infection
NetPath Pathway IL1 Signaling Pathway
PANTHER Pathway Alzheimer disease-presenilin pathway
Plasminogen activating cascadeP00003:Alzheimer disease-amyloid secretase pathway
Notch signaling pathway
Pathway Interaction Database Urokinase-type plasminogen activator (uPA) and uPAR-mediated signalingerbb4_pathway:ErbB4 signaling events
TNF receptor signaling pathway
p75(NTR)-mediated signaling
Reactome Collagen degradation
Degradation of the extracellular matrix
Activation of Matrix Metalloproteinases
Assembly of collagen fibrils and other multimeric structuresR-HSA-1251985:Nuclear signaling by ERBB4
Regulated proteolysis of p75NTR
Activated NOTCH1 Transmits Signal to the Nucleus
Constitutive Signaling by NOTCH1 PEST Domain Mutants
Constitutive Signaling by NOTCH1 t(7
M1580_K2555) Translocation Mutant
Constitutive Signaling by NOTCH1 HD Domain Mutants
Constitutive Signaling by NOTCH1 HD+PEST Domain Mutants
TNF signaling
Growth hormone receptor signaling
WikiPathways Endochondral Ossification
Activation of Matrix Metalloproteinases
Oncostatin M Signaling Pathway
AGE/RAGE pathway
Matrix MetalloproteinasesWP61:Notch Signaling Pathway
Copper homeostasis
Notch Signaling Pathway
Growth hormone receptor signaling
BDNF signaling pathway
Alzheimers Disease
Signalling by NGF
Extrinsic Pathway for Apoptosis
References
Ref 521616ClinicalTrials.gov (NCT00095342) Study Evaluating TMI-005 in Active Rheumatoid Arthritis. U.S. National Institutes of Health.
Ref 541616(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. (Ligand id: 6482).
Ref 528532Drug evaluation: apratastat, a novel TACE/MMP inhibitor for rheumatoid arthritis. Curr Opin Investig Drugs. 2006 Nov;7(11):1014-9.
Ref 536688Drug insight: tumor necrosis factor-converting enzyme as a pharmaceutical target for rheumatoid arthritis. Nat Clin Pract Rheumatol. 2008 Jun;4(6):300-9. Epub 2008 Apr 15.

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