Drug General Information
Drug ID
D05ENJ
Former ID
DIB009130
Drug Name
Fasitibant chloride
Synonyms
MEN-16132; Bradykinin B2 antagonist (inflammation), Menarini; MEN-11270 analogs, Menarini
Drug Type
Small molecular drug
Indication Osteoarthritis [ICD9: 715; ICD10:M15-M19, M47] Phase 2 [522981]
Company
The Menarini Group
Structure
Download
2D MOL

3D MOL

Formula
C36H49Cl2N6O6S+
Canonical SMILES
C1(CCOCC1)(NS(=O)(=O)c1ccc(c(COc2cccc3c2nc(cc3C)C)c1Cl)<br />Cl)C(=O)N1CCN(CC1)C(=O)[C@H](CCC[N+](C)(C)C)N.[Cl-]
PubChem Compound ID
Target and Pathway
Target(s) B2 bradykinin receptor Target Info Antagonist [531763]
KEGG Pathway Calcium signaling pathway
cGMP-PKG signaling pathway
Sphingolipid signaling pathway
Neuroactive ligand-receptor interaction
Complement and coagulation cascades
Inflammatory mediator regulation of TRP channels
Regulation of actin cytoskeleton
Endocrine and other factor-regulated calcium reabsorption
Chagas disease (American trypanosomiasis)
Pathways in cancer
NetPath Pathway TGF_beta_Receptor Signaling Pathway
PANTHER Pathway Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway
Pathway Interaction Database Direct p53 effectors
Validated transcriptional targets of deltaNp63 isoforms
Reactome Peptide ligand-binding receptors
G alpha (q) signalling events
G alpha (i) signalling events
WikiPathways ACE Inhibitor Pathway
Regulation of Actin Cytoskeleton
GPCRs, Class A Rhodopsin-like
Gastrin-CREB signalling pathway via PKC and MAPK
Nifedipine Activity
Peptide GPCRs
GPCR ligand binding
GPCR downstream signaling
References
Ref 522981ClinicalTrials.gov (NCT01091116) A Locally Injected Bradykinin Antagonist for TReatment of OSteoarthritiS. U.S. National Institutes of Health.
Ref 531763Fasitibant chloride, a kinin B??receptor antagonist, and dexamethasone interact to inhibit carrageenan-induced inflammatory arthritis in rats. Br J Pharmacol. 2012 Jun;166(4):1403-10.

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