Drug General Information
Drug ID
D04ZBT
Former ID
DCL000131
Drug Name
Icatibant
Synonyms
Firazyr; Icatibant [INN]; HOE 140; HOE140; JE049; WIN 65365; Hoe-140; WIN-65365; D-Arg(Hyp(3)-Thi(5)-D-Tic(7)-Oic(8))BK
Drug Type
Small molecular drug
Indication Hereditary angioedema [ICD9: 277.6; ICD10:D84.1] Approved [531783], [532041], [541774]
Therapeutic Class
Antiinflammatory Agents
Company
Jerini AG
Structure
Download
2D MOL

3D MOL

Formula
C59H89N19O13S
CAS Number
CAS 138614-30-9
PubChem Compound ID
PubChem Substance ID
Target and Pathway
Target(s) B2 bradykinin receptor Target Info Antagonist [534937], [537337], [537519]
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 5317832011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
Ref 532041Icatibant , the bradykinin B2 receptor antagonist with target to the interconnected kinin systems. Expert Opin Pharmacother. 2012 Oct;13(15):2233-47.
Ref 541774(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: 667).
Ref 534937Bradykinin in the heart: friend or foe? Circulation. 1999 Dec 7;100(23):2305-7.
Ref 537337Pharmacological characterization of the bradykinin B2 receptor antagonist MEN16132 in rat in vitro bioassays. Eur J Pharmacol. 2009 Aug 1;615(1-3):10-6. Epub 2009 May 13.
Ref 537519Bradykinin receptor antagonists--a review of the patent literature 2005-2008. Expert Opin Ther Pat. 2009 Jul;19(7):919-41.

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