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Namespace Prefixes

PrefixIRI
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n16http://linked.opendata.cz/resource/drugbank/drug/DB06196/identifier/national-drug-code-directory/
n14http://www.rxlist.com/
n25http://bio2rdf.org/drugbank:
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n15http://linked.opendata.cz/resource/drugbank/drug/DB06196/identifier/wikipedia/
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n22http://www.drugs.com/cdi/
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n19http://linked.opendata.cz/resource/atc/
n18http://linked.opendata.cz/ontology/sukl/drug/

Statements

Subject Item
n2:DB06196
rdf:type
n3:Drug
n3:description
Icatibant (Firazyr) is a synthetic peptidomimetic drug consisting of ten amino acids, and acts as an effective and specific antagonist of bradykinin B2 receptors. It has been approved in the EU for use in hereditary angioedema, and is under investigation for a number of other conditions in which bradykinin is thought to play a significant role. Icatibant currently has orphan drug status in the United States and FDA approved on August 25, 2011.
n3:dosage
n4:271B4996-363D-11E5-9242-09173F13E4C5 n4:271B4995-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Cockcroft JR, Chowienczyk PJ, Brett SE, Bender N, Ritter JM: Inhibition of bradykinin-induced vasodilation in human forearm vasculature by icatibant, a potent B2-receptor antagonist. Br J Clin Pharmacol. 1994 Oct;38(4):317-21. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/7833220 # Bork K, Frank J, Grundt B, Schlattmann P, Nussberger J, Kreuz W: Treatment of acute edema attacks in hereditary angioedema with a bradykinin receptor-2 antagonist (Icatibant). J Allergy Clin Immunol. 2007 Jun;119(6):1497-503. Epub 2007 Apr 5. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17418383
n3:group
approved
n3:halfLife
After subcutaneous administration, mean elimination half-life was 1.4 ± 0.4 hours.
n3:indication
Approved for use in acute attacks of hereditary angioedema (HAE). Investigated for use/treatment in angioedema, liver disease, and burns and burn infections.
owl:sameAs
n9:DB06196 n25:DB06196
dcterms:title
Icatibant
adms:identifier
n11:68564 n12:D04492 n15:Icatibant n16:54092-702-02 n17:PA164749185 n23:71364 n24:99443237 n26:64461 n27:DB06196 n28:50142947
n3:mechanismOfAction
Bradykinin is a peptide-based hormone that is formed locally in tissues, very often in response to a trauma. It increases vessel permeability, dilates blood vessels and causes smooth muscle cells to contract. Bradykinin plays an important role in the mediation of pain. Surplus bradykinin is responsible for the typical symptoms of inflammation, such as swelling, redness, overheating and pain. These symptoms are mediated by activation of bradykinin B2 receptors. In patients with HAE, they have an absent or dysfunctional C1-esterase inhibitor. This inhibitor is responsible for the production of bradykinin in which displacement of bradykinin from B2 receptors by icatibant has an inhibitory effect on the receptor for a relatively long time.
n3:patent
n29:5648333
n3:routeOfElimination
Urine (<10% unchanged)
n3:synonym
HOE 140
n3:volumeOfDistribution
Vdss, subcutaneous injection = 29.0 ± 8.7 L.
n18:hasAHFSCode
n20:92-32
n3:salt
n6:hasConcept
n7:M0180524
foaf:page
n14:firazyr-drug.htm n22:icatibant.html
n3:IUPAC-Name
n5:271B499B-363D-11E5-9242-09173F13E4C5
n3:InChI
n5:271B49A1-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n5:271B49A0-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n5:271B499D-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n5:271B499E-363D-11E5-9242-09173F13E4C5
n3:SMILES
n5:271B499F-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n5:271B4999-363D-11E5-9242-09173F13E4C5 n5:271B49B1-363D-11E5-9242-09173F13E4C5
n3:logP
n5:271B4997-363D-11E5-9242-09173F13E4C5 n5:271B499A-363D-11E5-9242-09173F13E4C5
n3:logS
n5:271B4998-363D-11E5-9242-09173F13E4C5
n18:hasATCCode
n19:B06AC02
n3:H-Bond-Acceptor-Count
n5:271B49A7-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n5:271B49A8-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n5:271B49A2-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n5:271B49A3-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n5:271B49A5-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n5:271B49A4-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n5:271B49A6-363D-11E5-9242-09173F13E4C5
n3:absorption
The absolute bioavailability of icatibant following a 30 mg subcutaneous dose is approximately 97%. Maximum plasma concentrations (Cmax) of 974 ± 280 ng/mL was reached when a single subcutaneous dose of 30 mg was administered. The AUC was 2165 ± 568 ng∙hr/mL. Icatibant did not accumulate following multiple doses.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
130308-48-4
n3:category
n3:clearance
Plasma clearance following subcutaneous administration was 245 ± 58 mL/min.
n3:Bioavailability
n5:271B49AD-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n5:271B49AF-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n5:271B49B0-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n5:271B49AC-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n5:271B49AB-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n5:271B49AE-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n5:271B499C-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n5:271B49A9-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n5:271B49AA-363D-11E5-9242-09173F13E4C5