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Namespace Prefixes

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n14http://linked.opendata.cz/resource/drugbank/drug/DB05039/identifier/chebi/
n11http://linked.opendata.cz/ontology/sukl/drug/

Statements

Subject Item
n2:DB05039
rdf:type
n3:Drug
n3:description
Indacaterol is a novel, ultra-long-acting, rapid onset β(2)-adrenoceptor agonist developed for Novartis for the once-daily management of asthma and chronic obstructive pulmonary disease. It was approved by the European Medicines Agency (EMA) under the trade name Onbrez on November 30, 2009, and by the United States Food and Drug Administration (FDA), under the trade name Arcapta Neohaler, on July 1, 2011. Indacaterol is provided as its maleate salt form. Indacaterol is also a chiral molecule but only the pure R-enantiomer is dispensed.
n3:dosage
n5:271B62F4-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Naline E, Trifilieff A, Fairhurst RA, Advenier C, Molimard M: Effect of indacaterol, a novel long-acting beta2-agonist, on isolated human bronchi. Eur Respir J. 2007 Mar;29(3):575-81. Epub 2006 Nov 29. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17135231 # "Australian Public Assessment Report":http://www.tga.gov.au/pdf/auspar/auspar-onbrez.pdf # Kagan M, Dain J, Peng L, Reynolds C: Metabolism and pharmacokinetics of indacaterol in humans. Drug Metab Dispos. 2012 Sep;40(9):1712-22. doi: 10.1124/dmd.112.046151. Epub 2012 May 30. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/22648561 # Reid DJ, Pham NT: Emerging Therapeutic Options for the Management of COPD. Clin Med Insights Circ Respir Pulm Med. 2013 Apr 9;7:7-15. doi: 10.4137/CCRPM.S8140. Print 2013. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23641160
n3:group
approved
n3:halfLife
Indacaterol serum concentrations declined in a multi-phasic manner with an average terminal half-life ranging from 45.5 to 126 hours. The effective half-life, calculated from the accumulation of indacaterol after repeated dosing with once daily doses between 75 mcg and 600 mcg ranged from 40 to 56 hours which is consistent with the observed time-to-steady state of approximately 12-15 days.
n3:indication
For the long term, once-daily-dosing maintenance of airflow obstruction in patients with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and/or emphysema.
owl:sameAs
n21:DB05039 n22:DB05039
dcterms:title
Indacaterol
adms:identifier
n7:DB05039 n8:D09318 n14:68575 n15:0078-0619-15 n18:PA165958348 n19:Indacaterol
n3:mechanismOfAction
Indacaterol works by stimulating adrenergic beta-2 receptors in the smooth muscle of the airways. This causes relaxation of the muscle, thereby increasing the diameter of the airways, which become constricted in asthma and COPD. It is also long acting due to its high affinity to the lipid raft domains in the airway membrane so it slowly dissociates from the receptors. Indacaterol also has a high intrinsic efficacy so it is also very rapid acting - onset of action occurs within 5 minutes. The pharmacological effects of beta2-adrenoceptor agonist drugs, including indacaterol, are at least in part attributable to stimulation of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3’, 5’-adenosine monophosphate (cyclic monophosphate). Increased cyclic AMP levels cause relaxation of bronchial smooth muscle. In vitro studies have shown that indacaterol has more than 24-fold greater agonist activity at beta2-receptors compared to beta1-receptors and 20-fold greater agonist activity compared to beta3-receptors. This selectivity profile is similar to formoterol. The clinical significance of these findings is unknown.
n3:patent
n17:8067437 n17:6878721
n3:routeOfElimination
Renal clearance plays a minor role (about 2 to 6% of systemic clearance) in the elimination of systemically available indacaterol. In a human ADME study where indacaterol was given orally, the fecal route of excretion was dominant over the urinary route. Indacaterol was excreted into human feces primarily as unchanged parent drug (54% of the dose) and, to a lesser extent, hydroxylated indacaterol metabolites (23% of the dose).
n3:synonym
QAB 149 QAB-149 QAB149 5-(2-(5,6-Diethylindan-2-ylamino)-1-hydroxyethyl)-8-hydroxy-1H-quinolin-2-one
n3:toxicity
The expected signs and symptoms associated with overdosage of indacaterol are those of excessive beta-adrenergic stimulation and occurrence or exaggeration of any of the signs and symptoms, e.g., angina, hypertension or hypotension, tachycardia, with rates up to 200 bpm, arrhythmias, nervousness, headache, tremor, dry mouth, palpitation, muscle cramps, nausea, dizziness, fatigue, malaise, hypokalemia, hyperglycemia, metabolic acidosis and insomnia. As with all inhaled sympathomimetic medications, cardiac arrest and even death may be associated with an overdose of indacaterol.
n3:volumeOfDistribution
After intravenous infusion the volume of distribution (Vz) of indacaterol was 2,361 L to 2,557 L indicating an extensive distribution.
n11:hasAHFSCode
n12:12-12-08-12
n3:proteinBinding
The in vitro human serum and plasma protein binding was 94.1-95.3% and 95.1-96.2%, respectively.
n3:salt
foaf:page
n10:arcapta-neohaler-drug.htm n16:indacaterol.html
n3:IUPAC-Name
n4:271B62F9-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B62FF-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B62FE-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B62FB-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B62FC-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B62FD-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B62F7-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B62F8-363D-11E5-9242-09173F13E4C5 n4:271B62F5-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B62F6-363D-11E5-9242-09173F13E4C5
n11:hasATCCode
n13:R03AC18
n3:H-Bond-Acceptor-Count
n4:271B6305-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B6306-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B6300-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B6301-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B6303-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B6302-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B6304-363D-11E5-9242-09173F13E4C5
n3:absorption
The median time to reach peak serum concentrations of indacaterol was approximately 15 minutes after single or repeated inhaled doses. Absolute bioavailability of indacaterol after an inhaled dose was on average 43-45%.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
312753-06-3
n3:clearance
Renal clearance of indacaterol is, on average, between 0.46 and 1.2 L/h. Serum clearance of indacaterol is 18.8 L/h to 23.3 L/h.
n3:Bioavailability
n4:271B630B-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B630D-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B630E-363D-11E5-9242-09173F13E4C5
n3:Melting-Point
n4:271B630F-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B630A-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B6309-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B630C-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B62FA-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n4:271B6307-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B6308-363D-11E5-9242-09173F13E4C5