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Namespace Prefixes

PrefixIRI
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Statements

Subject Item
n2:DB06292
rdf:type
n3:Drug
n3:description
Dapagliflozin is indicated for the management of diabetes mellitus type 2, and functions to improve glycemic control in adults when combined with diet and exercise. Dapagliflozin is a sodium-glucose cotransporter 2 inhibitor, which prevents glucose reabsorption in the kidney. Using dapagliflozin leads to heavy glycosuria (glucose excretion in the urine), which can lead to weight loss and tiredness. Dapagliflozin was approved by the FDA on Jan 08, 2014. Dapagliflozin is not recommended for patients with type 1 diabetes mellitus or for the treatment of diabetic ketoacidosis.
n3:dosage
n5:271B4C21-363D-11E5-9242-09173F13E4C5 n5:271B4C22-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Obermeier M, Yao M, Khanna A, Koplowitz B, Zhu M, Li W, Komoroski B, Kasichayanula S, Discenza L, Washburn W, Meng W, Ellsworth BA, Whaley JM, Humphreys WG: In vitro characterization and pharmacokinetics of dapagliflozin (BMS-512148), a potent sodium-glucose cotransporter type II inhibitor, in animals and humans. Drug Metab Dispos. 2010 Mar;38(3):405-14. doi: 10.1124/dmd.109.029165. Epub 2009 Dec 8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/19996149 # Kasichayanula S, Liu X, Lacreta F, Griffen SC, Boulton DW: Clinical Pharmacokinetics and Pharmacodynamics of Dapagliflozin, a Selective Inhibitor of Sodium-Glucose Co-transporter Type 2. Clin Pharmacokinet. 2014 Jan;53(1):17-27. doi: 10.1007/s40262-013-0104-3. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/24105299 # Kasichayanula S, Chang M, Hasegawa M, Liu X, Yamahira N, LaCreta FP, Imai Y, Boulton DW: Pharmacokinetics and pharmacodynamics of dapagliflozin, a novel selective inhibitor of sodium-glucose co-transporter type 2, in Japanese subjects without and with type 2 diabetes mellitus. Diabetes Obes Metab. 2011 Apr;13(4):357-65. doi: 10.1111/j.1463-1326.2011.01359.x. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/21226818
n3:group
approved
n3:halfLife
13.8 hours with the consumption of a 50 mg dose.
n3:indication
Dapagliflozin is indicated for adjunct management of glycemic control in patients with type 2 diabetes mellitus, in combination with diet and exercise.
owl:sameAs
n11:DB06292
dcterms:title
Dapagliflozin
adms:identifier
n13:0003-1427-11 n14:Dapagliflozin n15:DB06292 n16:D09763
n3:mechanismOfAction
A competitive inhibitor of the sodium-glucose transport subtype 2 protein, dapagliflozin blocks glucose reabsorption into the kidney, resulting in the elimination of blood glucose through the urine.
n3:synonym
(2S,3R,4R,5S,6R)-2-[4-chloro-3-(4-ethoxybenzyl)phenyl]-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol
n3:toxicity
Compared to placebo-treated patients, patients with moderate renal impairment treated with dapagliflozin did not have improvement in glycemic control and had more renal-related adverse reactions and more bone fractures; therefore, dapagliflozin should not be initiated in this population. Based on its mechanism of action, dapagliflozin is not expected to be effective in patients with severe renal impairment (eGFR less than 30 mL/min/1.73 m2) or ESRD.
n3:mixture
n6:271B4C20-363D-11E5-9242-09173F13E4C5
n3:proteinBinding
91%.
n3:salt
foaf:page
n18:farxiga.html
n3:IUPAC-Name
n4:271B4C27-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B4C2D-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B4C2C-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B4C29-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B4C2A-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B4C2B-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B4C25-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B4C23-363D-11E5-9242-09173F13E4C5 n4:271B4C26-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B4C24-363D-11E5-9242-09173F13E4C5
n7:hasATCCode
n8:A10BX09
n3:H-Bond-Acceptor-Count
n4:271B4C33-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B4C34-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B4C2E-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B4C2F-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B4C31-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B4C30-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B4C32-363D-11E5-9242-09173F13E4C5
n3:absorption
Cmax is about 1 hour. (Obtained from 6 adult men in a fasted state administered a 50mg dose). 1.6% of unchanged dapagliflozin was found in the urine. A high-fat meal (52% caloric content) had no significant effect on previous pharmacokinetic parameters.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
461432-26-8
n3:category
n3:clearance
Oral plasma clearance of 4.9 mL/min/kg, and a renal clearance of 5.6 mL/min.
n3:Bioavailability
n4:271B4C39-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B4C3B-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B4C3C-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B4C38-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B4C37-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B4C3A-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B4C28-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n4:271B4C35-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B4C36-363D-11E5-9242-09173F13E4C5