About: Canagliflozin     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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rdf:type
http://linked.open...gbank/description
  • Canagliflozin belongs to a new class of anti-diabetic drugs that works by inhibiting the sodium-glucose transport protein (SGLT2). This transport protein is found in the kidney and is responsible for reabsorbing glucose that has been filtered. FDA approved on March 29, 2013. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...generalReferences
  • # Lamos EM, Younk LM, Davis SN: Canagliflozin , an inhibitor of sodium-glucose cotransporter 2, for the treatment of type 2 diabetes mellitus. Expert Opin Drug Metab Toxicol. 2013 Jun;9(6):763-75. doi: 10.1517/17425255.2013.791282. Epub 2013 Apr 17. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23590413 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
http://linked.open...drugbank/halfLife
  • The apparent terminal half-life (t1/2) was 10.6 hours and 13.1 hours for the 100 mg and 300 mg doses, respectively. (en)
http://linked.open...ugbank/indication
  • Canagliflozin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Use in type 1 diabetes mellitus patients or in treatment of diabetic ketoacidosis is not recommended. (en)
sameAs
Title
  • Canagliflozin (en)
adms:identifier
http://linked.open...mechanismOfAction
  • Sodium-glucose co-transporter 2 (SGLT2), expressed in the proximal renal tubules, is responsible for the majority of the reabsorption of filtered glucose from the tubular lumen. Canagliflozin is an inhibitor of SGLT2. By inhibiting SGLT2, canagliflozin reduces reabsorption of filtered glucose and lowers the renal threshold for glucose (RTG), and thereby increases urinary glucose excretion. (en)
http://linked.open...y/drugbank/patent
http://linked.open...outeOfElimination
  • Enterohepatic circulation of canagliflozin was negligible. When a single oral dose is administered to a healthy subject, canagliflozin is eliminated via the following: Feces (41.5%, 7.0%, 3.2% as canagliflozin, a hydroxylated metabolite, and an O-glucuronide metabolite, respectively). Urine (33%; 30.5% as O-glucuronide metabolite, <1% as unchanged drug). (en)
http://linked.open.../drugbank/synonym
  • Canagliflozin hydrate (en)
  • 1-(Glucopyranosyl)-4-methyl-3-(5-(4-fluorophenyl)-2-thienylmethyl)benzene (en)
http://linked.open...drugbank/toxicity
  • Most common adverse reactions associated with canagliflozin (5% or greater incidence): female genital mycotic infections, urinary tract infection, and increased urination. (en)
http://linked.open...umeOfDistribution
  • Steady state, single IV infusion, healthy subject = 119 L. This high value suggests that cangliflozin is extensively distributed to tissue. (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open...nk/proteinBinding
  • >99% protein bound, mainly to albumin. It also binds to alpha-acid glycoprotein. Protein binding is independent of canagliflozin plasma concentrations. Plasma protein binding is not meaningfully altered in patients with renal or hepatic impairment. (en)
foaf:page
http://linked.open...ugbank/IUPAC-Name
http://linked.open...gy/drugbank/InChI
http://linked.open...Molecular-Formula
http://linked.open.../Molecular-Weight
http://linked.open...noisotopic-Weight
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http://linked.open...bank/Refractivity
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http://linked.open...ugbank/absorption
  • The pharmacokinetics of canagliflozin is similar in healthy subjects and patients with type 2 diabetes. Plasma Cmax and AUC of canagliflozin increased in a dose-proportional manner from 50 mg to 300 mg. Accumulation in plasma has been observed following multiple doses of 100 - 300 mg. Food does not affect the absorption of canagliflozin. Tmax = 1- 2 hours; Cmax = 1059 - 3148 ng/mL; Time to steady state, once daily dose, 100 - 300 mg = 4-5 days; Absolute oral bioavailability = 65%. (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 842133-18-0 (en)
http://linked.open...drugbank/category
  • (en)
http://linked.open...rugbank/clearance
  • Mean systemic clearance, healthy subjects, IV administration = 192 mL/min. Renal clearance of canagliflozin 100 mg and 300 mg doses ranged from 1.30 to 1.55 mL/min. (en)
http://linked.open...k/Bioavailability
http://linked.open...bank/Ghose-Filter
http://linked.open...nk/MDDR-Like-Rule
http://linked.open...k/Number-of-Rings
http://linked.open...siological-Charge
http://linked.open...bank/Rule-of-Five
http://linked.open...tional-IUPAC-Name
http://linked.open...strongest-acidic-
http://linked.open...-strongest-basic-
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