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GLYBURIDE Drug Record

  • Summary
  • Interactions
  • Claims
  • GLYBURIDE chembl:CHEMBL472 Approved

    Alternate Names:

    DIABETAMIDE 5
    MALIX
    GLYNASE
    CALABREN
    GLIBENCLAMIDE
    HB 419
    U-26452
    U-26,45
    GLYNASE PRESTAB
    MICRONASE
    DIABETA
    LIBANIL
    DAONIL
    DIABETAMIDE 2.5
    GLYBURIDE
    LEDERGLIB
    HB-419
    EUGLUCON
    SEMI-DAONIL
    GLYBURIDE (MICRONIZED)
    GLIKEN
    DIABETA®
    GLIBENCLAMIDUM
    1-(P-(2-(5-CHLORO-2-METHOXYBENZAMIDO)ETHYL)BENZENESULFONYL)-3-CYCLOHEXYLUREA
    5-CHLORO-N-(2-(4-((((CYCLOHEXYLAMINO)CARBONYL)AMINO)SULFONYL)PHENYL)ETHYL)-2-METHOXYBENZAMIDE
    1-((P-(2-(5-CHLORO-O-ANISAMIDO)ETHYL)PHENYL)SULFONYL)-3-CYCLOHEXYLUREA
    GLIBENCLAMIDA
    GLYNASE®
    chembl:CHEMBL472
    chemidplus:10238-21-8
    drugbank:01016
    pubchem.compound:3488
    rxcui:4815

    Drug Info:

    Drug Class hypoglycemic agents
    Year of Approval 1984
    Drug Categories hypoglycemia-associated agents
    FDA Approval 1984
    Drug Class small molecule
    Drug Indications Hypoglycemic Agents
    FDA Approval approved
    Drug Indications antidiabetic
    Drug Categories bsep/abcb11 substrates
    Drug Categories cytochrome p-450 cyp2c9 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 cyp3a substrates
    Drug Categories cytochrome p-450 cyp3a4 inhibitors
    Drug Categories cytochrome p-450 cyp3a4 inhibitors (weak)
    Drug Categories cytochrome p-450 cyp3a5 substrates
    Drug Categories cytochrome p-450 cyp3a7 substrates
    Drug Categories cytochrome p-450 enzyme inhibitors
    Drug Categories cytochrome p-450 substrates
    Drug Categories drugs causing inadvertant photosensitivity
    Drug Categories oat1/slc22a6 inhibitors
    Drug Categories p-glycoprotein inhibitors
    Drug Categories photosensitizing agents
    (8 More Sources)

    Publications:

    Cook, 1987, The hypoglycemic sulfonylureas glyburide and tolbutamide inhibit fatty acid oxidation by inhibiting carnitine palmitoyltransferase., J. Biol. Chem.
    Patel, 1986, Effect of sulfonylureas on hepatic fatty acid oxidation., Am. J. Physiol.
    Klen J et al., 2014, CYP2C9, KCNJ11 and ABCC8 polymorphisms and the response to sulphonylurea treatment in type 2 diabetes patients., Eur J Clin Pharmacol
    Sesti G et al., 2006, The E23K variant of KCNJ11 encoding the pancreatic beta-cell adenosine 5'-triphosphate-sensitive potassium channel subunit Kir6.2 is associated with an increased risk of secondary failure to sulfonylurea in patients with type 2 diabetes., J Clin Endocrinol Metab
    Gloyn AL et al., 2001, Association studies of variants in promoter and coding regions of beta-cell ATP-sensitive K-channel genes SUR1 and Kir6.2 with Type 2 diabetes mellitus (UKPDS 53)., Diabet Med
    Jabůrek et al., 1998, State-dependent inhibition of the mitochondrial KATP channel by glyburide and 5-hydroxydecanoate., J. Biol. Chem.
    Javorsky M et al., 2012, KCNJ11 gene E23K variant and therapeutic response to sulfonylureas., Eur J Intern Med
    Li Q et al., 2014, KCNJ11 E23K variant is associated with the therapeutic effect of sulphonylureas in Chinese type 2 diabetic patients., Clin Exp Pharmacol Physiol
    Babenko et al., 2002, SUR-dependent modulation of KATP channels by an N-terminal KIR6.2 peptide. Defining intersubunit gating interactions., J. Biol. Chem.
    Serrano-Martín et al., 2006, Glibenclamide, a blocker of K+(ATP) channels, shows antileishmanial activity in experimental murine cutaneous leishmaniasis., Antimicrob. Agents Chemother.
    Nielsen et al., 2002, 6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide derivatives potently and selectively activate ATP sensitive potassium channels of pancreatic beta-cells., J. Med. Chem.
    Dabrowski et al., 2002, The novel diazoxide analog 3-isopropylamino-7-methoxy-4H-1,2,4-benzothiadiazine 1,1-dioxide is a selective Kir6.2/SUR1 channel opener., Diabetes
    Ueda et al., 1999, Cooperative binding of ATP and MgADP in the sulfonylurea receptor is modulated by glibenclamide., Proc. Natl. Acad. Sci. U.S.A.
    Hambrock et al., 2002, Four novel splice variants of sulfonylurea receptor 1., Am. J. Physiol., Cell Physiol.
    Hambrock et al., 2002, Glibenclamide binding to sulphonylurea receptor subtypes: dependence on adenine nucleotides., Br. J. Pharmacol.
    Rainbow et al., 2004, Proximal C-terminal domain of sulphonylurea receptor 2A interacts with pore-forming Kir6 subunits in KATP channels., Biochem. J.
    Wang et al., 2007, Involvement of ATP-sensitive potassium channels in proliferation and differentiation of rat preadipocytes., Sheng Li Xue Bao
    Zhao et al., 2006, Pretreatment with fosinopril or valsartan reduces myocardial no-reflow after acute myocardial infarction and reperfusion., Coron. Artery Dis.
    Felsch et al., 2004, Interaction of a novel dihydropyridine K+ channel opener, A-312110, with recombinant sulphonylurea receptors and KATP channels: comparison with the cyanoguanidine P1075., Br. J. Pharmacol.
    Zhang YF et al., 2005, [Impact of cytochrome P450 CYP2C9 variant allele CYP2C9 * 3 on the pharmacokinetics of glibenclamide and lornoxicam in Chinese subjects]., Yao Xue Xue Bao
    Kemp et al., 2004, Viability assessment in sandwich-cultured rat hepatocytes after xenobiotic exposure., Toxicol In Vitro
    Horikawa et al., 2003, Potential cholestatic activity of various therapeutic agents assessed by bile canalicular membrane vesicles isolated from rats and humans., Drug Metab. Pharmacokinet.
    Byrne et al., 2002, The human bile salt export pump: characterization of substrate specificity and identification of inhibitors., Gastroenterology
    Abu-Hamdah et al., 2004, Regulation of the water channel aquaporin-1: isolation and reconstitution of the regulatory complex., Cell Biol. Int.
    Sireci et al., 1999, Effects of glyburide-cyclosporin A interaction on interleukin-2 production in rats., Immunopharmacol Immunotoxicol
    Carette C et al., 2011, Diabetes mellitus and glucose-6-phosphate dehydrogenase deficiency: from one crisis to another., Diabetes Metab
    Youngster I et al., 2010, Medications and glucose-6-phosphate dehydrogenase deficiency: an evidence-based review., Drug Saf
    Vinzio S et al., 2004, Glibenclamide-induced acute haemolytic anaemia revealing a G6PD-deficiency., Diabetes Res Clin Pract
    Meloni G et al., 1996, Glyburide-induced acute haemolysis in a G6PD-deficient patient with NIDDM., Br J Haematol
    Kharbanda C et al., 2015, Antidiabetic effect of novel benzenesulfonylureas as PPAR-γ agonists and their anticancer effect., Bioorg Med Chem Lett
    Spraggs C et al., 2007, Genetic variants in the epithelial sodium channel associate with oedema in type 2 diabetic patients receiving the peroxisome proliferator-activated receptor gamma agonist farglitazar., Pharmacogenet Genomics
    Mühl et al., 2003, Inhibition of lipopolysaccharide/ATP-induced release of interleukin-18 by KN-62 and glyburide., Eur. J. Pharmacol.
    Nieland et al., 2004, Cross-inhibition of SR-BI- and ABCA1-mediated cholesterol transport by the small molecules BLT-4 and glyburide., J. Lipid Res.
    Lamkanfi et al., 2009, Glyburide inhibits the Cryopyrin/Nalp3 inflammasome., J. Cell Biol.
    Reddy et al., 2002, ATP-binding cassette transporter 1 participates in LDL oxidation by artery wall cells., Arterioscler. Thromb. Vasc. Biol.
    Alder-Baerens et al., 2005, Headgroup-specific exposure of phospholipids in ABCA1-expressing cells., J. Biol. Chem.
    Agassandian et al., 2004, Oxysterols trigger ABCA1-mediated basolateral surfactant efflux., Am. J. Respir. Cell Mol. Biol.
    Ren Q et al., 2016, Genetic and Clinical Predictive Factors of Sulfonylurea Failure in Patients with Type 2 Diabetes., Diabetes Technol Ther
    Kern et al., 1993, Increased muscle glucose uptake in response to chronic glyburide treatment is not related to changes in glucose transporter (GLUT4) protein., Int. J. Biochem.
    Zhou et al., 2002, Probing an open CFTR pore with organic anion blockers., J. Gen. Physiol.
    Reddy et al., 2002, Effect of anion transport blockers on CFTR in the human sweat duct., J. Membr. Biol.
    Jiang et al., 2003, Pleural surface fluorescence measurement of Na+ and Cl- transport across the air space-capillary barrier., J. Appl. Physiol.
    Larsen et al., 2003, Beta-adrenergic receptors couple to CFTR chloride channels of intercalated mitochondria-rich cells in the heterocellular toad skin epithelium., Biochim. Biophys. Acta
    Lee et al., 2005, Inhibition of Na+-K+ pump and L-type Ca2+ channel by glibenclamide in Guinea pig ventricular myocytes., J. Pharmacol. Exp. Ther.
    King ZA et al., 2018, Profile of intravenous glyburide for the prevention of cerebral edema following large hemispheric infarction: evidence to date., Drug Des Devel Ther
  • GLYBURIDE   CPT1A

    Interaction Score: 2.47

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    3104327 3090894


    Sources:
    DrugBank

  • GLYBURIDE   ABCA1

    Interaction Score: 2.16

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    14660039 15102890 19805629 12426219 15905177 15039140


    Sources:
    DrugBank

  • GLYBURIDE   ABCC8

    Interaction Score: 1.43

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name glyburide + metformin,Glucovance
    Mechanism of Interaction Sulfonylurea receptor 1, Kir6.2 blocker

    PMIDs:
    12213829 17015627 12213059 12031979 9990013 12107069 12145099


    Sources:
    TdgClinicalTrial TTD DrugBank ChemblInteractions

  • GLYBURIDE   ABCC9

    Interaction Score: 1.35

    Interaction Types & Directionality:
    modulator

    Interaction Info:

    PMIDs:
    14672537 17294036 16845255 12145099 15023854


    Sources:
    DrugBank

  • GLYBURIDE   AQP1

    Interaction Score: 0.99

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    14759764


    Sources:
    NCI

  • GLYBURIDE   ABCB11

    Interaction Score: 0.99

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    15465654 15618715 12404239


    Sources:
    DrugBank

  • GLYBURIDE   KCNJ11

    Interaction Score: 0.93

    Interaction Types & Directionality:
    blocker (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction? True
    Endogenous Drug? False
    Specific Action of the Ligand None

    PMIDs:
    24442125 16595597 11318841 9593694 22385882 25115353


    Sources:
    TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

  • GLYBURIDE   TRPM4

    Interaction Score: 0.82

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    30147301


    Sources:
    DrugBank

  • GLYBURIDE   SCNN1B

    Interaction Score: 0.82

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18004211


    Sources:
    PharmGKB

  • GLYBURIDE   CFTR

    Interaction Score: 0.58

    Interaction Types & Directionality:
    antagonist (inhibitory)
    blocker (inhibitory)

    Interaction Info:
    Specific Action of the Ligand None
    Endogenous Drug? False

    PMIDs:
    12407077 12202948 12391048 14729151 15365090


    Sources:
    DrugBank GuideToPharmacology

  • GLYBURIDE   ABCC5

    Interaction Score: 0.55

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27403931


    Sources:
    PharmGKB

  • GLYBURIDE   KCNJ1

    Interaction Score: 0.27

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TEND TdgClinicalTrial

  • GLYBURIDE   KCNJ8

    Interaction Score: 0.21

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand None
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • GLYBURIDE   G6PD

    Interaction Score: 0.2

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21147013 20701405 15126005 8562390


    Sources:
    FDA PharmGKB

  • GLYBURIDE   IL2

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10466081


    Sources:
    NCI

  • GLYBURIDE   SLC2A4

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    8224371


    Sources:
    NCI

  • GLYBURIDE   SLCO2B1

    Interaction Score: 0.1

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • GLYBURIDE   PPARG

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26384286


    Sources:
    DTC

  • GLYBURIDE   CYP2C9

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24442125 16342679


    Sources:
    DTC PharmGKB

  • GLYBURIDE   NR1I2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • GLYBURIDE   CYP2C19

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • GLYBURIDE   CYP2D6

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • GLYBURIDE   CYP3A4

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DrugBank: DB01016

    • Version: 5.1.7

    Alternate Names:
    GLYBURIDE DrugBank Drug Name
    10238-21-8 CAS Number
    Apo Glyburide Tab 2.5mg Drug Brand

    Drug Info:
    Drug Type small molecule
    Drug Groups approved
    Drug Categories alimentary tract and metabolism

    Publications:
    King ZA et al., 2018, Profile of intravenous glyburide for the prevention of cerebral edema following large hemispheric infarction: evidence to date., Drug Des Devel Ther
    Zhou et al., 2002, Probing an open CFTR pore with organic anion blockers., J. Gen. Physiol.
    Reddy et al., 2002, Effect of anion transport blockers on CFTR in the human sweat duct., J. Membr. Biol.

  • TEND: GLIBENCLAMIDE

    • Version: 01-August-2011

    Alternate Names:
    GLIBENCLAMIDE Primary Drug Name

    Drug Info:
    Year of Approval 1984
    Drug Class hypoglycemic agents

    Publications:

  • TdgClinicalTrial: GLIBENCLAMIDE

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications Hypoglycemic Agents
    Drug Class small molecule
    FDA Approval 1984

    Publications:

  • TdgClinicalTrial: GLYBURIDE

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications antidiabetic
    Drug Class Small molecule
    FDA Approval approved

    Publications:

  • NCI: GLYBURIDE

    • Version: 14-September-2017

    Alternate Names:
    C29076 NCI drug code

    Drug Info:

    Publications:
    Abu-Hamdah et al., 2004, Regulation of the water channel aquaporin-1: isolation and reconstitution of the regulatory complex., Cell Biol. Int.
    Sireci et al., 1999, Effects of glyburide-cyclosporin A interaction on interleukin-2 production in rats., Immunopharmacol Immunotoxicol
    Kern et al., 1993, Increased muscle glucose uptake in response to chronic glyburide treatment is not related to changes in glucose transporter (GLUT4) protein., Int. J. Biochem.

  • DTC: GLYBURIDE

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL472 ChEMBL Drug ID

    Drug Info:

    Publications:
    Kharbanda C et al., 2015, Antidiabetic effect of novel benzenesulfonylureas as PPAR-γ agonists and their anticancer effect., Bioorg Med Chem Lett

  • PharmGKB: glibenclamide

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Klen J et al., 2014, CYP2C9, KCNJ11 and ABCC8 polymorphisms and the response to sulphonylurea treatment in type 2 diabetes patients., Eur J Clin Pharmacol
    Sesti G et al., 2006, The E23K variant of KCNJ11 encoding the pancreatic beta-cell adenosine 5'-triphosphate-sensitive potassium channel subunit Kir6.2 is associated with an increased risk of secondary failure to sulfonylurea in patients with type 2 diabetes., J Clin Endocrinol Metab
    Gloyn AL et al., 2001, Association studies of variants in promoter and coding regions of beta-cell ATP-sensitive K-channel genes SUR1 and Kir6.2 with Type 2 diabetes mellitus (UKPDS 53)., Diabet Med

  • TTD: Glibenclamide

    • Version: 2020.06.01

    Alternate Names:
    D05LYX TTD Drug ID

    Drug Info:

    Publications:

  • GuideToPharmacology: 135650306

    • Version: 29-September-2020

    Alternate Names:
    GLIBENCLAMIDE GuideToPharmacology Ligand Name

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL472

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL472

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Glyburide

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2021-04-13