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SITAGLIPTIN Drug Record

  • Summary
  • Interactions
  • Claims
  • SITAGLIPTIN chembl:CHEMBL1422 Approved

    Alternate Names:

    MK-0431
    JANUVIA
    LEZ763
    SITAGLIPTIN
    LEZ-763
    SITAGLIPTINUM
    SITAGLIPTINA
    SITAGLIPTAN
    SITAGLIPTINE
    SITAGLIPTIN PHOSPHATE
    JANUVIA®
    (2R)-4-OXO-4-[3-(TRIFLUOROMETHYL)-5,6-DIHYDRO[1,2,4]TRIAZOLO[4,3-A]PYRAZIN-7(8H)-YL]-1-(2,4,5-TRIFLUOROPHENYL)BUTAN-2-AMINE
    drugbank:01261
    rxcui:593411
    chemidplus:486460-32-6
    pubchem.compound:4369359
    chembl:CHEMBL1422

    Drug Info:

    Drug Class hypoglycemic agents
    Year of Approval 2006
    FDA Approval not approved
    Drug Class Small Molecule
    Drug Indications antidiabetic
    Drug Categories pyrazines
    Drug Categories agents causing angioedema
    Drug Categories cytochrome p-450 cyp3a substrates
    Drug Categories cytochrome p-450 substrates
    Drug Categories drugs that are mainly renally excreted
    Drug Categories hypoglycemia-associated agents
    Drug Categories oat3/slc22a8 substrates
    Drug Categories p-glycoprotein substrates
    (4 More Sources)

    Publications:

    Javorský M et al., 2016, A missense variant in GLP1R gene is associated with the glycaemic response to treatment with gliptins., Diabetes Obes Metab
    Bergman et al., 2006, Pharmacokinetic and pharmacodynamic properties of multiple oral doses of sitagliptin, a dipeptidyl peptidase-IV inhibitor: a double-blind, randomized, placebo-controlled study in healthy male volunteers., Clin Ther
    Gallwitz, 2007, Sitagliptin: Profile of a novel DPP-4 inhibitor for the treatment of type 2 diabetes., Drugs Today
    Pratley et al., 2007, Inhibition of DPP-4: a new therapeutic approach for the treatment of type 2 diabetes., Curr Med Res Opin
    Lyseng-Williamson, 2007, Sitagliptin., Drugs
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Richter et al., 2008, Emerging role of dipeptidyl peptidase-4 inhibitors in the management of type 2 diabetes., Vasc Health Risk Manag
    Herman et al., 2005, Pharmacokinetics and pharmacodynamics of sitagliptin, an inhibitor of dipeptidyl peptidase IV, in healthy subjects: results from two randomized, double-blind, placebo-controlled studies with single oral doses., Clin. Pharmacol. Ther.
    Karasik et al., 2008, Sitagliptin, a DPP-4 inhibitor for the treatment of patients with type 2 diabetes: a review of recent clinical trials., Curr Med Res Opin
    Miller et al., Sitagliptin: a dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes., Ann Pharmacother
    Herman et al., 2006, Pharmacokinetics and pharmacodynamic effects of the oral DPP-4 inhibitor sitagliptin in middle-aged obese subjects., J Clin Pharmacol
    Gallwitz, 2006, Therapies for the treatment of type 2 diabetes mellitus based on incretin action., Minerva Endocrinol.
    Hermansen et al., 2007, Efficacy and safety of the dipeptidyl peptidase-4 inhibitor, sitagliptin, in patients with type 2 diabetes mellitus inadequately controlled on glimepiride alone or on glimepiride and metformin., Diabetes Obes Metab
  • SITAGLIPTIN   DPP4

    Interaction Score: 5.55

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name Sitagliptin
    Novel drug target Established target
    Specific Action of the Ligand Inhibition

    PMIDs:
    16490580 17315049 17407649 17352516 11752352 19065993 16338283 18182122 16868220 16855072 16682937 17593236


    Sources:
    DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD

  • SITAGLIPTIN   GPR119

    Interaction Score: 2.71

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • SITAGLIPTIN   GLP1R

    Interaction Score: 0.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27160388


    Sources:
    PharmGKB

  • DrugBank: DB01261

    • Version: 5.1.7

    Alternate Names:
    SITAGLIPTIN DrugBank Drug Name
    486460-32-6 CAS Number
    Janumet Drug Brand

    Drug Info:
    Drug Type small molecule
    Drug Groups approved
    Drug Groups investigational

    Publications:
    Richter et al., 2008, Emerging role of dipeptidyl peptidase-4 inhibitors in the management of type 2 diabetes., Vasc Health Risk Manag
    Herman et al., 2005, Pharmacokinetics and pharmacodynamics of sitagliptin, an inhibitor of dipeptidyl peptidase IV, in healthy subjects: results from two randomized, double-blind, placebo-controlled studies with single oral doses., Clin. Pharmacol. Ther.
    Gallwitz, 2006, Therapies for the treatment of type 2 diabetes mellitus based on incretin action., Minerva Endocrinol.

  • TEND: SITAGLIPTIN

    • Version: 01-August-2011

    Alternate Names:
    SITAGLIPTIN Primary Drug Name

    Drug Info:
    Year of Approval 2006
    Drug Class hypoglycemic agents

    Publications:

  • TdgClinicalTrial: SITAGLIPTIN

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications antidiabetic
    Drug Class Small Molecule
    FDA Approval not approved

    Publications:

  • PharmGKB: sitagliptin

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Javorský M et al., 2016, A missense variant in GLP1R gene is associated with the glycaemic response to treatment with gliptins., Diabetes Obes Metab

  • TTD: LEZ763

    • Version: 2020.06.01

    Alternate Names:
    D05RTM TTD Drug ID

    Drug Info:

    Publications:

  • GuideToPharmacology: 178102906

    • Version: 29-September-2020

    Alternate Names:
    SITAGLIPTIN GuideToPharmacology Ligand Name

    Drug Info:

    Publications:

  • TTD: Sitagliptin

    • Version: 2020.06.01

    Alternate Names:
    D0U2JP TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL1422

    • Version: ChEMBL_27

    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.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21