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METFORMIN Drug Record

  • Summary
  • Interactions
  • Claims
  • METFORMIN chembl:CHEMBL1431 ApprovedAntineoplastic

    Alternate Names:

    METFORMIN
    LA-6023
    N1,N1-DIMETHYLBIGUANIDE
    OBIMET
    DIANBEN
    DIAFORMIN
    METFORMINA
    RIOMET
    DIMETHYLBIGUANIDE
    METFORMINUM
    DIABEFAGOS
    XLA399
    GLUCOPHAGE
    1,1-DIMETHYL BIGUANIDE
    GLUMETZA
    N,N-DIMETHYLBIGUANIDE
    DIABEX
    FORTAMET
    1,1-DIMETHYLBIGUANIDE
    GLUCOPHAGE®
    METIGUANIDE
    METFORMINE
    1-CARBAMIMIDAMIDO-N,N-DIMETHYLMETHANIMIDAMIDE
    DMBG
    DIMETHYLBIGUANID
    MEGUAN
    pubchem.compound:4091
    rxcui:6809
    chemidplus:657-24-9
    chembl:CHEMBL1431
    drugbank:00331

    Drug Info:

    Year of Approval 1995
    Drug Class hypoglycemic agents
    Drug Class Small molecule
    FDA Approval approved
    Drug Class Small Molecule
    Drug Indications antidiabetic
    (5 More Sources)

    Publications:

    Tkáč I et al., 2015, A pharmacogenetic association between a variation in calpain 10 (CAPN10) gene and the response to metformin treatment in patients with type 2 diabetes., Eur J Clin Pharmacol
    Pedersen AJT et al., 2018, The Pharmacogenetics of Metformin in Women with Polycystic Ovary Syndrome: A Randomized Trial., Basic Clin Pharmacol Toxicol
    Santoro AB et al., 2018, Influence of pharmacogenetic polymorphisms and demographic variables on metformin pharmacokinetics in an admixed Brazilian cohort., Br J Clin Pharmacol
    Goswami S et al., 2014, Genetic variants in transcription factors are associated with the pharmacokinetics and pharmacodynamics of metformin., Clin Pharmacol Ther
    Seo WD et al., 2015, Saponarin activates AMPK in a calcium-dependent manner and suppresses gluconeogenesis and increases glucose uptake via phosphorylation of CRTC2 and HDAC5., Bioorg Med Chem Lett
    Gong L et al., 2012, Metformin pathways: pharmacokinetics and pharmacodynamics., Pharmacogenet Genomics
    Vucicevic et al., 2009, AMP-activated protein kinase-dependent and -independent mechanisms underlying in vitro antiglioma action of compound C., Biochem. Pharmacol.
    Ruderman et al., 2003, Minireview: malonyl CoA, AMP-activated protein kinase, and adiposity., Endocrinology
    Kovacic et al., 2003, Akt activity negatively regulates phosphorylation of AMP-activated protein kinase in the heart., J. Biol. Chem.
    Towler et al., 2007, AMP-activated protein kinase in metabolic control and insulin signaling., Circ. Res.
    Leverve et al., 2003, Mitochondrial metabolism and type-2 diabetes: a specific target of metformin., Diabetes Metab.
    Musi et al., 2002, Metformin increases AMP-activated protein kinase activity in skeletal muscle of subjects with type 2 diabetes., Diabetes
    Hardie, 2003, Minireview: the AMP-activated protein kinase cascade: the key sensor of cellular energy status., Endocrinology
    Leclerc et al., 2004, Metformin, but not leptin, regulates AMP-activated protein kinase in pancreatic islets: impact on glucose-stimulated insulin secretion., Am. J. Physiol. Endocrinol. Metab.
    Sundelin E et al., 2017, Genetic Polymorphisms in Organic Cation Transporter 1 Attenuates Hepatic Metformin Exposure in Humans., Clin Pharmacol Ther
    Dujic T et al., 2017, Variants in Pharmacokinetic Transporters and Glycemic Response to Metformin: A Metgen Meta-Analysis., Clin Pharmacol Ther
    Chien HC et al., 2016, Rapid Method To Determine Intracellular Drug Concentrations in Cellular Uptake Assays: Application to Metformin in Organic Cation Transporter 1-Transfected Human Embryonic Kidney 293 Cells., Drug Metab Dispos
    Todd JN et al., 2014, An update on the pharmacogenomics of metformin: progress, problems and potential., Pharmacogenomics
    Tarasova L et al., 2012, Association of genetic variation in the organic cation transporters OCT1, OCT2 and multidrug and toxin extrusion 1 transporter protein genes with the gastrointestinal side effects and lower BMI in metformin-treated type 2 diabetes patients., Pharmacogenet Genomics
    Becker ML et al., 2009, Genetic variation in the organic cation transporter 1 is associated with metformin response in patients with diabetes mellitus., Pharmacogenomics J
    Shu Y et al., 2008, Effect of genetic variation in the organic cation transporter 1, OCT1, on metformin pharmacokinetics., Clin Pharmacol Ther
    Shikata E et al., 2007, Human organic cation transporter (OCT1 and OCT2) gene polymorphisms and therapeutic effects of metformin., J Hum Genet
    Christensen MM et al., 2011, The pharmacogenetics of metformin and its impact on plasma metformin steady-state levels and glycosylated hemoglobin A1c., Pharmacogenet Genomics
    Dorosz J et al., 2010, Membrane interactions of novicidin, a novel antimicrobial peptide: phosphatidylglycerol promotes bilayer insertion., J Phys Chem B
    Becker ML et al., 2010, Interaction between polymorphisms in the OCT1 and MATE1 transporter and metformin response., Pharmacogenet Genomics
    Tzvetkov MV et al., 2009, The effects of genetic polymorphisms in the organic cation transporters OCT1, OCT2, and OCT3 on the renal clearance of metformin., Clin Pharmacol Ther
    Liu et al., 2016, High Sensitivity of an Ha-RAS Transgenic Model of Superficial Bladder Cancer to Metformin Is Associated with ∼240-Fold Higher Drug Concentration in Urine than Serum., Mol. Cancer Ther.
    Iglesias et al., 2013, Another surprise from Metformin: novel mechanism of action via K-Ras influences endometrial cancer response to therapy., Mol. Cancer Ther.
    Molenaar et al., 2015, Radioprotection of IDH1-Mutated Cancer Cells by the IDH1-Mutant Inhibitor AGI-5198., Cancer Res.
    Zakikhani et al., 2006, Metformin is an AMP kinase-dependent growth inhibitor for breast cancer cells., Cancer Res.
    Dowling et al., 2007, Metformin inhibits mammalian target of rapamycin-dependent translation initiation in breast cancer cells., Cancer Res.
    Christensen MMH et al., 2015, Steady-state pharmacokinetics of metformin is independent of the OCT1 genotype in healthy volunteers., Eur J Clin Pharmacol
    Yoon H et al., 2013, Influences of organic cation transporter polymorphisms on the population pharmacokinetics of metformin in healthy subjects., AAPS J
    He R et al., 2015, SLC47A1 gene rs2289669 G>A variants enhance the glucose-lowering effect of metformin via delaying its excretion in Chinese type 2 diabetes patients., Diabetes Res Clin Pract
    Christensen MM et al., 2013, A gene-gene interaction between polymorphisms in the OCT2 and MATE1 genes influences the renal clearance of metformin., Pharmacogenet Genomics
    Stocker SL et al., 2013, The effect of novel promoter variants in MATE1 and MATE2 on the pharmacokinetics and pharmacodynamics of metformin., Clin Pharmacol Ther
    Tkáč I et al., 2013, Pharmacogenomic association between a variant in SLC47A1 gene and therapeutic response to metformin in type 2 diabetes., Diabetes Obes Metab
    Chung JY et al., 2013, Functional characterization of MATE2-K genetic variants and their effects on metformin pharmacokinetics., Pharmacogenet Genomics
    Choi JH et al., 2011, A common 5'-UTR variant in MATE2-K is associated with poor response to metformin., Clin Pharmacol Ther
    Breitenstein MK et al., 2015, Leveraging an Electronic Health Record-Linked Biorepository to Generate a Metformin Pharmacogenomics Hypothesis., AMIA Jt Summits Transl Sci Proc
    Liang X et al., 2015, Metformin Is a Substrate and Inhibitor of the Human Thiamine Transporter, THTR-2 (SLC19A3)., Mol Pharm
    Vujic et al., 2015, Metformin and trametinib have synergistic effects on cell viability and tumor growth in NRAS mutant cancer., Oncotarget
    Rotroff DM et al., 2018, Genetic Variants in <i>CPA6</i> and <i>PRPF31</i> Are Associated With Variation in Response to Metformin in Individuals With Type 2 Diabetes., Diabetes
    Chen EC et al., 2015, Targeted disruption of organic cation transporter 3 attenuates the pharmacologic response to metformin., Mol Pharmacol
    Chen L et al., 2010, Role of organic cation transporter 3 (SLC22A3) and its missense variants in the pharmacologic action of metformin., Pharmacogenet Genomics
    Ma et al., 2013, K‑ras gene mutation as a predictor of cancer cell responsiveness to metformin., Mol Med Rep
    Xie J et al., 2020, Metformin selectively inhibits metastatic colorectal cancer with the &lt;i&gt;KRAS&lt;/i&gt; mutation by intracellular accumulation through silencing MATE1., Proc Natl Acad Sci U S A
    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
    Cufí et al., 2013, Dietary restriction-resistant human tumors harboring the PIK3CA-activating mutation H1047R are sensitive to metformin., Oncotarget
    Houlleberghs et al., 2016, Oligonucleotide-directed mutagenesis screen to identify pathogenic Lynch syndrome-associated MSH2 DNA mismatch repair gene variants., Proc. Natl. Acad. Sci. U.S.A.
    Sonnenblick et al., 2017, Impact of Diabetes, Insulin, and Metformin Use on the Outcome of Patients With Human Epidermal Growth Factor Receptor 2-Positive Primary Breast Cancer: Analysis From the ALTTO Phase III Randomized Trial., J. Clin. Oncol.
  • METFORMIN   SLC47A2

    Interaction Score: 7.32

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28834135 25939711 24624919 23652408 23417334 23267855 22722338 21956618


    Sources:
    PharmGKB

  • METFORMIN   SLC47A1

    Interaction Score: 7.32

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28834135 26004431 24624919 23873119 23267855 22882994 22722338


    Sources:
    PharmGKB TTD

  • METFORMIN   AMHR2

    Interaction Score: 4.88

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    29352482 24853734


    Sources:
    PharmGKB

  • METFORMIN   PRKAB1

    Interaction Score: 4.56

    Interaction Types & Directionality:
    activator (activating)
    inducer (activating)

    Interaction Info:
    Trial Name glyburide + metformin,Glucovance
    Novel drug target Established target
    Trial Name metformin GR,Glumetza

    PMIDs:
    26471090 22722338 19428322 14500570 12890675 17307971 14502105 12086935 12960015 14871885


    Sources:
    DTC TdgClinicalTrial TEND PharmGKB

  • METFORMIN   PRPF31

    Interaction Score: 3.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    29650774


    Sources:
    PharmGKB

  • METFORMIN   NBEA

    Interaction Score: 3.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    29650774


    Sources:
    PharmGKB

  • METFORMIN   PRKAB2

    Interaction Score: 3.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26471090 22722338


    Sources:
    DTC PharmGKB

  • METFORMIN   CPA6

    Interaction Score: 3.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    29650774


    Sources:
    PharmGKB

  • METFORMIN   SLC19A3

    Interaction Score: 3.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26528626


    Sources:
    PharmGKB

  • METFORMIN   PRKAG3

    Interaction Score: 3.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26471090 22722338


    Sources:
    DTC PharmGKB

  • METFORMIN   FMO5

    Interaction Score: 3.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26306225


    Sources:
    PharmGKB

  • METFORMIN   PRKAG1

    Interaction Score: 3.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26471090 22722338


    Sources:
    DTC PharmGKB

  • METFORMIN   C11ORF65

    Interaction Score: 3.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28834135


    Sources:
    PharmGKB

  • METFORMIN   SP1

    Interaction Score: 2.44

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    29352482 24853734


    Sources:
    PharmGKB

  • METFORMIN   SLC22A3

    Interaction Score: 2.17

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25920679 22722338 20859243


    Sources:
    PharmGKB

  • METFORMIN   PRKAG2

    Interaction Score: 2.17

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26471090 22722338


    Sources:
    DTC PharmGKB

  • METFORMIN   SLC22A1

    Interaction Score: 1.86

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    29352482 28834135 28380657 27859023 26700958 24624919 22735389 22722338 19381165 17609683 17111267 21989078 20690652 19898263 19536068


    Sources:
    PharmGKB

  • METFORMIN   SLC29A4

    Interaction Score: 1.63

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22722338


    Sources:
    PharmGKB

  • METFORMIN   CAPN10

    Interaction Score: 1.63

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25327507


    Sources:
    PharmGKB

  • METFORMIN   SLC22A2

    Interaction Score: 1.36

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25939711 24624919 23417334 22722338


    Sources:
    PharmGKB

  • METFORMIN   PRKAA2

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22722338 26471090


    Sources:
    DTC PharmGKB

  • METFORMIN   ACACB

    Interaction Score: 0.81

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • METFORMIN   SLC2A2

    Interaction Score: 0.81

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • METFORMIN   HNF1B

    Interaction Score: 0.81

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • METFORMIN   PRKAA1

    Interaction Score: 0.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26471090 22722338


    Sources:
    DTC PharmGKB

  • METFORMIN   STK11

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type Advanced Solid Tumor
    Response Type no benefit
    Approval Status Preclinical

    PMIDs:
    17062558 18006825


    Sources:
    JAX-CKB

  • METFORMIN   HRAS

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type urinary bladder cancer
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    26921394 26951660


    Sources:
    JAX-CKB

  • METFORMIN   KCNJ11

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16595597


    Sources:
    PharmGKB

  • METFORMIN   NRAS

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25504439


    Sources:
    CIViC

  • METFORMIN   KRAS

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type endometrial cancer
    Response Type sensitive
    Approval Status Preclinical - Cell line xenograft

    PMIDs:
    23877793 24077915 32444490


    Sources:
    JAX-CKB CIViC

  • METFORMIN   ATM

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28834135


    Sources:
    PharmGKB

  • METFORMIN   PPARA

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24853734


    Sources:
    PharmGKB

  • METFORMIN   PTEN

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Approval Status Preclinical
    Indication/Tumor Type urinary bladder cancer
    Evidence Type Actionable

    PMIDs:
    26921394 24077915


    Sources:
    JAX-CKB

  • METFORMIN   NR1I2

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22722338


    Sources:
    PharmGKB

  • METFORMIN   PIK3CA

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type Advanced Solid Tumor
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    23986086


    Sources:
    JAX-CKB

  • METFORMIN   ERBB2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type Her2-receptor positive breast cancer
    Response Type predicted – sensitive
    Approval Status Phase III

    PMIDs:
    28375706


    Sources:
    JAX-CKB

  • METFORMIN   MTOR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • METFORMIN   IDH1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type colorectal cancer
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    26363012


    Sources:
    JAX-CKB

  • TEND: METFORMIN

    • Version: 01-August-2011

    Alternate Names:
    METFORMIN Primary Drug Name

    Drug Info:
    Drug Class hypoglycemic agents
    Year of Approval 1995

    Publications:

  • TdgClinicalTrial: METFORMIN

    • Version: January-2014

    Alternate Names:

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

    Publications:

  • DTC: METFORMIN

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL1431 ChEMBL Drug ID

    Drug Info:

    Publications:
    Seo WD et al., 2015, Saponarin activates AMPK in a calcium-dependent manner and suppresses gluconeogenesis and increases glucose uptake via phosphorylation of CRTC2 and HDAC5., Bioorg Med Chem Lett

  • PharmGKB: metformin

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Tkáč I et al., 2015, A pharmacogenetic association between a variation in calpain 10 (CAPN10) gene and the response to metformin treatment in patients with type 2 diabetes., Eur J Clin Pharmacol
    Goswami S et al., 2014, Genetic variants in transcription factors are associated with the pharmacokinetics and pharmacodynamics of metformin., Clin Pharmacol Ther
    Santoro AB et al., 2018, Influence of pharmacogenetic polymorphisms and demographic variables on metformin pharmacokinetics in an admixed Brazilian cohort., Br J Clin Pharmacol

  • JAX-CKB: Metformin

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Iglesias et al., 2013, Another surprise from Metformin: novel mechanism of action via K-Ras influences endometrial cancer response to therapy., Mol. Cancer Ther.
    Ma et al., 2013, K‑ras gene mutation as a predictor of cancer cell responsiveness to metformin., Mol Med Rep
    Sonnenblick et al., 2017, Impact of Diabetes, Insulin, and Metformin Use on the Outcome of Patients With Human Epidermal Growth Factor Receptor 2-Positive Primary Breast Cancer: Analysis From the ALTTO Phase III Randomized Trial., J. Clin. Oncol.

  • CIViC: METFORMIN

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Vujic et al., 2015, Metformin and trametinib have synergistic effects on cell viability and tumor growth in NRAS mutant cancer., Oncotarget
    Xie J et al., 2020, Metformin selectively inhibits metastatic colorectal cancer with the &lt;i&gt;KRAS&lt;/i&gt; mutation by intracellular accumulation through silencing MATE1., Proc Natl Acad Sci U S A

  • TTD: Metformin

    • Version: 2020.06.01

    Alternate Names:
    D0D7LA TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL1431

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • MyCancerGenomeClinicalTrial: METFORMIN

    • Version: 30-February-2014

    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 2020-10-21