Drug/Small Molecule:
metformin

PharmGKB contains no dosing guidelines for this drug/small molecule. To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.

PharmGKB has no annotated drug labels with pharmacogenomic information for this drug/small molecule. If you know of a drug label with PGx, send us a message.

Links to Unannotated Labels

These links are to labels associated with metformin that have not been annotated by PharmGKB.

  1. DailyMed - DrugLabel PA166105191

PharmGKB contains no Clinical Variants that meet the highest level of criteria.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

? = Mouse-over for quick help

This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?

The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

List of all metformin variant annotations

Gene ? Variant?
(142)
Alternate Names ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available No Clinical Annotations available VA
rs10213440 15048136T>C, 234+20036A>G, 23866339T>C, 30362A>G
T > C
Intronic
No VIP available No Clinical Annotations available VA
rs10747673 15898518A>G, 53755212A>G
A > G
Not Available
No VIP available CA VA
rs11212617 108283161C>A, 11845577C>A, 175-5285G>T
C > A
Intronic
rs12208357 160543148C>T, 181C>T, 64712605C>T, Arg61Cys, R61C, SLC22A1: R61C, SLC22A1:148C>T
C > T
Missense
Arg61Cys
No VIP available CA VA
rs12943590 -130C>T, 19223372G>A, 19619998G>A
G > A
5' UTR
No VIP available No Clinical Annotations available VA
rs13266634 118184783C>T, 227272C>T, 31458332C>T, 826C>T, 973C>T, SLC30A8:Arg325Trp, SLC30A8:R325W
C > T
Missense
Arg276Trp
No VIP available No Clinical Annotations available VA
rs149711321 -42-204T>C, 25984604T>C, 46594035T>C, 52537T>C
T > C
Intronic
No VIP available No Clinical Annotations available VA
rs1801282 -2-28078C>G, 12333125C>G, 12393125C>G, 34C>G, 68777C>G, PPARG: Pro12Ala, Pro12Ala
C > G
Intronic
Pro12Ala
No VIP available No Clinical Annotations available VA
rs2252281 -66T>C, 19040561T>C, 19437187T>C, SLC47A1: ¿66T>C
T > C
5' UTR
No VIP available CA VA
rs2282143 1022C>T, 160557643C>T, 64727100C>T, Pro341Leu, SLC22A1: P341L
C > T
Missense
Pro341Leu
No VIP available No Clinical Annotations available VA
rs2289669 19066717G>A, 19463343G>A, 922-158G>A
G > A
Intronic
No VIP available No Clinical Annotations available VA
rs249429 128-4551G>A, 40772239C>T, 40782239C>T
C > T
Intronic
No VIP available No Clinical Annotations available VA
rs2683511 15947796C>T, 1901-221C>T, 2024-221C>T, 2045-221C>T, 35512C>T, 53804490C>T
C > T
Intronic
No VIP available No Clinical Annotations available VA
rs2815752 42784358G>A, 72812440G>A
G > A
Not Available
No VIP available CA VA
rs316019 160670282A>C, 64839739A>C, 808T>G, SLC22A2: A270S, SLC22A2: Ala270Ser, Ser270Ala
A > C
Missense
Ser270Ala
rs34059508 1386-1170G>A, 1386-1170G>C, 1393G>A, 1393G>C, 160575837G>A, 160575837G>C, 64745294G>A, 64745294G>C, G465R, Gly465Arg, SLC22A1: G465R, SLC22A1:1393G>A
G > A
G > C
Intronic
Gly465Arg
VIP No Clinical Annotations available No Variant Annotations available
rs34130495 1201G>A, 160560824G>A, 64730281G>A, Gly401Ser, SLC22A1: G401S
G > A
Missense
Gly401Ser
No VIP available No Clinical Annotations available VA
rs34399035 1177G>A, 1219G>A, 1285G>A, 19188345C>T, 19584971C>T, Gly393Arg, Gly407Arg, Gly429Arg
C > T
Missense
Gly407Arg
No VIP available No Clinical Annotations available VA
rs34834489 -396C>T, 19223638G>A, 19620264G>A
G > A
5' Flanking
No VIP available No Clinical Annotations available VA
rs36056065 1276+1delG, 1276+1delGinsGTAAGTTG, 160560900delG, 160560900delGinsGTAAGTTG, 64730357delG, 64730357delGinsGTAAGTTG
GTAAGTTG > -
Intronic
No VIP available No Clinical Annotations available VA
rs3792269 10347A>G, 241531479A>G, 600A>G, 722347A>G, Pro200=
A > G
Synonymous
Pro200Pro
No VIP available No Clinical Annotations available VA
rs391300 -4-2593T>C, 1819632T>C, 2216258T>C
T > C
Intronic
No VIP available No Clinical Annotations available VA
rs461473 160543562G>A, 411+184G>A, 64713019G>A
G > A
Intronic
No VIP available No Clinical Annotations available VA
rs4810083 26316363T>C, 56120271T>C
T > C
Not Available
No VIP available CA VA
rs5219 -16-179A>G, 17349572T>C, 17409572T>C, 5635A>G, 67A>G, E23K, KCNJ11: Lys23Glu, KCNJ11:67A>G, KCNJ11:E23K, Lys23Glu
T > C
Intronic
Lys23Glu
No VIP available No Clinical Annotations available VA
rs578427 30531984C>T, 92412150C>T
C > T
Not Available
No VIP available CA VA
rs622342 1386-2964C>A, 1386-4141C>A, 160572866C>A, 64742323C>A
C > A
Intronic
No VIP available No Clinical Annotations available VA
rs6265 196G>A, 220G>A, 241G>A, 27619916C>T, 27679916C>T, 283G>A, 434C>T, 442G>A, 503C>T, 68690G>A, BDNF:Val66Met, Val148Met, Val66Met, Val74Met, Val81Met, Val95Met
C > T
Missense
Val66Met
No VIP available No Clinical Annotations available VA
rs628031 1222A>G, 160560845A>G, 64730302A>G, Met408Val
A > G
Missense
Met408Val
rs72552763 1260_1262delGAT, 160560883_160560885delGAT, 64730340_64730342delGAT, Met420_Ile421delinsIle
GAT > -
Non-synonymous
No VIP available No Clinical Annotations available VA
rs784888 1141-453G>C, 11870G>C, 1421+442G>C, 1425+442G>C, 15967814G>C, 53824508G>C
G > C
Intronic
No VIP available No Clinical Annotations available VA
rs784892 10246G>A, 15966190G>A, 53822884G>A, 967+90G>A
G > A
Intronic
No VIP available No Clinical Annotations available VA
rs8187725 1199C>T, 160858154C>T, 65027611C>T, Thr400Ile
C > T
Missense
Thr400Ile
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 142
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • Metformin HCL
  • metformin hydrochloride
Trade Names
  • Apo-Metformin
  • Fortamet
  • Gen-Metformin
  • Glucophage
  • Glucophage XR
  • Glumetza
  • Glycon
  • Mylan-Metformin
  • Novo-Metformin
  • Nu-Metformin
  • PMS-Metformin
  • Ran-Metformin
  • Ratio-Metformin
  • Riomet
  • Sandoz Metformin
  • Teva-Metformin
Brand Mixture Names

PharmGKB Accession Id:
PA450395

Description

Metformin is a biguanide antihyperglycemic agent used for treating non-insulin-dependent diabetes mellitus (NIDDM). It improves glycemic control by decreasing hepatic glucose production, decreasing glucose absorption and increasing insulin-mediated glucose uptake. Metformin is the only oral antihyperglycemic agent that is not associated with weight gain. Metformin may induce weight loss and is the drug of choice for obese NIDDM patients. When used alone, metformin does not cause hypoglycemia; however, it may potentiate the hypoglycemic effects of sulfonylureas and insulin. Its main side effects are dyspepsia, nausea and diarrhea. Dose titration and/or use of smaller divided doses may decrease side effects. Metformin should be avoided in those with severely compromised renal function (creatinine clearance < 30 ml/min), acute/decompensated heart failure, severe liver disease and for 48 hours after the use of iodinated contrast dyes due to the risk of lactic acidosis. Lower doses should be used in the elderly and those with decreased renal function. Metformin decreases fasting plasma glucose, postprandial blood glucose and glycosolated hemoglobin (HbA1c) levels, which are reflective of the last 8-10 weeks of glucose control. Metformin may also have a positive effect on lipid levels.

Source: Drug Bank

Indication

For use as an adjunct to diet and exercise in adult patients (18 years and older) with NIDDM. May also be used for the management of metabolic and reproductive abnormalities associated with polycystic ovary syndrome (PCOS).

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Metformin's mechanisms of action differ from other classes of oral antihyperglycemic agents. Metformin decreases blood glucose levels by decreasing hepatic glucose production, decreasing intestinal absorption of glucose, and improving insulin sensitivity by increasing peripheral glucose uptake and utilization. These effects are mediated by the initial activation by metformin of AMP-activated protein kinase (AMPK), a liver enzyme that plays an important role in insulin signaling, whole body energy balance, and the metabolism of glucose and fats. Activation of AMPK is required for metformin's inhibitory effect on the production of glucose by liver cells. Increased peripheral utilization of glucose may be due to improved insulin binding to insulin receptors. Metformin administration also increases AMPK activity in skeletal muscle. AMPK is known to cause GLUT4 deployment to the plasma membrane, resulting in insulin-independent glucose uptake. The rare side effect, lactic acidosis, is thought to be caused by decreased liver uptake of serum lactate, one of the substrates of gluconeogenesis. In those with healthy renal function, the slight excess is simply cleared. However, those with severe renal impairment may accumulate clinically significant serum lactic acid levels. Other conditions that may precipitate lactic acidosis include severe hepatic disease and acute/decompensated heart failure.

Source: Drug Bank

Pharmacology

Metformin is an oral antihyperglycemic agent that improves glucose tolerance in patients with NIDDM, lowering both basal and postprandial plasma glucose. Metformin is not chemically or pharmacologically related to any other class of oral antihyperglycemic agents. Unlike sulfonylureas, metformin does not produce hypoglycemia in either patients with NIDDM or healthy subjects and does not cause hyperinsulinemia. Metformin does not affect insulin secretion.

Source: Drug Bank

Food Interaction

Avoid alcohol.|Take with food to reduce gastric irritation.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Metformin is not metabolized.

Source: Drug Bank

Protein Binding

Metformin is negligibly bound to plasma proteins.

Source: Drug Bank

Absorption

Absorbed over 6 hours, bioavailability is 50 to 60% under fasting conditions. Administration with food decreases and delays absorption. Some evidence indicates that the level of absorption is not dose-related, suggesting that absorption occurs through a saturable process. Limited data from animal and human cell cultures indicate that absorption occurs through a passive, non-saturable process, possibly involving a paracellular route. Peak action occurs 3 hours after oral administration.

Source: Drug Bank

Half-Life

6.2 hours. Duration of action is 8-12 hours.

Source: Drug Bank

Toxicity

Acute oral toxicity (LD 50): 350 mg/kg Rabbit. It would be expected that adverse reactions of a more intense character including epigastric discomfort, nausea, and vomiting followed by diarrhea, drowsiness, weakness, dizziness, malaise and headache might be seen.

Source: Drug Bank

Clearance

718-1552 mL/minute following single oral dose of 0.5-1.5 g. Metformin is removed by hemodialysis at a rate of approximately 170 ml/min under good hemodynamic conditions.

Source: Drug Bank

Route of Elimination

Intravenous single-dose studies in normal subjects demonstrate that metformin is excreted unchanged in the urine and does not undergo hepatic metabolism (no metabolites have been identified in humans) nor biliary excretion. Approximately 90% of the drug is eliminated in 24 hours in those with healthy renal function. Renal clearance of metformin is approximately 3.5 times that of creatinine clearance, indicating the tubular secretion is the primary mode of metformin elimination.

Source: Drug Bank

Volume of Distribution

654 L for metformin 850 mg administered as a single dose. The volume of distribution following IV administration is 63-276 L, likely due to less binding in the GI tract and/or different methods used to determine volume of distribution.

Source: Drug Bank

Chemical Properties

Chemical Formula

C4H11N5

Source: Drug Bank

Isomeric SMILES

CC(=N)NC(=N)N(C)C

Source: OpenEye

Canonical SMILES

CN(C)C(=N)NC(N)=N

Source: Drug Bank

Average Molecular Weight

129.1636

Source: Drug Bank

Monoisotopic Molecular Weight

129.101445377

Source: Drug Bank

PharmGKB Curated Pathways

Pathways created internally by PharmGKB based primarily on literature evidence.

External Pathways

Links to non-PharmGKB pathways.

PharmGKB contains no links to external pathways for this drug. To report a pathway, click here.

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
PRKAB1 (source: Drug Bank)

Drug Interactions

Drug Description
metformin Increases the effect of metformin (source: Drug Bank)
metformin Increases the effect of metformin (source: Drug Bank)
cimetidine Cimetidine increases the effect of metformin (source: Drug Bank)
cimetidine Cimetidine increases the effect of metformin (source: Drug Bank)
glucosamine Possible hyperglycemia (source: Drug Bank)
somatropin recombinant Somatropin may antagonize the hypoglycemic effect of metformin. Monitor for changes in fasting and postprandial blood sugars. (source: Drug Bank)

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

Publications related to metformin: 67

No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
A pharmacogenetic association between a variation in calpain 10 (CAPN10) gene and the response to metformin treatment in patients with type 2 diabetes. European journal of clinical pharmacology. 2014. Tkáč Ivan, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
OCT1 is a high-capacity thiamine transporter that regulates hepatic steatosis and is a target of metformin. Proceedings of the National Academy of Sciences of the United States of America. 2014. Chen Ligong, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Genetic Variants in Transcription Factors Associate with the Pharmacokinetics and Pharmacodynamics of Metformin. Clinical pharmacology and therapeutics. 2014. Goswami Srijib, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Adoption of a clinical pharmacogenomics implementation program during outpatient care-initial results of the University of Chicago "1,200 Patients Project". American journal of medical genetics. Part C, Seminars in medical genetics. 2014. O'Donnell Peter H, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
A gene-gene interaction between polymorphisms in the OCT2 and MATE1 genes influences the renal clearance of metformin. Pharmacogenetics and genomics. 2013. Christensen Mette M H, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Functional characterization of MATE2-K genetic variants and their effects on metformin pharmacokinetics. Pharmacogenetics and genomics. 2013. Chung Jae-Yong, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Emerging Transporters of Clinical Importance: An Update from the International Transporter Consortium. Clinical pharmacology and therapeutics. 2013. Hillgren Kathleen M, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Influences of organic cation transporter polymorphisms on the population pharmacokinetics of metformin in healthy subjects. The AAPS journal. 2013. Yoon Hwa, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
The Effect of Novel Promoter Variants in MATE1 and MATE2 on the Pharmacokinetics and Pharmacodynamics of Metformin. Clinical pharmacology and therapeutics. 2013. Stocker S L, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Trimethoprim-Metformin Interaction and its Genetic Modulation by OCT2 and MATE1. British journal of clinical pharmacology. 2013. Grün Barbara, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Metformin-induced Pseudoporphyria. Journal of drugs in dermatology : JDD. 2012. Lenfestey Amy, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenomics in clinical practice and drug development. Nature biotechnology. 2012. Harper Andrew R, et al. PubMed
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. Pharmacogenetics and genomics. 2012. Tarasova Linda, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Pharmacogenomic association between a variant in SLC47A1 gene and therapeutic response to metformin in type 2 diabetes. Diabetes, obesity & metabolism. 2012. Tkáč Ivan, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
A gene variant near ATM is significantly associated with metformin treatment response in type 2 diabetes: a replication and meta-analysis of five cohorts. Diabetologia. 2012. van Leeuwen N, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
The C Allele of ATM rs11212617 Does Not Associate With Metformin Response in the Diabetes Prevention Program. Diabetes care. 2012. Florez Jose C, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The role of ATM in response to metformin treatment and activation of AMPK. Nature genetics. 2012. Yee Sook Wah, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Mortality After Incident Cancer in People With and Without Type 2 Diabetes: Impact of metformin on survival. Diabetes care. 2012. Currie Craig J, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Serine racemase rs391300¿G/A polymorphism influences the therapeutic efficacy of metformin in Chinese patients with diabetes mellitus type 2. Clinical and experimental pharmacology & physiology. 2011. Dong Min, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Genetic Predictors of Weight Loss and Weight Regain After Intensive Lifestyle Modification, Metformin Treatment, or Standard Care in the Diabetes Prevention Program. Diabetes care. 2011. Delahanty Linda M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Effects of genetic variants previously associated with fasting glucose and insulin in the diabetes prevention program. PloS one. 2012. Florez Jose C, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Association of the SLC30A8 missense polymorphism R325W with proinsulin levels at baseline and after lifestyle, metformin or troglitazone intervention in the Diabetes Prevention Program. Diabetologia. 2011. Majithia A R, et al. PubMed
The pharmacogenetics of metformin and its impact on plasma metformin steady-state levels and glycosylated hemoglobin A1c. Pharmacogenetics and genomics. 2011. Christensen Mette M H, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
A Common 5'-UTR Variant in MATE2-K Is Associated With Poor Response to Metformin. Clinical pharmacology and therapeutics. 2011. Choi J H, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Transporter-mediated drug-drug interactions. Pharmacogenomics. 2011. Müller Fabian, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Levels of evidence needed for changing indications, contraindications, and food and drug administration labeling: the case of metformin. Archives of internal medicine. 2011. Eurich Dean T, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Rifampin enhances the glucose-lowering effect of metformin and increases OCT1 mRNA levels in healthy participants. Clinical pharmacology and therapeutics. 2011. Cho S K, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Common variants near ATM are associated with glycemic response to metformin in type 2 diabetes. Nature genetics. 2010. The GoDARTS and UKPDS Diabetes Pharmacogenetics Study Group, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Role of organic cation transporter 3 (SLC22A3) and its missense variants in the pharmacologic action of metformin. Pharmacogenetics and genomics. 2010. Chen Ligong, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Common variants in 40 genes assessed for diabetes incidence and response to metformin and lifestyle intervention in the diabetes prevention program. Diabetes. 2010. Jablonski Kathleen A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Organic cation transporter 1 polymorphisms predict the metabolic response to metformin in women with the polycystic ovary syndrome. The Journal of clinical endocrinology and metabolism. 2010. Gambineri Alessandra, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Genetic polymorphisms in organic cation transporter 1 (OCT1) in Chinese and Japanese populations exhibit altered function. The Journal of pharmacology and experimental therapeutics. 2010. Chen Ligong, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Membrane interactions of novicidin, a novel antimicrobial peptide: phosphatidylglycerol promotes bilayer insertion. The journal of physical chemistry. B. 2010. Dorosz Jerzy, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Drug transporter pharmacogenetics in nucleoside-based therapies. Pharmacogenomics. 2010. Errasti-Murugarren Ekaitz, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Genotype-dependent effects of inhibitors of the organic cation transporter, OCT1: predictions of metformin interactions. The pharmacogenomics journal. 2010. Ahlin G, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Role of human placental apical membrane transporters in the efflux of glyburide, rosiglitazone, and metformin. American journal of obstetrics and gynecology. 2010. Hemauer Sarah J, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenomics of membrane transporters: past, present and future. Pharmacogenomics. 2010. Yee Sook Wah, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Heterozygous variants of multidrug and toxin extrusions (MATE1 and MATE2-K) have little influence on the disposition of metformin in diabetic patients. Pharmacogenetics and genomics. 2010. Toyama Kana, et al. PubMed
Interaction between polymorphisms in the OCT1 and MATE1 transporter and metformin response. Pharmacogenetics and genomics. 2010. Becker Matthijs L, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Current understanding of the pharmacogenomics of metformin. Clinical pharmacology and therapeutics. 2009. Zolk O. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
The effects of genetic polymorphisms in the organic cation transporters OCT1, OCT2, and OCT3 on the renal clearance of metformin. Clinical pharmacology and therapeutics. 2009. Tzvetkov M V, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The LKB1-AMPK pathway: metabolism and growth control in tumour suppression. Nature reviews. Cancer. 2009. Shackelford David B, et al. PubMed
Genetic variation in the organic cation transporter 1 is associated with metformin response in patients with diabetes mellitus. The pharmacogenomics journal. 2009. Becker M L, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Effect of genetic variation in the organic cation transporter 2 on the renal elimination of metformin. Pharmacogenetics and genomics. 2009. Chen Ying, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Genetic variants in multidrug and toxic compound extrusion-1, hMATE1, alter transport function. The pharmacogenomics journal. 2009. Chen Ying, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Genetic variation in the multidrug and toxin extrusion 1 transporter protein influences the glucose-lowering effect of metformin in patients with diabetes: a preliminary study. Diabetes. 2009. Becker Matthijs L, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The antidiabetic drug metformin suppresses HER2 (erbB-2) oncoprotein overexpression via inhibition of the mTOR effector p70S6K1 in human breast carcinoma cells. Cell cycle (Georgetown, Tex.). 2009. Vazquez-Martin Alejandro, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Genetic variants of the organic cation transporter 2 influence the disposition of metformin. Clinical pharmacology and therapeutics. 2008. Song I S, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Is pharmacogenomics our future? Metformin, ovulation and polymorphism of the STK11 gene in polycystic ovary syndrome. Pharmacogenomics. 2008. Goldenberg Naila, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
OCT2 polymorphisms and in-vivo renal functional consequence: studies with metformin and cimetidine. Pharmacogenetics and genomics. 2008. Wang Zhi-Jun, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The antidiabetic drug metformin exerts an antitumoral effect in vitro and in vivo through a decrease of cyclin D1 level. Oncogene. 2008. Ben Sahra I, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Metformin versus insulin for the treatment of gestational diabetes. The New England journal of medicine. 2008. Rowan Janet A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Polymorphism in human organic cation transporters and metformin action. Pharmacogenomics. 2008. Takane Hiroshi, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Ovulatory response to treatment of polycystic ovary syndrome is associated with a polymorphism in the STK11 gene. The Journal of clinical endocrinology and metabolism. 2008. Legro Richard S, et al. PubMed
Effect of genetic variation in the organic cation transporter 1, OCT1, on metformin pharmacokinetics. Clinical pharmacology and therapeutics. 2008. Shu Y, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Cell cycle arrest in Metformin treated breast cancer cells involves activation of AMPK, downregulation of cyclin D1, and requires p27Kip1 or p21Cip1. Journal of molecular signaling. 2008. Zhuang Yongxian, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Metformin transport by a newly cloned proton-stimulated organic cation transporter (plasma membrane monoamine transporter) expressed in human intestine. Drug metabolism and disposition: the biological fate of chemicals. 2007. Zhou Mingyan, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Effect of genetic variation in the organic cation transporter 1 (OCT1) on metformin action. The Journal of clinical investigation. 2007. Shu Yan, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Human organic cation transporter (OCT1 and OCT2) gene polymorphisms and therapeutic effects of metformin. Journal of human genetics. 2007. Shikata Eriko, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenetics of glucose-lowering drug treatment: a systematic review. Molecular diagnosis & therapy. 2007. Bozkurt Ozlem, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
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. The Journal of clinical endocrinology and metabolism. 2006. Sesti Giorgio, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Glibenclamide-induced acute haemolytic anaemia revealing a G6PD-deficiency. Diabetes research and clinical practice. 2004. Vinzio Stéphane, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Evolutionary conservation predicts function of variants of the human organic cation transporter, OCT1. Proceedings of the National Academy of Sciences of the United States of America. 2003. Shu Yan, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Role of AMP-activated protein kinase in mechanism of metformin action. The Journal of clinical investigation. 2001. Zhou G, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
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). Diabetic medicine : a journal of the British Diabetic Association. 2001. Gloyn A L, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Evidence that metformin exerts its anti-diabetic effects through inhibition of complex 1 of the mitochondrial respiratory chain. The Biochemical journal. 2000. Owen M R, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Dimethylbiguanide inhibits cell respiration via an indirect effect targeted on the respiratory chain complex I. The Journal of biological chemistry. 2000. El-Mir M Y, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0781-5050-61
DrugBank:
DB00331
ChEBI:
6801
KEGG Compound:
C07151
KEGG Drug:
D04966
PubChem Compound:
4091
PubChem Substance:
46507752
9360
Drugs Product Database (DPD):
2265583
ChemSpider:
3949
Therapeutic Targets Database:
DAP000205
FDA Drug Label at DailyMed:
e455ec79-08cd-4d75-9cb2-625d3912ee88

Clinical Trials

These are trials that mention metformin and are related to either pharmacogenetics or pharmacogenomics.

Common Searches

Search PubMed
Search Medline Plus
Search PubChem
Search CTD

Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.