Metformin
Highest phase reached
Approved
Drug type
Small molecule
First approval year
1995
- First approval year
- 1995
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Metformin
- Molecular weight
- 129.17
- Structure (SMILES)
- CN(C)C(=N)NC(=N)N
- la 6023
- LA-6023
- metformin
- Metformin
- METFORMIN
- Metformin (1 mg/ 50 mg/ 500 mg)
- metformin [INN]
- METFORMIN [MI]
- METFORMIN [USAN]
- METFORMIN [VANDF]
- Metformin [WHO-DD]
- metformin 1 mg 50 mg 500 mg
- metformin 12 5mg 1000mg film coated tablets
- Metformin 12.5mg/1000mg Film-coated tablets
- metformin 50 mg 1000 mg fdc tablet
- metformin 50 mg 500 mg fdc tablet
- metformin 50 mg 850 mg fdc tablet
- metformin 50 mg/1000 mg FDC tablet
- metformin 50 mg/500 mg FDC tablet
- metformin 50 mg/850 mg FDC tablet
- metformin 500 mg xr
- Metformin 500 mg XR
- metformin 750 mg
- Metformin 750 mg
- metformin extended release
And 10 more, listed on the interactive page.
- ATC classification codes
- A10BA02
Sources for recorded values
- CAS registry numbers
- 657-24-9
- ChEMBL ID
- CHEMBL1431
- InChIKey
- XZWYZXLIPXDOLR-UHFFFAOYSA-N
- FDA ingredient codes (UNII)
- 9100L32L2N
- 4091
- 152743144
- 155906370
- 6809
- 235743
- Applicant
- EMD SERONO INC
- Approval date
- 3 Mar 1995
- Application number
- NDA020357
- Patents
- 0
- Designations
- 1
- First in class
- No
- Fast track
- No
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Boxed warning
- Yes
- United States (FDA)
- Approved
- Pharmacology name
- metformin
- Type
- Synthetic organic
- Drug name stem
- -formin
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Mechanism
- Mitochondrial complex I (NADH dehydrogenase) inhibitor
- Action type
- Inhibitor
- Target
- Mitochondrial complex I (NADH dehydrogenase)
- Mechanism
- Mitochondrial glycerol-3-phosphate dehydrogenase inhibitor
- Action type
- Inhibitor
- Target
- Glycerol-3-phosphate dehydrogenase, mitochondrial
DrugCentral mechanisms
- Action type
- Inhibitor
- Gene symbol
- NDUFS8|NDUFA4|NDUFAB1|NDUFA1|NDUFS4|NDUFB5|NDUFB3|NDUFC1|NDUFA2|NDUFS5|NDUFS7|NDUFS2|NDUFS6|NDUFB1|NDUFS3|NDUFB6|NDUFA3|NDUFB4|NDUFB8|NDUFB2|NDUFA7|NDUFC2|NDUFA10|NDUFB10|MT-ND1|MT-ND2|MT-ND3|MT-ND4L|MT-ND4|MT-ND5|MT-ND6|NDUFB7|NDUFV2|NDUFS1|NDUFV1|NDUFA8|NDUFV3|NDUFA6|NDUFA5|NDUFA9|NDUFA11|NDUFAF2|NDUFAF3|NDUFA4L2|NDUFB11|NDUFAF4|NDUFA13|NDUFA12|NDUFAF1|NDUFB9
- Protein identifier
- O00217|O00483|O14561|O15239|O43181|O43674|O43676|O43677|O43678|O43920|O75251|O75306|O75380|O75438|O75489|O95139|O95167|O95168|O95169|O95178|O95182|O95298|O95299|O96000|P03886|P03891|P03897|P03901|P03905|P03915|P03923|P17568|P19404|P28331|P49821|P51970|P56181|P56556|Q16718|Q16795|Q86Y39|Q8N183|Q9BU61|Q9NRX3|Q9NX14|Q9P032|Q9P0J0|Q9UI09|Q9Y375|Q9Y6M9
- Organism
- Homo sapiens
- Target development level
- Tclin|Tbio|Tchem|NA
- Condition
- Leukemia, Lymphocytic, Chronic, B-Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000095
- Subject identifier
- D015451
- Condition
- Carcinoma, Squamous Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000181
- Subject identifier
- D002294
- Condition
- Carcinoma, Hepatocellular
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000182
- Subject identifier
- D006528
- Condition
- Metabolic Syndrome
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000195
- Subject identifier
- D024821
- Condition
- Prostatic Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000196
- Subject identifier
- D011471
- Condition
- Squamous Cell Carcinoma of Head and Neck
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000199
- Subject identifier
- D000077195
- Condition
- Precursor Cell Lymphoblastic Leukemia-Lymphoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000220
- Subject identifier
- D054198
- Condition
- Adenocarcinoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000228
- Subject identifier
- D000230
- Condition
- Atrial Fibrillation
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000275
- Subject identifier
- D001281
- Condition
- Barrett Esophagus
- Highest recorded phase
- 0.5
- Condition identifier
- EFO:0000280
- Subject identifier
- D001471
- Condition
- Breast Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000305
- Subject identifier
- D001943
- Condition
- Adenocarcinoma, Bronchiolo-Alveolar
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000308
- Subject identifier
- D002282
- Condition
- Carcinoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000313
- Subject identifier
- D002277
- Condition
- Cardiovascular Diseases
- Highest recorded phase
- 0.5
- Condition identifier
- EFO:0000319
- Subject identifier
- D002318
- Condition
- Pulmonary Disease, Chronic Obstructive
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000341
- Subject identifier
- D029424
- Condition
- Colorectal Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000365
- Subject identifier
- D015179
- Condition
- Diabetes Mellitus
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000400
- Subject identifier
- D003920
- Condition
- Lymphoma, Large B-Cell, Diffuse
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000403
- Subject identifier
- D016403
- Condition
- Epilepsy
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000474
- Subject identifier
- D004827
- Condition
- Glioblastoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000519
- Subject identifier
- D005909
- Condition
- Hypertension
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000537
- Subject identifier
- D006973
- Condition
- Infertility
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000545
- Subject identifier
- D007246
- Condition
- Adenocarcinoma of Lung
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000571
- Subject identifier
- D000077192
- Condition
- Metabolic Diseases
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000589
- Subject identifier
- D008659
- Condition
- Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
And 132 more, listed on the interactive page.
- Condition identifier
- EFO_0000095
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000181
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000182
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000195
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000196
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000199
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000220
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000228
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000275
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000319
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000341
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000365
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000400
- Condition identifier
- EFO_0000403
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000474
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000519
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000537
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000545
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000589
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000616
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000649
- Condition identifier
- EFO_0000660
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000668
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000673
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000676
- Highest recorded phase
- 3
And 355 more, listed on the interactive page.
- Warning
- Black Box Warning
- Effect
- cardiotoxicity
- Country
- United States
- Warning
- Black Box Warning
- Effect
- metabolic toxicity
- Country
- United States
- Warning
- Black Box Warning
- Effect
- respiratory toxicity
- Country
- United States
- Warning
- Black Box Warning
- Effect
- vascular toxicity
- Country
- United States
- Event
- acute kidney injury
- Reports
- 5,387
- Reporting signal score
- 10,192.8
- Event
- anuria
- Reports
- 466
- Reporting signal score
- 1,001.57
- Event
- blood glucose increased
- Reports
- 694
- Reporting signal score
- 492.308
- Event
- blood lactic acid increased
- Reports
- 260
- Reporting signal score
- 536.85
- Event
- diabetes mellitus inadequate control
- Reports
- 618
- Reporting signal score
- 1,249.12
- Event
- diabetic ketoacidosis
- Reports
- 657
- Reporting signal score
- 881.913
- Event
- diabetic metabolic decompensation
- Reports
- 223
- Reporting signal score
- 689.285
- Event
- diarrhoea
- Reports
- 2,429
- Reporting signal score
- 554.094
- Event
- euglycaemic diabetic ketoacidosis
- Reports
- 252
- Reporting signal score
- 546.968
- Event
- glycosylated haemoglobin increased
- Reports
- 403
- Reporting signal score
- 631.354
- Event
- hyperglycaemia
- Reports
- 722
- Reporting signal score
- 931.634
- Event
- hyperkalaemia
- Reports
- 1,327
- Reporting signal score
- 2,231.92
- Event
- hyperlactacidaemia
- Reports
- 392
- Reporting signal score
- 1,182.08
- Event
- hypoglycaemia
- Reports
- 2,567
- Reporting signal score
- 5,471.19
- Event
- hypoglycaemic coma
- Reports
- 282
- Reporting signal score
- 699.224
- Event
- hypotension
- Reports
- 1,394
- Reporting signal score
- 568.004
- Event
- hypothermia
- Reports
- 341
- Reporting signal score
- 523.621
- Event
- ketoacidosis
- Reports
- 282
- Reporting signal score
- 530.84
- Event
- lactic acidosis
- Reports
- 7,697
- Reporting signal score
- 27,700.7
- Event
- metabolic acidosis
- Reports
- 2,412
- Reporting signal score
- 6,093.29
- Event
- pemphigoid
- Reports
- 435
- Reporting signal score
- 897.84
- Event
- renal failure
- Reports
- 1,098
- Reporting signal score
- 923.3
- Event
- renal failure acute
- Reports
- 657
- Reporting signal score
- 441.611
- Event
- shock
- Reports
- 760
- Reporting signal score
- 1,379.98
- Event
- suicide attempt
- Reports
- 743
- Reporting signal score
- 540.561
And 3 more, listed on the interactive page.
- NCT00000620
- NCT00032487
- NCT00067951
- NCT00069836
- NCT00081328
- NCT00086502
- NCT00086515
- NCT00087516
- NCT00097279
- NCT00097500
- NCT00099866
- NCT00102466
- NCT00103857
- NCT00106340
- NCT00110851
- NCT00111631
- NCT00121641
- NCT00121667
- NCT00131664
- NCT00174642
- NCT00184574
- NCT00251953
- NCT00261352
- NCT00263276
- NCT00263965
And 595 more, listed on the interactive page.
- Dose
- 500 mg
- Route
- Oral
- How often
- Twice daily
- Hydrogen bond acceptors
- 2
- Hydrogen bond donors
- 4
- Polar surface area
- 88.99
- Calculated partition coefficient (ALogP)
- -1.03
- Calculated partition coefficient (XLogP)
- -1.3
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 0
- Heavy atoms
- 9
- Molecular formula
- C4H11N5
- Monoisotopic mass
- 129.10144537
- Natural product
- Yes
- Recorded assays
- 4,318
- Active assays
- 17
- Confirmatory
- Other
- Hypoglycemic Agents
Distribution coefficient (LogD)
- Median
- -3.37
- Mean
- -3.38333
- Minimum
- -3.41
- Maximum
- -3.37
- Unit
- unitless
- Assays
- 3
- Standard deviation
- 0.023094
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- LogD
Oral bioavailability
- Median
- 50
- Mean
- 47.6667
- Minimum
- 43
- Maximum
- 50
- Unit
- %
- Assays
- 3
- Standard deviation
- 4.04145
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- F
Related records
Trials (1,830)
- "MetCool ACS"- Metformin "Cooling" Effect on Metformin-naive Patients Treated With PCI Because of Acute Coronary Syndrome
- 1% Metformin in Moderate and Severe Periodontitis
- 12 Weeks Treatment With 3 Different Doses of BI 10773 in Type 2 Diabetic Patients
- 24-Hour Glycemia: Rosiglitazone Versus Glimepiride In Type 2 Diabetes
- 24-week Study Comparing Lixisenatide to Sitagliptin as add-on to Metformin in Obese Type 2 Diabetic Patients Younger Than 50 Years
- 24-week Treatment With Lixisenatide in Type 2 Diabetes Insufficiently Controlled With Metformin and Insulin Glargine
- 30-Week Extension to an Initial Combination Study (24 Weeks in Duration) of Sitagliptin With Pioglitazone (0431-064)
- 52-week add-on to Metformin Comparison of Saxagliptin and Sulphonylurea, With a 52-week Extension Period
- A 12 Week Study in Patients With Type 2 Diabetes Mellitus (T2DM)
- A 24-week Open-Label, Phase 3b Trial With a 28-week Extension to Evaluate the Efficacy and Safety of Saxagliptin Co-administered With Dapagliflozin Compared to Insulin Glargine in Subjects withType 2 Diabetes Who Have Glycemic Control on Metformin
- A Clinical Drug-Drug Interaction (DDI) Study With Omaveloxolone
- A Clinical Study of Calderasib (MK-1084) With Rosuvastatin and Metformin in Healthy People (MK-1084-016)
- A Clinical Study of Ulonivirine (MK-8507) With Atorvastatin and Metformin in Healthy Adults (MK-8507-018)
- A Clinical Trial for Analysis of Intestinal Microbiome Affecting PK, PD, and Safety of Metformin
- A Clinical Trial of Metformin in the Maintenance of Non-Hodgkin's Lymphoma Patients
- A Clinical Trial of Metformin to Decrease Glucocorticoids Side Effects in Patients With Autoimmune Uveitis
- A Clinical Trial Study to Determine the Effect of an Investigational Drug (SEP-363856) Has on the Way That the Drug Metformin Travels Through the Body in People With Schizophrenia.
- A Clinical Trial to Evaluate the Effect of Nilotinib on the PK/PD of Meformin
- A Clinical Trial to Evaluate the Efficacy, Tolerability, and Safety of a Fixed Dose Combination of Spironolactone, Pioglitazone & Metformin (SPIOMET) in Polycystic Ovary Syndrome (PCOS)
- A Clinical Trial to Prevent the Complications of Insulin Resistance (Including Type-2 Diabetes)
Approved for (1)
In development for (233)
- Abdominal aortic aneurysm Phase 2
- Acanthosis nigricans Phase 2
- Acne Phase 2
- Acute coronary syndrome Phase 3
- Acute kidney injury Phase 2
- Acute leukemia Phase 1
- Acute lymphoblastic leukemia Phase 1
- Acute myeloid leukemia Phase 2
- Adenocarcinoma Phase 2
- Adenoma Phase 1
- Age-related macular degeneration Phase 2
- Alopecia areata Phase 1
- Alopecia totalis Phase 1
- Alopecia universalis congenita Phase 1
- Alzheimer disease Phase 1
- Amyotrophic lateral sclerosis Phase 2
- Angiosarcoma Phase 2
- Asthma Phase 2
- Atherosclerosis Phase 3
- Atrial fibrillation Phase 2
Other linked conditions (17)
- Anovulation
- Anxiety
- Autism
- Chronic hepatitis B virus infection
- Chronic pancreatitis
- Cognitive disorder
- Differentiated thyroid carcinoma
- Endocrine system disorder
- Glucose metabolism disease
- Heart disorder
- Hepatitis B virus infection
- Hyperlipidemia
- Hyperprolactinemia
- Myocardial ischemia
- Open-angle glaucoma
- Pregnancy disorder
- Psoriatic arthritis
Targets (51)
- COXFA4 Mitochondrial complex I (NADH dehydrogenase) inhibitor
- COXFA4L2 Mitochondrial complex I (NADH dehydrogenase) inhibitor
- GPD2 Mitochondrial glycerol-3-phosphate dehydrogenase inhibitor
- MT-ND1 Mitochondrial complex I (NADH dehydrogenase) inhibitor
- MT-ND2 Mitochondrial complex I (NADH dehydrogenase) inhibitor
- MT-ND3 Mitochondrial complex I (NADH dehydrogenase) inhibitor
- MT-ND4 Mitochondrial complex I (NADH dehydrogenase) inhibitor
- MT-ND4L Mitochondrial complex I (NADH dehydrogenase) inhibitor
- MT-ND5 Mitochondrial complex I (NADH dehydrogenase) inhibitor
- MT-ND6 Mitochondrial complex I (NADH dehydrogenase) inhibitor
- NDUFA1 Mitochondrial complex I (NADH dehydrogenase) inhibitor
- NDUFA10 Mitochondrial complex I (NADH dehydrogenase) inhibitor
- NDUFA11 Mitochondrial complex I (NADH dehydrogenase) inhibitor
- NDUFA12 Mitochondrial complex I (NADH dehydrogenase) inhibitor
- NDUFA13 Mitochondrial complex I (NADH dehydrogenase) inhibitor
- NDUFA2 Mitochondrial complex I (NADH dehydrogenase) inhibitor
- NDUFA3 Mitochondrial complex I (NADH dehydrogenase) inhibitor
- NDUFA5 Mitochondrial complex I (NADH dehydrogenase) inhibitor
- NDUFA6 Mitochondrial complex I (NADH dehydrogenase) inhibitor
- NDUFA7 Mitochondrial complex I (NADH dehydrogenase) inhibitor