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metformin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
antihyperglycaemics, phenformin derivatives	1725	657-24-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: metformin metformin hydrochloride glucophage LA-6023 LA 6023 N,N-dimethylguanylguanidine metformin HCl	A biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. (From Martindale, The Extra Pharmacopoeia, 30th ed, p289) Molecular weight: 129.17 Formula: C4H11N5 CLOGP: -1.43 LIPINSKI: 0 HAC: 5 HDO: 4 TPSA: 88.99 ALOGS: -1.97 ROTB: 0 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

metformin
metformin hydrochloride
glucophage
LA-6023
LA 6023
N,N-dimethylguanylguanidine
metformin HCl

A biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. (From Martindale, The Extra Pharmacopoeia, 30th ed, p289)

Molecular weight: 129.17
Formula: C4H11N5
CLOGP: -1.43
LIPINSKI: 0
HAC: 5
HDO: 4
TPSA: 88.99
ALOGS: -1.97
ROTB: 0

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
2	g	O

ADMET properties:

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Property	Value	Reference
EoM (Fraction excreted unchanged in urine)	99 %	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	7.40 mL/min/kg	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	52 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
MRTD (Maximum Recommended Therapeutic Daily Dose)	387.10 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	100 mg/mL	Bocci G, Oprea TI, Benet LZ
t_half (Half-life)	1.70 hours	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	1 %	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.64 L/kg	Lombardo F, Berellini G, Obach RS

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Approvals:

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Date	Agency	Company
Jan. 1, 1961	PMDA
July 28, 2006	EMA	CHEPLAPHARM Arzneimittel GmbH
March 3, 1995	FDA	BRISTOL MYERS SQUIBB

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FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Lactic acidosis	15268.58	9.90	6357	360186	31930	63090549
Acute kidney injury	4034.17	9.90	6179	360364	257236	62865243
Hypoglycaemia	3384.52	9.90	2791	363752	57274	63065205
Metabolic acidosis	3180.93	9.90	2392	364151	42677	63079802
Diabetic ketoacidosis	2288.60	9.90	1444	365099	19061	63103418
Blood glucose increased	1988.43	9.90	2434	364109	81322	63041157
Ketoacidosis	1117.57	9.90	533	366010	3845	63118634
Diabetes mellitus inadequate control	1100.09	9.90	818	365725	14308	63108171
Glycosylated haemoglobin increased	1056.06	9.90	738	365805	11660	63110819
Euglycaemic diabetic ketoacidosis	1038.74	9.90	480	366063	3194	63119285

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Lactic acidosis	10902.89	11.05	5543	299849	29229	34622310
Acute kidney injury	2197.74	11.05	6730	298662	298258	34353281
Hypoglycaemia	2045.89	11.05	2453	302939	52187	34599352
Metabolic acidosis	1969.40	11.05	2159	303233	41521	34610018
Diabetic ketoacidosis	1561.18	11.05	1280	304112	16752	34634787
Blood glucose increased	1104.48	11.05	2042	303350	64676	34586863
Glycosylated haemoglobin increased	852.67	11.05	743	304649	10617	34640922
Euglycaemic diabetic ketoacidosis	847.99	11.05	458	304934	2764	34648775
Diabetes mellitus inadequate control	761.42	11.05	752	304640	12712	34638827
Hyperkalaemia	736.10	11.05	1771	303621	67618	34583921

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Lactic acidosis	25611.77	10.19	11672	559962	58687	79114067
Acute kidney injury	6251.11	10.19	12353	559281	507051	78665703
Metabolic acidosis	5123.91	10.19	4445	567189	78084	79094670
Hypoglycaemia	5047.32	10.19	4828	566806	96766	79075988
Diabetic ketoacidosis	3388.94	10.19	2426	569208	31696	79141058
Blood glucose increased	2177.58	10.19	3350	568284	111625	79061129
Hyperkalaemia	1849.65	10.19	3102	568532	111296	79061458
Euglycaemic diabetic ketoacidosis	1838.29	10.19	924	570710	5920	79166834
Diabetes mellitus inadequate control	1510.10	10.19	1310	570324	22954	79149800
Ketoacidosis	1476.30	10.19	836	570798	7018	79165736

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	A10BA02	ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Biguanides
ATC	A10BD02	ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Combinations of oral blood glucose lowering drugs
ATC	A10BD03	ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Combinations of oral blood glucose lowering drugs
ATC	A10BD05	ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Combinations of oral blood glucose lowering drugs
ATC	A10BD07	ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Combinations of oral blood glucose lowering drugs
ATC	A10BD08	ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Combinations of oral blood glucose lowering drugs
ATC	A10BD10	ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Combinations of oral blood glucose lowering drugs
ATC	A10BD11	ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Combinations of oral blood glucose lowering drugs
ATC	A10BD13	ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Combinations of oral blood glucose lowering drugs
ATC	A10BD14	ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Combinations of oral blood glucose lowering drugs

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Diabetes mellitus type 2	indication	44054006	DOID:9352
Induction of ovulation in polycystic ovarian syndrome	indication	237055002	DOID:11612
Controlled ovarian stimulation	indication	732970000
Treatment Refractory Type 2 Diabetes Mellitus	indication
Gestational diabetes mellitus	off-label use	11687002	DOID:11714
Polycystic ovaries	off-label use	69878008
Weight loss	off-label use	89362005
Polycystic ovary syndrome	off-label use	237055002	DOID:11612
Prevention of Type 2 Diabetes Mellitus	off-label use
Alcoholism	contraindication	7200002

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	12.63	Basic
pKa2	3.34	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
10MG;1GM	XIGDUO XR	ASTRAZENECA AB	N205649	Oct. 29, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	6515117	Oct. 4, 2025	TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG;1GM	XIGDUO XR	ASTRAZENECA AB	N205649	Oct. 29, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	8501698	June 20, 2027	TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG;1GM	XIGDUO XR	ASTRAZENECA AB	N205649	Oct. 29, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	8685934	May 26, 2030	TREATMENT OF TYPE 2 DIABETES MELLITUS IN A PATIENT, WHEREIN GLYCEMIC CONTROL (HBA1C < 7.0%) IS NOT ACHIEVABLE USING ONE OR MORE OF INSULIN, METFORMIN, PIOGLITAZONE, OR ROSIGLITAZONE
10MG;1GM	SYNJARDY XR	BOEHRINGER INGELHEIM	N208658	Dec. 9, 2016	RX	TABLET, EXTENDED RELEASE	ORAL	10596120	March 7, 2032	TREATMENT OF A TREATMENT-NAÏVE PATIENT WITH INADEQUATELY CONTROLLED TYPE 2 DIABETES USING A COMPOSITION COMPRISING AN EXTENDED RELEASE CORE COMPRISING METFORMIN AND AN OUTER COATING COMPRISING EMPAGLIFLOZIN
10MG;1GM	SYNJARDY XR	BOEHRINGER INGELHEIM	N208658	Dec. 9, 2016	RX	TABLET, EXTENDED RELEASE	ORAL	10596120	March 7, 2032	TREATMENT OF A TYPE 2 DIABETES MELLITUS PATIENT WITH INSUFFICIENT GLYCEMIC CONTROL DESPITE METFORMIN THERAPY USING A COMPOSITION COMPRISING AN EXTENDED RELEASE CORE COMPRISING METFORMIN AND AN OUTER COATING COMPRISING EMPAGLIFLOZIN
10MG;1GM	SYNJARDY XR	BOEHRINGER INGELHEIM	N208658	Dec. 9, 2016	RX	TABLET, EXTENDED RELEASE	ORAL	10258637	April 3, 2034	METHOD OF TREATING TYPE 2 DIABETES MELLITUS IN A PATIENT WITH RENAL IMPAIRMENT (45 ML/MIN/1.73 M2<=EGFR<60 ML/MIN/1.73 M2) BY ONCE DAILY ADMINISTRATION OF 10 MG OR 25 MG OF EMPAGLIFLOZIN
10MG;1GM	SYNJARDY XR	BOEHRINGER INGELHEIM	N208658	Dec. 9, 2016	RX	TABLET, EXTENDED RELEASE	ORAL	11090323	April 3, 2034	METHOD OF TREATING TYPE 2 DIABETES MELLITUS IN A PATENT WITH RENAL IMPAIRMENT (EGFR<60 ML/MIN/1.73 M2) BY INITIATION OF EMPAGLIFLOZIN AND METFORMIN HCL IF EGFR>=45 ML/MIN/1.73 M2 AND DISCONTINUATION IF EGFR<30 ML/MIN/1.73 M2
10MG;1GM	SYNJARDY XR	BOEHRINGER INGELHEIM	N208658	Dec. 9, 2016	RX	TABLET, EXTENDED RELEASE	ORAL	9949997	May 17, 2034	METHOD FOR REDUCING THE RISK OF CARDIOVASCULAR DEATH AND HOSPITALIZATION FOR HEART FAILURE IN ADULTS WITH TYPE 2 DIABETES MELLITUS BY ONCE DAILY ADMINISTRATION OF EMPAGLIFLOZIN
10MG;1GM	SYNJARDY XR	BOEHRINGER INGELHEIM	N208658	Dec. 9, 2016	RX	TABLET, EXTENDED RELEASE	ORAL	9949997	May 17, 2034	METHOD FOR REDUCING THE RISK OF CARDIOVASCULAR DEATH IN ADULT PATIENTS WITH TYPE 2 DIABETES MELLITUS AND CARDIOVASCULAR DISEASE BY ONCE DAILY ADMINISTRATION OF 10 MG OR 25 MG OF EMPAGLIFLOZIN
10MG;1GM	SYNJARDY XR	BOEHRINGER INGELHEIM	N208658	Dec. 9, 2016	RX	TABLET, EXTENDED RELEASE	ORAL	9949998	June 11, 2034	METHOD OF TREATING TYPE 2 DIABETES MELLITUS IN A PATIENT WITH RENAL IMPAIRMENT (45 ML/MIN/1.73 M2<=EGFR<60 ML/MIN/1.73 M2) BY ONCE DAILY ADMINISTRATION OF 10 MG OR 25 MG OF EMPAGLIFLOZIN

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
10MG;1GM	SYNJARDY XR	BOEHRINGER INGELHEIM	N208658	Dec. 9, 2016	RX	TABLET, EXTENDED RELEASE	ORAL	June 20, 2026	REVISIONS TO THE LABELING TO INCLUDE RESULTS FROM PROTOCOL 1218- 0091
10MG;1GM	SYNJARDY XR	BOEHRINGER INGELHEIM	N208658	Dec. 9, 2016	RX	TABLET, EXTENDED RELEASE	ORAL	Dec. 20, 2026	PEDIATRIC EXCLUSIVITY
12.5MG;1GM	SYNJARDY	BOEHRINGER INGELHEIM	N206111	Aug. 26, 2015	RX	TABLET	ORAL	June 20, 2026	NEW PATIENT POPULATION
12.5MG;1GM	SYNJARDY XR	BOEHRINGER INGELHEIM	N208658	Dec. 9, 2016	RX	TABLET, EXTENDED RELEASE	ORAL	June 20, 2026	REVISIONS TO THE LABELING TO INCLUDE RESULTS FROM PROTOCOL 1218- 0091
12.5MG;1GM	SYNJARDY	BOEHRINGER INGELHEIM	N206111	Aug. 26, 2015	RX	TABLET	ORAL	Dec. 20, 2026	PEDIATRIC EXCLUSIVITY
12.5MG;1GM	SYNJARDY XR	BOEHRINGER INGELHEIM	N208658	Dec. 9, 2016	RX	TABLET, EXTENDED RELEASE	ORAL	Dec. 20, 2026	PEDIATRIC EXCLUSIVITY
12.5MG;500MG	SYNJARDY	BOEHRINGER INGELHEIM	N206111	Aug. 26, 2015	RX	TABLET	ORAL	June 20, 2026	NEW PATIENT POPULATION
12.5MG;500MG	SYNJARDY	BOEHRINGER INGELHEIM	N206111	Aug. 26, 2015	RX	TABLET	ORAL	Dec. 20, 2026	PEDIATRIC EXCLUSIVITY
1GM;EQ 100MG BASE	JANUMET XR	MERCK SHARP DOHME	N202270	Feb. 2, 2012	RX	TABLET, EXTENDED RELEASE	ORAL	Feb. 12, 2023	PEDIATRIC EXCLUSIVITY
1GM;EQ 50MG BASE	JANUMET	MSD SUB MERCK	N022044	March 30, 2007	RX	TABLET	ORAL	Feb. 12, 2023	PEDIATRIC EXCLUSIVITY

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Mitochondrial complex I (NADH dehydrogenase)	Enzyme	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	NDUS8_HUMAN NDUA4_HUMAN ACPM_HUMAN NDUA1_HUMAN NDUS4_HUMAN NDUB5_HUMAN NDUB3_HUMAN NDUC1_HUMAN NDUA2_HUMAN NDUS5_HUMAN NDUS7_HUMAN NDUS2_HUMAN NDUS6_HUMAN NDUB1_HUMAN NDUS3_HUMAN NDUB6_HUMAN NDUA3_HUMAN NDUB4_HUMAN NDUB8_HUMAN NDUB2_HUMAN NDUA7_HUMAN NDUC2_HUMAN NDUAA_HUMAN NDUBA_HUMAN NU1M_HUMAN NU2M_HUMAN NU3M_HUMAN NU4LM_HUMAN NU4M_HUMAN NU5M_HUMAN NU6M_HUMAN NDUB7_HUMAN NDUV2_HUMAN NDUS1_HUMAN NDUV1_HUMAN NDUA8_HUMAN NDUV3_HUMAN NDUA6_HUMAN NDUA5_HUMAN NDUA9_HUMAN NDUAB_HUMAN MIMIT_HUMAN NDUF3_HUMAN NUA4L_HUMAN NDUBB_HUMAN NDUF4_HUMAN NDUAD_HUMAN NDUAC_HUMAN CIA30_HUMAN NDUB9_HUMAN	INHIBITOR			CHEMBL	CHEMBL
5'-AMP-activated protein kinase subunit beta-1	Kinase	Q9Y478	AAKB1_HUMAN				WOMBAT-PK
Dipeptidyl peptidase 4	Enzyme	P27487	DPP4_HUMAN		IC50	4.54	CHEMBL
Solute carrier family 22 member 1	Transporter	O15245	S22A1_HUMAN		IC50	2.70	WOMBAT-PK
Solute carrier family 22 member 2	Transporter	O15244	S22A2_HUMAN		IC50	3.40	WOMBAT-PK
Solute carrier family 22 member 3	Transporter	O75751	S22A3_HUMAN		Km	2.50	WOMBAT-PK

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External reference:

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ID	Source
MF8	PDB_CHEM_ID
003483	NDDF
004534	NDDF
109081006	SNOMEDCT_US
109083009	SNOMEDCT_US
1115-70-4	SECONDARY_CAS_RN
151827	RXNORM
372567009	SNOMEDCT_US
4020898	VANDF
4023979	VUID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Glipizide and Metformin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	2	0093-7455	TABLET, FILM COATED	250 mg	ORAL	ANDA	27 sections
Glipizide and Metformin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	2	0093-7456	TABLET, FILM COATED	500 mg	ORAL	ANDA	27 sections
Glipizide and Metformin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	2	0093-7457	TABLET, FILM COATED	500 mg	ORAL	ANDA	27 sections
JANUMET	HUMAN PRESCRIPTION DRUG LABEL	2	0006-0575	TABLET, FILM COATED	500 mg	ORAL	NDA	29 sections
JANUMET	HUMAN PRESCRIPTION DRUG LABEL	2	0006-0575	TABLET, FILM COATED	500 mg	ORAL	NDA	29 sections
JANUMET	HUMAN PRESCRIPTION DRUG LABEL	2	0006-0575	TABLET, FILM COATED	500 mg	ORAL	NDA	29 sections
JANUMET	HUMAN PRESCRIPTION DRUG LABEL	2	0006-0577	TABLET, FILM COATED	1000 mg	ORAL	NDA	29 sections
JANUMET	HUMAN PRESCRIPTION DRUG LABEL	2	0006-0577	TABLET, FILM COATED	1000 mg	ORAL	NDA	29 sections
JANUMET	HUMAN PRESCRIPTION DRUG LABEL	2	0006-0577	TABLET, FILM COATED	1000 mg	ORAL	NDA	29 sections
JANUMET XR	HUMAN PRESCRIPTION DRUG LABEL	2	0006-0078	TABLET, FILM COATED, EXTENDED RELEASE	500 mg	ORAL	NDA	30 sections

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