Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DM89QE1)

Drug Name
Metformin Drug Info
Synonyms
657-24-9; 1,1-Dimethylbiguanide; N,N-dimethylimidodicarbonimidic diamide; Metiguanide; Dimethylbiguanide; Glucophage; Haurymelin; Gliguanid; Fluamine; Glumetza; Flumamine; Melbin; Diabex; N,N-Dimethylbiguanide; Metformina; Metforminum; Metformine; Islotin; Glifage; Siofor; N1,N1-Dimethylbiguanide; DMGG; NNDG; Dimethyldiguanide; N,N-Dimethyldiguanide; Metformina [DCIT]; Imidodicarbonimidic diamide, N,N-dimethyl-; Metformina [Spanish]; Metforminum [INN-Latin]; Metformine [INN-French]; Metformin [USAN:INN:BAN]; 1,1-Dimethyl; Diabetosan; Dimethylbiguanidine; Dimethylguanylguanidine; Glycon; Diabex (TN); Diaformin (TN); Dianben (TN); Fortamet (TN); Gen-Metformin; Glucophage (TN); Glumetza (TN); LA-6023; Nu-Metformin; Obimet (TN); Riomet (TN); Metformin (USAN/INN); 1,1-Dimethyl biguanide; 3-(diaminomethylidene)-1,1-dimethylguanidine; [14C]metformin
Indication
Disease Entry ICD 11 Status REF
Colorectal carcinoma Approved [1]
Non-insulin dependent diabetes 5A11 Approved [1]
Ovarian serous cystadenocarcinoma Approved [1]
Prostate carcinoma Approved [1]
Type-2 diabetes 5A11 Approved [2]
Coronavirus Disease 2019 (COVID-19) 1D6Y Investigative [3]
Therapeutic Class
Hypoglycemic Agents
Cross-matching ID
PubChem CID
4091
ChEBI ID
CHEBI:6801
CAS Number
CAS 657-24-9
TTD Drug ID
DM89QE1
VARIDT Drug ID
DR00133
ACDINA Drug ID
D00405

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
Drug Status:
Clinical Trial Drug(s)
Discontinued Drug(s)
Investigative Drug(s)
Approved Drug(s)
Preclinical Drug(s)
Download the Complete Related Drug List
Drug(s) Targeting Acetyl-CoA carboxylase 2 (ACACB)
Drug Name Drug ID Indication ICD 11 Highest Status REF
PF-05175157 DMLQ3OK Type-2 diabetes 5A11 Phase 2 [13]
Axokine DMT5O8I Obesity 5B81 Discontinued in Phase 3 [14]
CP-640186 DMO0PS9 Discovery agent N.A. Investigative [15]
A-80040 DML20N9 Discovery agent N.A. Investigative [16]
AC-8632 DM09BJ4 Parkinson disease 8A00.0 Investigative [13]
QLT-091382 DMWOSFJ Sebaceous gland disease EM0Z Investigative [13]
2-[4-(2,4-Dichlorophenoxy)Phenoxy]Propanoic Acid DMWXI06 Discovery agent N.A. Investigative [17]
Soraphen A DM18IKZ Discovery agent N.A. Investigative [18]
⏷ Show the Full List of 8 Drug(s)
Drug(s) Targeting Solute carrier family 47 member 1 (SLC47A1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
[14C]TEA DM6SFYH Discovery agent N.A. Investigative [5]
Drug(s) Transported By Breast cancer resistance protein (ABCG2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [19]
Methotrexate DM2TEOL Anterior urethra cancer Approved [20]
Folic Acid DMEMBJC Colorectal carcinoma Approved [21]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [22]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [23]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [24]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [25]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [24]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [26]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [27]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Transported By Organic cation transporter 2 (SLC22A2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [28]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [29]
Oxaliplatin DMQNWRD Adenocarcinoma 2D40 Approved [30]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [31]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [32]
Propranolol DM79NTF Angina pectoris BA40 Approved [33]
Ergotidine DM78IME Osteoarthritis FA00-FA05 Approved [34]
Clonidine DM6RZ9Q Attention deficit hyperactivity disorder 6A05.Z Approved [33]
Ranitidine DM0GUSX Gastric ulcer DA60 Approved [35]
Cimetidine DMH61ZB Acid-reflux disorder DA22 Approved [36]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Transported By Multidrug and toxin extrusion protein 1 (SLC47A1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Aciclovir DMYLOVR Genital herpes 1A94 Approved [10]
Ganciclovir DM1MBYQ Cytomegalovirus infection 1D82 Approved [10]
Cimetidine DMH61ZB Acid-reflux disorder DA22 Approved [10]
Chloroquine DMSI5CB Malaria 1F40-1F45 Approved [37]
Procainamide DMNMXR8 Ventricular arrhythmias BC71 Approved [10]
Topotecan DMP6G8T Central nervous system neoplasm Approved [10]
Cephalexin DMD5JU8 Acute otitis media AB00 Approved [38]
LY2835219 DM93VBZ Breast cancer 2C60-2C65 Approved [39]
Dofetilide DMPN1TW Sinus rhythm disorder BC9Y Approved [40]
Pyrimethamine DM5X7VY Malaria 1F40-1F45 Approved [41]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Transported By Organic cation transporter 3 (SLC22A3)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Propranolol DM79NTF Angina pectoris BA40 Approved [33]
Ergotidine DM78IME Osteoarthritis FA00-FA05 Approved [32]
Clonidine DM6RZ9Q Attention deficit hyperactivity disorder 6A05.Z Approved [33]
Entecavir DM7VTQO Hepatitis B virus infection 1E51.0 Approved [42]
Epinephrine DM3KJBC Acute asthma CA23 Approved [32]
Norepinephrine DMOUC09 Alopecia ED70 Approved [32]
Amphetamine DMSZQAK Attention deficit hyperactivity disorder 6A05.Z Approved [43]
Acetylcholine DMDF79Z Cataract 9B10 Approved [44]
Sodium chloride DMM3950 Skin burns ME65.0 Approved [45]
Etilefrine DM67PWD Cardiovascular disease BA00-BE2Z Withdrawn from market [46]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Transported By Organic cation transporter 1 (SLC22A1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [28]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [47]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [48]
Oxaliplatin DMQNWRD Adenocarcinoma 2D40 Approved [49]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [50]
Verapamil DMA7PEW Angina pectoris BA40 Approved [51]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [52]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [53]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [54]
Propranolol DM79NTF Angina pectoris BA40 Approved [33]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Transported By Multidrug and toxin extrusion protein 2 (SLC47A2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Aciclovir DMYLOVR Genital herpes 1A94 Approved [10]
Ganciclovir DM1MBYQ Cytomegalovirus infection 1D82 Approved [10]
Cimetidine DMH61ZB Acid-reflux disorder DA22 Approved [10]
Procainamide DMNMXR8 Ventricular arrhythmias BC71 Approved [10]
Topotecan DMP6G8T Central nervous system neoplasm Approved [10]
LY2835219 DM93VBZ Breast cancer 2C60-2C65 Approved [39]
Dofetilide DMPN1TW Sinus rhythm disorder BC9Y Approved [40]
Estrone sulfate DMVBIZL Atrophic vaginitis GA30.2 Approved [10]
N-methylpyridinium DMVUKEW N. A. N. A. Preclinical [10]
[14C]TEA DM6SFYH Discovery agent N.A. Investigative [10]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Transported By Thiamine transporter 2 (SLC19A3)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Vitamin B1 DMZ1WXJ Vitamin B1 deficiency 5B5A Approved [55]
Drug(s) Transported By Equilibrative nucleoside transporter 4 (SLC29A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ergotidine DM78IME Osteoarthritis FA00-FA05 Approved [56]
SEROTONIN DMOFCRY Discovery agent N.A. Investigative [57]

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas
Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Acetyl-CoA carboxylase 2 (ACACB) TTY84UG ACACB_HUMAN Activator [4]
Solute carrier family 47 member 1 (SLC47A1) TTMHCGA S47A1_HUMAN Modulator [5]
HUMAN mannose receptor (MRC1) TTKV8W5 MRC1_HUMAN Inhibitor [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Equilibrative nucleoside transporter 4 (SLC29A4) DT3EAQP S29A4_HUMAN Substrate [6]
Thiamine transporter 1 (SLC19A2) DTLA4Q2 S19A2_HUMAN Substrate [7]
Thiamine transporter 2 (SLC19A3) DT39CEA S19A3_HUMAN Substrate [7]
Organic cation transporter 3 (SLC22A3) DT6201N S22A3_HUMAN Substrate [8]
Organic cation transporter 1 (SLC22A1) DTT79CX S22A1_HUMAN Substrate [9]
Multidrug and toxin extrusion protein 2 (SLC47A2) DT3TX4H S47A2_HUMAN Substrate [10]
Multidrug and toxin extrusion protein 1 (SLC47A1) DTZGT0P S47A1_HUMAN Substrate [11]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [12]
Organic cation transporter 2 (SLC22A2) DT9IDPW S22A2_HUMAN Substrate [9]

References

1 Metformin FDA Label
2 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
3 A SARS-CoV-2-Human Protein-Protein Interaction Map Reveals Drug Targets and Potential Drug-Repurposing. March 2020
4 AMP-activated protein kinase-dependent and -independent mechanisms underlying in vitro antiglioma action of compound C. Biochem Pharmacol. 2009 Jun 1;77(11):1684-93.
5 Molecular cloning, functional characterization and tissue distribution of rat H+/organic cation antiporter MATE1. Pharm Res. 2006 Aug;23(8):1696-701.
6 Metformin: from mechanisms of action to therapies. Cell Metab. 2014 Dec 2;20(6):953-66.
7 Metformin Is a Substrate and Inhibitor of the Human Thiamine Transporter, THTR-2 (SLC19A3). Mol Pharm. 2015 Dec 7;12(12):4301-10.
8 Expression of organic cation transporters OCT1 (SLC22A1) and OCT3 (SLC22A3) is affected by genetic factors and cholestasis in human liver. Hepatology. 2009 Oct;50(4):1227-40.
9 Metformin is a superior substrate for renal organic cation transporter OCT2 rather than hepatic OCT1. Drug Metab Pharmacokinet. 2005 Oct;20(5):379-86.
10 Substrate specificity of MATE1 and MATE2-K, human multidrug and toxin extrusions/H(+)-organic cation antiporters. Biochem Pharmacol. 2007 Jul 15;74(2):359-71.
11 Human multidrug and toxin extrusion 1 (MATE1/SLC47A1) transporter: functional characterization, interaction with OCT2 (SLC22A2), and single nucleotide polymorphisms. Am J Physiol Renal Physiol. 2010 Apr;298(4):F997-F1005.
12 Role of human placental apical membrane transporters in the efflux of glyburide, rosiglitazone, and metformin. Am J Obstet Gynecol. 2010 Apr;202(4):383.e1-7.
13 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1264).
14 Obesity: pathophysiology and clinical management. Curr Med Chem. 2009;16(4):506-21.
15 (4-Piperidinyl)-piperazine: a new platform for acetyl-CoA carboxylase inhibitors. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6645-8.
16 Synthesis and structure-activity relationships of N-{3-[2-(4-alkoxyphenoxy)thiazol-5-yl]-1- methylprop-2-ynyl}carboxy derivatives as selective acet... J Med Chem. 2006 Jun 29;49(13):3770-3.
17 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
18 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
19 Doxorubicin transport by RALBP1 and ABCG2 in lung and breast cancer. Int J Oncol. 2007 Mar;30(3):717-25.
20 Wild-type breast cancer resistance protein (BCRP/ABCG2) is a methotrexate polyglutamate transporter. Cancer Res. 2003 Sep 1;63(17):5538-43.
21 The effect of low pH on breast cancer resistance protein (ABCG2)-mediated transport of methotrexate, 7-hydroxymethotrexate, methotrexate diglutamate, folic acid, mitoxantrone, topotecan, and resveratrol in in vitro drug transport models. Mol Pharmacol. 2007 Jan;71(1):240-9.
22 Role of BCRP as a biomarker for predicting resistance to 5-fluorouracil in breast cancer. Cancer Chemother Pharmacol. 2009 May;63(6):1103-10.
23 Inhibiting the function of ABCB1 and ABCG2 by the EGFR tyrosine kinase inhibitor AG1478. Biochem Pharmacol. 2009 Mar 1;77(5):781-93.
24 Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. J Biol Chem. 2003 Jun 6;278(23):20645-51.
25 The phytoestrogen genistein enhances multidrug resistance in breast cancer cell lines by translational regulation of ABC transporters. Cancer Lett. 2016 Jun 28;376(1):165-72.
26 Curcumin inhibits the activity of ABCG2/BCRP1, a multidrug resistance-linked ABC drug transporter in mice. Pharm Res. 2009 Feb;26(2):480-7.
27 Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. Blood. 2004 Nov 1;104(9):2940-2.
28 Are organic cation transporters capable of transporting prostaglandins? Naunyn Schmiedebergs Arch Pharmacol. 2005 Aug;372(2):125-30.
29 Cisplatin nephrotoxicity is critically mediated via the human organic cation transporter 2. Am J Pathol. 2005 Dec;167(6):1477-84.
30 Relevance of copper transporter 1 and organic cation transporters 1-3 for oxaliplatin uptake and drug resistance in colorectal cancer cells. Metallomics. 2018 Mar 1;10(3):414-425.
31 Cloning and characterization of two human polyspecific organic cation transporters. DNA Cell Biol. 1997 Jul;16(7):871-81.
32 Differential pharmacological in vitro properties of organic cation transporters and regional distribution in rat brain. Neuropharmacology. 2006 Jun;50(8):941-52.
33 Influx Transport of Cationic Drug at the Blood-Retinal Barrier: Impact on the Retinal Delivery of Neuroprotectants. Biol Pharm Bull. 2017;40(8):1139-1145.
34 The organic cation transporters (OCT1, OCT2, EMT) and the plasma membrane monoamine transporter (PMAT) show differential distribution and cyclic expression pattern in human endometrium and early pregnancy decidua. Mol Reprod Dev. 2007 Oct;74(10):1303-11.
35 A species difference in the transport activities of H2 receptor antagonists by rat and human renal organic anion and cation transporters. J Pharmacol Exp Ther. 2005 Oct;315(1):337-45.
36 Elevated systemic elimination of cimetidine in rats with acute biliary obstruction: the role of renal organic cation transporter OCT2. Drug Metab Pharmacokinet. 2010;25(4):328-34.
37 Molecular mechanism of renal tubular secretion of the antimalarial drug chloroquine. Antimicrob Agents Chemother. 2011 Jul;55(7):3091-8.
38 Reduced renal clearance of a zwitterionic substrate cephalexin in MATE1-deficient mice. J Pharmacol Exp Ther. 2010 Aug;334(2):651-6.
39 Abemaciclib Inhibits Renal Tubular Secretion Without Changing Glomerular Filtration Rate. Clin Pharmacol Ther. 2019 May;105(5):1187-1195.
40 FDA Drug Development and Drug Interactions
41 Expression of Organic Anion Transporter 1 or 3 in Human Kidney Proximal Tubule Cells Reduces Cisplatin Sensitivity. Drug Metab Dispos. 2018 May;46(5):592-599.
42 Multiple SLC and ABC Transporters Contribute to the Placental Transfer of Entecavir. Drug Metab Dispos. 2017 Mar;45(3):269-278.
43 Interaction of organic cation transporter 3 (SLC22A3) and amphetamine. J Neurochem. 2010 Jul;114(1):142-9.
44 Organic cation transporters: physiology, toxicology and special focus on ethidium as a novel substrate. Curr Drug Metab. 2009 Jul;10(6):617-31.
45 Organic cation transporter 3 (Slc22a3) is implicated in salt-intake regulation. J Neurosci. 2004 Mar 17;24(11):2846-51.
46 Drug specificity and intestinal membrane localization of human organic cation transporters (OCT). Biochem Pharmacol. 2005 Dec 5;70(12):1851-60.
47 Cisplatin and oxaliplatin, but not carboplatin and nedaplatin, are substrates for human organic cation transporters (SLC22A1-3 and multidrug and toxin extrusion family). J Pharmacol Exp Ther. 2006 Nov;319(2):879-86.
48 Pharmacologic markers and predictors of responses to imatinib therapy in patients with chronic myeloid leukemia. Leuk Lymphoma. 2008 Apr;49(4):639-42.
49 Organic cation transporters are determinants of oxaliplatin cytotoxicity. Cancer Res. 2006 Sep 1;66(17):8847-57.
50 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
51 Implications of genetic polymorphisms in drug transporters for pharmacotherapy. Cancer Lett. 2006 Mar 8;234(1):4-33.
52 Upregulation of histone acetylation reverses organic anion transporter 2 repression and enhances 5-fluorouracil sensitivity in hepatocellular carcinoma
53 Comparison of type I and type II organic cation transport by organic cation transporters and organic anion-transporting polypeptides. J Pharmacol Exp Ther. 2001 Jul;298(1):110-5.
54 Organic cation transporters and their pharmacokinetic and pharmacodynamic consequences. Drug Metab Pharmacokinet. 2008;23(4):243-53.
55 Folate and thiamine transporters mediated by facilitative carriers (SLC19A1-3 and SLC46A1) and folate receptors. Mol Aspects Med. 2013 Apr-Jun;34(2-3):373-85.
56 Histamine uptake mediated by plasma membrane monoamine transporter and organic cation transporters in rat mast cell lines. Eur J Pharmacol. 2019 Apr 15;849:75-83.
57 Autism spectrum disorder associated with low serotonin in CSF and mutations in the SLC29A4 plasma membrane monoamine transporter (PMAT) gene. Mol Autism. 2014 Aug 13;5:43.