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Metformin

Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

In Vitro Substrates

* denotes drugs that can potentially be used for in vivo (clinical) studies of the designated transporter
Transporter Synonyms Km (μM) Cell System Reference
SLC22A2 OCT2 990 HEK293-OCT2 Kimura, 2005
SLC22A1 OCT1 1470 HEK293-OCT1 Kimura, 2005
SLC47A2 MATE2K 1050 HEK293-MATE2K Masuda, 2006
SLC47A1 MATE1 780 HEK293-MATE1 Tanihara, 2007
SLC47A2 MATE2K 1980 HEK293-MATE2K Tanihara, 2007
SLC22A1 OCT1 1060 HEK293-OCT1 Choi, 2007
SLC22A2 OCT2 1072 HEK293-OCT2 Choi, 2007
SLC22A2 OCT2 3356 HEK293-OCT2 Zolk, 2009
SLC47A1 MATE1 227 HEK293-MATE1 Chen, 2009
SLC22A2 OCT2 3171 HEK293-OCT2 Zolk, 2009
SLC22A1 OCT1 2160 CHO-OCT1 Nies, 2009
SLC22A3 OCT3 2260 CHO-OCT3 Nies, 2009
SLC47A1 MATE1 202 HeLa-MATE1 Meyer, 2010
SLC22A2 OCT2 680 HeLa-OCT2 Meyer, 2010
SLC22A1 OCT1 5450 HEK293-OCT1 Ahlin, 2010
SLC22A2 OCT2 235 OCT2-expressing oocytes Sogame, 2013
SLC22A2 OCT2 518 CHO-OCT2 Severance, 2017
SLC22A1 OCT1 5422 Caco-OCT1 Elsby, 2017
SLC22A2 OCT2 285.2 CHO-OCT2 Sandoval, 2018

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In Vitro Inhibitors

* denotes drugs that can potentially be used for in vivo (clinical) studies of the designated transporter
Transporter Synonyms Inhibitor IC50 (μM) Ki (μM) Substrate used Cell System Reference
SLC22A1 OCT1 Metformin 3420 1-methyl-4-phenylpyridinium (MPP+) CHO-OCT1 Nies, 2009
SLC47A1 MATE1 Metformin 47 1-methyl-4-phenylpyridinium (MPP+) CHO-MATE1 Astorga, 2012
SLC47A2 MATE2K Metformin 89.3 1-methyl-4-phenylpyridinium (MPP+) CHO-MATE2K Astorga, 2012
SLC22A2 OCT2 Metformin 566 1-methyl-4-phenylpyridinium (MPP+) CHO-OCT2 Belzer, 2013
SLC22A2 OCT2 Metformin 223 1-methyl-4-phenylpyridinium (MPP+) CHO-OCT2 Severance, 2017
SLC47A1 MATE1 Metformin 250 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-MATE1 Wittwer, 2013
ABCC2 MRP2, cMOAT Metformin >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC3 MRP3 Metformin >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC4 MRP4 Metformin >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
SLC22A5 OCTN2 Metformin 2050 L-carnitine MDCKII-hOCTN2 Diao, 2010
SLC22A1 OCT1 Metformin 1231 N-methylpyridinium OCT1-expressing oocytes Bourdet, 2005
SLC22A2 OCT2 Metformin 521 N-methylpyridinium OCT2-expressing oocytes Bourdet, 2005
SLC22A3 OCT3 Metformin 2332 N-methylpyridinium OCT3-expressing oocytes Bourdet, 2005
SLC22A1 OCT1 Metformin 493 N-methylpyridinium HEK293-OCT1 Umehara, 2007
SLC22A2 OCT2 Metformin 289 N-methylpyridinium HEK293-OCT2 Umehara, 2007
SLC22A3 OCT3 Metformin 904 N-methylpyridinium HEK293-OCT3 Umehara, 2007
SLC22A2 OCT2 Metformin 398 N-methylpyridinium HEK293-OCT2 Zolk, 2009
SLC22A2 OCT2 Metformin 1180 NBD-MTMA CHO-OCT2 Belzer, 2013
SLC22A2 OCT2 Metformin 125.6 Para-Aminosalicylic acid (PAS) HEK293-OCT2 Parvez, 2017
ABCB11 BSEP Metformin >133 Taurocholate Sf9 cell membrane vesicles Morgan, 2013
SLC22A1 OCT1 Metformin 2820 Tetraethylammonium HEK293-OCT1 Umehara, 2007
SLC22A2 OCT2 Metformin 1380 Tetraethylammonium HEK293-OCT2 Umehara, 2007
SLC47A1 MATE1 Metformin 666.9 Tetraethylammonium HEK293-MATE1 Tsuda, 2009
SLC47A2 MATE2K Metformin 6515.7 Tetraethylammonium HEK293-MATE2 Tsuda, 2009

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Clinical Drug-Drug Interactions

DDI Implicated Transporter* Interacting Drug Affected Drug AUC Cmax CLR CL/F t1/2 Effect on PD Reference More Details
Clinical PK Impact(fold change)
1 OCT2/MATEs Abemaciclib Metformin 1.37 1.22 0.55 ND NS yes Chappell, 2019 DDI 1
2 OCTs/MATE2K Cefiderocol Metformin 1.05 1.09 ND NR 0.88 ND Katsube, 2018 DDI 2
3 OCTs/MATEs Cimetidine Metformin 1.5 1.7 0.7 ND ND ND Somogyi, 1987 DDI 3
4 OCT2 Dolutegravir (q12h) Metformin 2.45 2.11 ND 0.409 1.114 Song, 2016 DDI 4
5 OCT2 Dolutegravir (q24h) Metformin 1.79 1.66 ND 0.559 1.09 Song, 2016 DDI 5
6 OCTs/MATEs Isavuconazole Metformin 1.52 1.22 ND 0.66 1.14 ND Yamazaki, 2017 DDI 6
7 OCTs/MATEs Plazomicin Metformin 1.04 1.1 0.99 0.97 0.92 Choi, 2019 DDI 7
8 MATEs Pyrimethamine Metformin 1.4 1.4 0.6 ND ND ND Kusuhara, 2011 DDI 8
9 OCTs Rifampin Metformin 1.13 1.10 1.16 NR 0.92 Yes Cho, 2011 DDI 9
10 OCT1 St John's wort Metformin 1.03 1.04 0.97 1.01 0.89 Yes Stage, 2015 DDI 10
11 OCTs/MATEs Test cocktail 1: digoxin, furosemide, metformin, and rosuvastatin Metformin 0.99 1.1 Stopfer, 2016 DDI 11
12 OCTs/MATEs Test cocktail 3: digoxin, metformin, rosuvastatin, and increased furosemide Metformin 1.03 1.03 Stopfer, 2016 DDI 12
13 OCT2 Vandetanib Metformin 1.74 1.5 0.48 0.58 1.06 Johansson, 2014 DDI 13
14 OCT1/MATEs Verapamil Metformin 1.07 1.09 0.98 NR 0.80 Yes Cho, 2014 DDI 14

PK = pharmacokinetic
The transporters are implicated by in vitro data and/or studies in humans with genetic polymorphisms of the transporter
DDI = Drug Drug Interaction
PD = pharmacodynamic
ND = not determined
NS = not significant
N/A = information not available
Calculation of Fold Change: fold change in the presence of the interacting drug = (value with interacting drug)/(value without interacting drug)
fold change > 1: increase in pharmacokinetic value
fold change < 1: decrease in pharmacokinetic value


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