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Cimetidine

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
SLC22A8 OAT3 57.4 OAT3-expressing oocytes Cha, 2001
SLC22A2 OCT2 72.6 HEK293-OCT2 Tahara, 2005
SLC22A8 OAT3 113 HEK293-OAT3 Tahara, 2006
SLC47A2 MATE2K 370 HEK293-MATE2K Masuda, 2006
SLC22A8 OAT3 174 CHO-OAT3 Chu, 2007
SLC47A2 MATE2K 120 HEK293-MATE2K Tanihara, 2007
SLC47A1 MATE1 170 HEK293-MATE1 Tanihara, 2007
SLC22A2 OCT2 20.8 CHO-OCT2 Severance, 2017
SLC22A2 OCT2 15.1 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
SLC22A2 OCT2 Cimetidine 146 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT2 Ito, 2012
SLC22A2 OCT2 Cimetidine 171 1-methyl-4-phenylpyridinium (MPP+) CHO-OCT2 Belzer, 2013
SLC22A2 OCT2 Cimetidine 113 1-methyl-4-phenylpyridinium (MPP+) CHO-OCT2 Severance, 2017
SLC22A1 OCT1 Cimetidine >100 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Kido, 2011
SLC47A1 MATE1 Cimetidine 5.7 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-MATE1 Kido, 2011
SLC47A2 MATE2K Cimetidine 39 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-MATE2K Kido, 2011
SLC22A2 OCT2 Cimetidine 104 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT2 Ito, 2012
SLC47A1 MATE1 Cimetidine 1.2 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-MATE1 Wittwer, 2013
ABCB1 MDR1, P-gp Cimetidine >50 Calcein AM MDR1 expressing LLC-PK1 cells Schwab, 2003
mouse_Abcb1a Mdr, Pgp, Pgy, Mdr3, P-gp, Abcb4, Mdr1a Cimetidine >50 Calcein AM Mouse mdr1a expressing LLC-PK1 cells Schwab, 2003
mouse_Abcb1b mdr, Mdr1, Pgy1, Abcb1, Mdr1b, Pgy-1 Cimetidine >50 Calcein AM Mouse mdr1b expressing LLC-PK1 cells Schwab, 2003
ABCC2 MRP2, cMOAT Cimetidine >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC3 MRP3 Cimetidine >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC4 MRP4 Cimetidine >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
SLC22A1 OCT1 Cimetidine 2830 Ethidium CHO-OCT1 Lee, 2009
SLC22A2 OCT2 Cimetidine 95 m-iodobenzylguanidine (MIBG) HEK293-OCT2 Ito, 2012
SLC22A2 OCT2 Cimetidine 124 Metformin HEK293-OCT2 Ito, 2012
SLC47A1 MATE1 Cimetidine 3.8 Metformin HEK293-MATE1 Ito, 2012
SLC22A2 OCT2 Cimetidine 25.4 Metformin CHO-OCT2 Belzer, 2013
SLC47A1 MATE1 Cimetidine 2.56 Metformin HEK293-MATE1 Lechner, 2016
SLC47A2 MATE2K Cimetidine 5.47 Metformin HEK293-MATE2K Lechner, 2016
SLC22A1 OCT1 Cimetidine 275 Metformin Caco-OCT1 Elsby, 2017
SLC22A2 OCT2 Cimetidine 120 N-methylpyridinium HEK293-OCT2 Zolk, 2009
SLC22A2 OCT2 Cimetidine 70.4 NBD-MTMA CHO-OCT2 Belzer, 2013
SLC22A2 OCT2 Cimetidine 111.5 Para-Aminosalicylic acid (PAS) HEK293-OCT2 Parvez, 2017
SLC22A8 OAT3 Cimetidine 79 Sitagliptin CHO-OAT3 Chu, 2007
ABCB11 BSEP Cimetidine >133 Taurocholate Sf9 cell membrane vesicles Morgan, 2013
SLC22A2 OCT2 Cimetidine 373 Tetraethylammonium OCT2-expressing oocytes Okuda, 1999
SLC22A4 OCTN1 Cimetidine 1500 Tetraethylammonium HRPE-rOCTN1 Wu, 2000
SLC22A4 OCTN1 Cimetidine 434.8 Tetraethylammonium HEK293-hOCTN1 Peltekova, 2004
SLC47A1 MATE1 Cimetidine 1.1 Tetraethylammonium HEK293-MATE1 Tsuda, 2009
SLC47A2 MATE2K Cimetidine 7.3 Tetraethylammonium HEK293-MATE2 Tsuda, 2009
SLC22A2 OCT2 Cimetidine 144 Tetraethylammonium HEK293-OCT2 Ito, 2012
SLC47A2 MATE2K Cimetidine 2.1 Tetraethylammonium HEK293-MATE2K Ito, 2012
ABCB1 MDR1, P-gp Cimetidine 6500 Verapamil Caco-2 cells Doppenshmitt, 1998
SLC22A1 OCT1 Cimetidine 149 YM155 HEK293-OCT1 Minematsu, 2010
SLC22A2 OCT2 Cimetidine 110 YM155 HEK293-OCT2 Minematsu, 2010

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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 OCTs/MATEs Cimetidine Cephalexin NS NS 0.8 0.8 NS ND van, 1986 DDI 1
2 OCTs/MATEs Cimetidine Dofetilide 1.5 1.3 0.7 0.7 1.3 yes Abel, 2000 DDI 2
3 OCT2/MATE1 Cimetidine Glycopyrronium 1.22 NS 0.77 Dumitras, 2013 DDI 3
4 OCT2 Cimetidine Lucerastat 1.22 NS Boof, 2020 DDI 4
5 OCTs/MATEs Cimetidine Metformin 1.5 1.7 0.7 ND ND ND Somogyi, 1987 DDI 5
6 OCTs/MATEs Cimetidine Pilsicainide 1.3 NS 0.7 0.7 1.2 ND Shiga, 2000 DDI 6
7 OCTs/MATEs Cimetidine Pindolol (S-enantiomer) 1.4 1.3 0.7 ND NS ND Somogyi, 1992 DDI 7
8 OCTs/MATEs Cimetidine Procainamide 1.4 NS 0.6 ND 1.3 ND Somogyi, 1983 DDI 8
9 OCTs/MATEs Cimetidine Ranitidine 1.3 NS 0.7 ND 1.3 ND van, 1986 DDI 9
10 OCTs/MATEs Cimetidine Varenicline 1.3 ND 0.8 0.8 ND ND Feng, 2008 DDI 10

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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