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Trimethoprim

Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

In Vitro Substrates

No substrate information.

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	Trimethoprim	20		1-methyl-4-phenylpyridinium (MPP+)	HEK293-OCT1	Jung, 2008
SLC47A1	MATE1	Trimethoprim	9.7		1-methyl-4-phenylpyridinium (MPP+)	CHO-MATE1	Astorga, 2012
SLC47A2	MATE2K	Trimethoprim	2.61		1-methyl-4-phenylpyridinium (MPP+)	CHO-MATE2K	Astorga, 2012
SLC22A2	OCT2	Trimethoprim	775		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Belzer, 2013
SLC22A2	OCT2	Trimethoprim	199.2		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Sandoval, 2018
SLC22A1	OCT1	Trimethoprim	56.8		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT1	Ahlin, 2008
SLC22A1	OCT1	Trimethoprim	50.68		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT1	Chen, 2017
SLC22A2	OCT2	Trimethoprim	14.1		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	CHO-OCT2	Sandoval, 2018
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Trimethoprim		>100	Estradiol-17beta-glucuronide	HEK-OATP1B1	Yoshida, 2012
ABCC2	MRP2, cMOAT	Trimethoprim	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Trimethoprim	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Trimethoprim	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A1	OCT1	Trimethoprim	27.7		Metformin	Caco-OCT1	Elsby, 2017
SLC22A2	OCT2	Trimethoprim	19.8		Metformin	CHO-OCT2	Sandoval, 2018
SLC22A2	OCT2	Trimethoprim	1318		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
SLC22A2	OCT2	Trimethoprim	113		NBD-MTMA	CHO-OCT2	Belzer, 2013
SLC22A2	OCT2	Trimethoprim	43		NBD-MTMA	CHO-OCT2	Sandoval, 2018
ABCB11	BSEP	Trimethoprim	>133		Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A2	OCT2	Trimethoprim	50.2		Tetraethylammonium	CHO-OCT2	Sandoval, 2018

Clinical Drug-Drug Interactions

DDI	Implicated Transporter*	Interacting Drug	Affected Drug	AUC	Cmax	CLR	CL/F	t1/2	Effect on PD	Reference	More Details
DDI	Implicated Transporter*	Interacting Drug	Affected Drug	Clinical PK Impact(fold change)					Effect on PD	Reference	More Details
1	OCTs	Trimethoprim	Zidovudine	NS	ND	0.5	NS	NS	ND	Chatton, 1992	DDI 1

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