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Probenecid

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
ABCC5	MRP5	Probenecid	70		5-fluorodeoxyuridine monophosphate	MRP5-expressing HEK293 vesicles	Pratt, 2005
SLC22A6	OAT1	Probenecid	6.3		6-carboxyfluorescein	CHO-OAT1	Cihlar, 2000
SLC22A8	OAT3	Probenecid	1.25		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
SLC22A6	OAT1	Probenecid	7.74		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
ABCC4	MRP4	Probenecid	2300		9-(2-phosphonomethoxyethyl)adenine (PMEA)	MRP4-expressing HEK293 vesicles	Reid, 2003
ABCC5	MRP5	Probenecid	200		9-(2-phosphonomethoxyethyl)adenine (PMEA)	MRP4-expressing HEK293 vesicles	Reid, 2003
SLC22A6	OAT1	Probenecid	7.4		Adefovir	CHO-OAT1	Mulato, 2000
SLC22A8	OAT3	Probenecid	14.4		Amoxicillin	HEK293-OAT3	Parvez, 2018
SLC22A8	OAT3	Probenecid	4.41		Baricitinib	HEK-PEAK-OAT3	Posada, 2017
ABCC5	MRP5	Probenecid	34		Carboxydichlorofluorescein	MRP5-expressing HEK293 vesicles	Pratt, 2006
ABCC4	MRP4	Probenecid	~100		Cholyltaurine	MRP4-expressing V79 vesicles	Rius, 2003
SLC22A6	OAT1	Probenecid	3.9		Cidofovir	CHO-OAT1	Chu, 2007
SLC22A8	OAT3	Probenecid	3.1		Cimetidine	CHO-OAT3	Chu, 2007
ABCC4	MRP4	Probenecid	<100		Cyclic GMP	MRP4-expressing Sf9 vesicles	van, 2002
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Probenecid		39.8	Dichlorofluorescein	HEK-OATP1B1	Izumi, 2016
SLC22A6	OAT1	Probenecid		26	Dimesna	HeLa-OAT1	Cutler, 2012
SLC22A8	OAT3	Probenecid		32	Dimesna	HeLa-OAT3	Cutler, 2012
ABCC2	MRP2, cMOAT	Probenecid	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Probenecid	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Probenecid	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A8	OAT3	Probenecid		9	Estrone sulfate	S2-OAT3	Takeda, 2001
SLC22A8	OAT3	Probenecid		1.3	Fexofenadine	HEK293-OAT3	Tahara, 2006
SLCO1B3	OATP1B3, OATP8	Probenecid		130	Fexofenadine	HEK293-OATP1B3	Tahara, 2006
SLC22A6	OAT1	Probenecid	7.1		Hydrochlorothiazide	HEK293-OAT1	Yin, 2019
SLC22A8	OAT3	Probenecid	5.8		Hydrochlorothiazide	HEK293-OAT3	Yin, 2019
SLC22A8	OAT3	Probenecid	12.5		Isoniazid	HEK293-OAT3	Parvez, 2018
SLC22A6	OAT1	Probenecid	17		Methotrexate	OAT1-expressing oocytes	Elsby, 2011
ABCC6	MRP6	Probenecid	ND		N-ethylmaleimide S-glutathione	MRP6-expressing Sf9 vesicles	Ilias, 2002
SLC22A6	OAT1	Probenecid		4.29	Ochratoxin A	S2-OAT1	Jung, 2001
SLC22A8	OAT3	Probenecid		4.41	Ochratoxin A	S2-OAT3	Jung, 2001
SLC22A11	OAT4	Probenecid		44.4	Ochratoxin A	S2-OAT4	Babu, 2002
SLC22A6	OAT1	Probenecid	6.5		Para-aminohippurate	CHO-OAT1	Ho, 2000
SLC22A6	OAT1	Probenecid		12.1	Para-aminohippurate	S2-OAT1	Takeda, 2001
SLC22A6	OAT1	Probenecid	17		Para-aminohippurate	OAT1-expressing oocytes	Elsby, 2011
SLC22A6	OAT1	Probenecid	16.3		Para-Aminosalicylic acid (PAS)	HEK293-OAT1	Parvez, 2017
SLC22A8	OAT3	Probenecid	24.6		Para-Aminosalicylic acid (PAS)	HEK293-OAT3	Parvez, 2017
SLC22A11	OAT4	Probenecid		54.9	Prostaglandin F2-alpha	S2-OAT4	Enomoto, 2002
SLC22A7	OAT2	Probenecid		766	Prostaglandin F2-alpha	S2-OAT2	Enomoto, 2002
SLC22A8	OAT3	Probenecid	1.9		Relebactam	MDCKII-OAT3	Chan, 2019
ABCC2	MRP2, cMOAT	Probenecid		42.2	S-(2,4-dinitrophenyl)-glutathione	Liver canalicular membrane vesicles	Horikawa, 2002
SLC22A8	OAT3	Probenecid	5.6		Sitagliptin	CHO-OAT3	Chu, 2007
ABCB11	BSEP	Probenecid	>133		Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A12	URAT1	Probenecid	~50		Uric acid	HEK293-URAT1	Yu, 2007

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	OATs	Probenecid	Acyclovir	1.4	ND	0.7	NS	ND	ND	Laskin, 1982	DDI 1
2	OATs	Probenecid	Baricitinib	2.03	1.03	0.31	0.49	1.63	ND	Posada, 2017	DDI 2
3	OATs	Probenecid	Cefaclor	2.1	1.5	ND	ND	1.6	ND	Welling, 1979	DDI 3
4	MRPs	Probenecid	Cefmetazole	1.6	NS	0.6	0.6	1.5	ND	Ko, 1989	DDI 4
5	OATs	Probenecid	Cefonicid	2.1	1.2	0.3	ND	1.5	ND	Pitkin, 1981	DDI 5
6	OATs	Probenecid	Cefoxitin	2.4	ND	0.4	ND	2.0	ND	Vlasses, 1980	DDI 6
7	OATs	Probenecid	Ceftriaxone	0.7	ND	ND	1.3	0.8	ND	Stoeckel, 1988	DDI 7
8	OATs	Probenecid	Cephradine	2.4	1.9	ND	ND	1.5	ND	Welling, 1979	DDI 8
9	OATs	Probenecid	Cidofovir	ND	ND	0.5	0.6	ND	ND	Cundy, 1995	DDI 9
10	OATs/MRPs	Probenecid	Ciprofloxacin	1.7	NS	0.4	0.6	1.5	ND	Jaehde, 1995	DDI 10
11	OATs	Probenecid	Dicloxacillin	1.9	1.8	0.3	0.5	ND	ND	Beringer, 2008	DDI 11
12	OATs	Probenecid	Empagliflozin	1.52	1.24	0.46	ND	1.10	ND	Macha, 2014	DDI 12
13	OATs	Probenecid	Famotidine	1.8	1.5	0.4	0.1	NS	ND	Inotsume, 1990	DDI 13
14	OATs/MRPs	Probenecid	Furosemide	2.7	1.5	0.3	0.4	1.7	ND	Vree, 1995	DDI 14
15	OATs	Probenecid	Mesna	1.89	1.44	0.44	ND	1.05	ND	Cutler, 2012	DDI 15
16	OATs	Probenecid	Mesna	1.89	1.44	0.44	ND	1.05	ND	Cutler, 2012	DDI 16

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