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Sulfasalazine

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
ABCG2	BCRP, MXR	0.7	Caco-2 cells	Wang, 2008
ABCG2	BCRP, MXR	0.7	BCRP-expressing Sf9 vesicles	Jani, 2009
ABCG2	BCRP, MXR	0.4	Sf9 cell membranes	Bircsak, 2013

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
SLCO2B1	OATP2B1, OATP-B	Sulfasalazine	2.7		Dibromofluorescein	HEK293-OATP2B1	Unger, 2020
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Sulfasalazine	0.56	0.53	Estradiol-17beta-glucuronide	HEK-OATP1B1	Karlgren, 2012
SLCO1B3	OATP1B3, OATP8	Sulfasalazine	12	11	Estradiol-17beta-glucuronide	HEK293-OATP1B3	Karlgren, 2012
ABCC3	MRP3	Sulfasalazine	14.6		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Sulfasalazine	1.5		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCG2	BCRP, MXR	Sulfasalazine	0.73		Estrone sulfate	BCRP-expressing oocytes	Elsby, 2011
ABCG2	BCRP, MXR	Sulfasalazine	0.61		Estrone sulfate	BCRP membrane vesicles	Elsby, 2016
SLC22A6	OAT1	Sulfasalazine	4.6		Methotrexate	OAT1-expressing oocytes	Elsby, 2011
SLC22A8	OAT3	Sulfasalazine	3		Methotrexate	OAT3-expressing oocytes	Elsby, 2011
ABCG2	BCRP, MXR	Sulfasalazine	2.9		Rosuvastatin	polarized Caco-2 monolayer	Elsby, 2016
ABCB11	BSEP	Sulfasalazine	>133		Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013

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	ABCG2	Curcumin	Sulfasalazine	3.2	3.72	ND	3.24	ND		Kusuhara, 2012	DDI 1
2	ABCG2	Pantoprazole	Sulfasalazine	1	1	ND	ND	1		Adkison, 2010	DDI 2

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