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Erythromycin

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
SLC22A7	OAT2	18.5	OAT2-expressing oocytes	Kobayashi, 2005

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
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Erythromycin	217		Bromsulphthalein	HEK-OATP1B1	Seithel, 2007
SLCO1B3	OATP1B3, OATP8	Erythromycin	34		Bromsulphthalein	HEK293-OATP1B3	Seithel, 2007
ABCB1	MDR1, P-gp	Erythromycin		1000	Calcein AM	MDR1-expressing LLC-PK1 cells	Ekins, 2002
ABCB1	MDR1, P-gp	Erythromycin	>50		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
mouse_Abcb1a	Mdr, Pgp, Pgy, Mdr3, P-gp, Abcb4, Mdr1a	Erythromycin	>50		Calcein AM	Mouse mdr1a expressing LLC-PK1 cells	Schwab, 2003
mouse_Abcb1b	mdr, Mdr1, Pgy1, Abcb1, Mdr1b, Pgy-1	Erythromycin	>50		Calcein AM	Mouse mdr1b expressing LLC-PK1 cells	Schwab, 2003
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Erythromycin		5.27	Dichlorofluorescein	HEK-OATP1B1	Izumi, 2016
ABCB1	MDR1, P-gp	Erythromycin	10		Digoxin	Caco-2 cells	Ekins, 2002
ABCB1	MDR1, P-gp	Erythromycin	22.7		Digoxin	Caco-2 cells	Eberl, 2007
ABCC2	MRP2, cMOAT	Erythromycin	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Erythromycin	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Erythromycin	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A5	OCTN2	Erythromycin		2870	L-carnitine	MDCKII-hOCTN2	Diao, 2009
SLC22A5	OCTN2	Erythromycin		2870	L-carnitine	MDCKII-hOCTN2	Diao, 2010
ABCB11	BSEP	Erythromycin	>133		Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013
ABCB1	MDR1, P-gp	Erythromycin		37.79	Vinblastine	MDR1-expressing LLC-PK1 cells	Ekins, 2002
ABCB1	MDR1, P-gp	Erythromycin	119		Ximelagatran	Caco-2 cells	Eriksson, 2006

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	ABCB1/OATPs	Erythromycin	Simvastatin	6.2	3.5	ND	ND	NS	ND	Kantola, 1998	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