UCSF home page | About UCSF | UCSF Medical Center

Skip to TransPortal content

Enlarge Text
Click to increase the text size. Restore Text
Click to restore original text size. Reduce Text
Click to decrease the text size.


Decrease the text size \| Restore text size \| Increase the text size

Clarithromycin

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)	Substrate used	Cell System	Reference
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Clarithromycin	96	Bromsulphthalein	HEK-OATP1B1	Seithel, 2007
SLCO1B3	OATP1B3, OATP8	Clarithromycin	32	Bromsulphthalein	HEK293-OATP1B3	Seithel, 2007
ABCB1	MDR1, P-gp	Clarithromycin	56.1	Calcein AM	NIH-3T3-G185 cells	Wang, 2001
ABCB1	MDR1, P-gp	Clarithromycin	3.8	Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
ABCB1	MDR1, P-gp	Clarithromycin	4.1	Digoxin	Caco-2 cells	Eberl, 2007
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Clarithromycin	5.3	Estradiol-17beta-glucuronide	HEK-OATP1B1	Vermeer, 2016
ABCC2	MRP2, cMOAT	Clarithromycin	>133	Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Clarithromycin	>133	Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Clarithromycin	>133	Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCB1	MDR1, P-gp	Clarithromycin	86.7	Fluo-3	NIH-3T3-G185 cells	Wang, 2001
ABCB1	MDR1, P-gp	Clarithromycin	50.2	JC-1	NIH-3T3-G185 cells	Wang, 2001
ABCB1	MDR1, P-gp	Clarithromycin	7.2	LDS-751	NIH-3T3-G185 cells	Wang, 2001
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Clarithromycin	75	Lithocholyl-(Ne-NBD)-lysine	HEK-OATP1B1	Yamaguchi, 2011
ABCB1	MDR1, P-gp	Clarithromycin	15.1	Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
ABCB11	BSEP	Clarithromycin	>133	Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013
ABCB1	MDR1, P-gp	Clarithromycin	23.8	Tetramethylrosamine	NIH-3T3-G185 cells	Wang, 2001

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	OATP1B1, OATP1B3,OATP2B1	Clarithromycin	Atorvastatin	4.45	5.38	ND	ND	ND		Jacobson, 2004	DDI 1
2	OATP1B1, OATP1B3	Clarithromycin	Bosentan	3.73	3.82	ND	0.27	NR		Markert, 2014	DDI 2
3	OATP1B1, OATP1B3,OATP2B1	Clarithromycin	Pravastatin	2.11	2.28	ND	ND	ND		Jacobson, 2004	DDI 3
4	OATP1B1, OATP1B3,OATP2B1	Clarithromycin	Simvastatin	9.95	7.14	ND	ND	ND		Jacobson, 2004	DDI 4

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