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

Rifampicin

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
SLCO1B3	OATP1B3, OATP8	2.3	OATP1B3-expressing oocytes	Vavricka, 2002
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	13	OATP1B1-expressing oocytes	Vavricka, 2002
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	1.5	HeLa-OATP1B1	Tirona, 2003

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	Rifampicin	2.4		8-fluorescein-cAMP	HEK293 cells	Bajraktari-Sylejmani, 2020
SLCO1B3	OATP1B3, OATP8	Rifampicin	2.1		8-fluorescein-cAMP	HEK293 cells	Bajraktari-Sylejmani, 2020
SLCO1B3	OATP1B3, OATP8	Rifampicin	0.8		Amanitin	MDCK II-OATP1B3	Letschert, 2006
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Rifampicin	3.25	3.08	Atorvastatin	HEK293-OATP1B1	Lau, 2007
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Rifampicin	3.2		Bosentan	CHO-OATP1B1	Treiber, 2007
SLCO1B3	OATP1B3, OATP8	Rifampicin	1.6		Bosentan	CHO-OATP1B1	Treiber, 2007
SLCO1A2	OATP1A2, OATP-A	Rifampicin		51	Bromsulphthalein	OATP1A2-expressing oocytes	Vavricka, 2002
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Rifampicin		17	Bromsulphthalein	OATP1B1-expressing oocytes	Vavricka, 2002
SLCO1B3	OATP1B3, OATP8	Rifampicin		5	Bromsulphthalein	OATP1B3-expressing oocytes	Vavricka, 2002
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Rifampicin	120		Bromsulphthalein	MDCK II-OATP1B1	Letschert, 2006
SLCO1B3	OATP1B3, OATP8	Rifampicin	1.5		Bromsulphthalein	MDCK II-OATP1B3	Letschert, 2006
SLCO2B1	OATP2B1, OATP-B	Rifampicin	90		Bromsulphthalein	MDCK II-OATP2B1	Letschert, 2006
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Rifampicin	11.9		Bromsulphthalein	HEK-OATP1B1	Leonhardt, 2010
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Rifampicin	5.65		Cerivastatin	HEK-OATP1B1	Tamraz, 2013
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Rifampicin	1.8	1.6	Cholyl-glycylamido-fluorescein (CGamF)	CHO-OATP1B1	Annaert, 2010
SLCO1B3	OATP1B3, OATP8	Rifampicin	1.3	0.9	Cholyl-glycylamido-fluorescein (CGamF)	CHO-OATP1B3	Annaert, 2010
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Rifampicin		6.75	Cilostazol	HEK-OATP1B1	Wang, 2017
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Rifampicin		0.355	Dichlorofluorescein	HEK-OATP1B1	Izumi, 2016
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Rifampicin	0.94		Estradiol-17beta-glucuronide	HeLa-OATP1B1	Tirona, 2003
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Rifampicin	0.94		Estradiol-17beta-glucuronide	HeLa cells	Tirona, 2003
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Rifampicin	1.5		Estradiol-17beta-glucuronide	CHO-OATP1B1	Gui, 2008
SLCO1B3	OATP1B3, OATP8	Rifampicin	2.6		Estradiol-17beta-glucuronide	CHO-OATP1B3	Gui, 2008
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Rifampicin	1.2	1.1	Estradiol-17beta-glucuronide	HEK-OATP1B1	Karlgren, 2012
SLCO1B3	OATP1B3, OATP8	Rifampicin	1.5	1.4	Estradiol-17beta-glucuronide	HEK293-OATP1B3	Karlgren, 2012
ABCC2	MRP2, cMOAT	Rifampicin	53		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Rifampicin	69		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Rifampicin	41.9		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Rifampicin	0.24		Estradiol-17beta-glucuronide	HEK-OATP1B1	Pahwa, 2017
SLCO2B1	OATP2B1, OATP-B	Rifampicin	2.1	1.6	Estrone sulfate	Caco-2	Annaert, 2010
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Rifampicin	0.88		Estrone sulfate	HEK-OATP1B1	Tamraz, 2013
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Rifampicin	10.46		Estrone sulfate	CHO-OATP1B1	Khurana, 2014
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Rifampicin	1.9		Estrone sulfate	HEK-OATP1B1	Parvez, 2016
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Rifampicin	1.3		Fluorescein-Methotrexate	CHO-OATP1B1	Gui, 2010
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Rifampicin	8.8		Lithocholyl-(Ne-NBD)-lysine	HEK-OATP1B1	Yamaguchi, 2011
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Rifampicin		0.48	Pitavastatin	HEK293-OATP1B1	Hirano, 2006
ABCB11	BSEP	Rifampicin	10.5		Taurocholate	BSEP-expressing Sf9 vesicles	Kis, 2009
ABCB11	BSEP	Rifampicin	25.3		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	OATP1B1	Rifampicin	Atorvastatin	7.25	10.5	ND	0.13	0.37	ND	Lau, 2007	DDI 1
2	OATP1B1/OATP1B3	Rifampicin	Glecaprevir	8.55	6.52	ND	ND	ND	ND	Yu, 2019	DDI 2
3	OATPs	Rifampicin	Glyburide	2.2	1.8	NS	0.5	ND	yes	Zheng, 2009	DDI 3
4	OATP1B1	Rifampicin	Pitavastatin	5.28	7.65	ND	0.15	0.51	ND	Chen, 2013	DDI 4
5	OATP1B1	Rifampicin	Pitavastatin	5.41	4.77	ND	ND	NS	ND	Prueksaritanont, 2014	DDI 5
6	OATP1B1	Rifampicin	Pravastatin	2.27	2.73	ND	0.5	NS	ND	Deng, 2009	DDI 6
7	ABCG2/OATP1B1	Rifampicin	Rosuvastatin	4.09	9.39	ND	ND	NS	ND	Prueksaritanont, 2014	DDI 7
8	OATP1B1/OATP1B3	Rifampicin	Voxilaprevir	7.96	8.74	ND	ND	ND	ND	Yu, 2019	DDI 8

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