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Ritonavir

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
ABCB1	MDR1, P-gp	0.8	MDR1 transfected LLC-PK1	Woodahl, 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
SLC22A1	OCT1	Ritonavir	33.9		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT1	Wittwer, 2013
SLC22A3	OCT3	Ritonavir	>300		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT3	Wittwer, 2013
SLC22A2	OCT2	Ritonavir	24.8		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
SLC47A1	MATE1	Ritonavir	4.4		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-MATE1	Wittwer, 2013
SLC47A2	MATE2K	Ritonavir	4.4		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-MATE2K	Wittwer, 2013
SLC47A2	MATE2K	Ritonavir	23.7		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-MATE2K	Wittwer, 2013
ABCB1	MDR1, P-gp	Ritonavir	12		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
mouse_Abcb1a	Mdr, Pgp, Pgy, Mdr3, P-gp, Abcb4, Mdr1a	Ritonavir	50		Calcein AM	Mouse mdr1a expressing LLC-PK1 cells	Schwab, 2003
mouse_Abcb1b	mdr, Mdr1, Pgy1, Abcb1, Mdr1b, Pgy-1	Ritonavir	>50		Calcein AM	Mouse mdr1b expressing LLC-PK1 cells	Schwab, 2003
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Ritonavir	1.6	1.4	Cholyl-glycylamido-fluorescein (CGamF)	CHO-OATP1B1	Annaert, 2010
SLCO1B3	OATP1B3, OATP8	Ritonavir	3.6	2.5	Cholyl-glycylamido-fluorescein (CGamF)	CHO-OATP1B3	Annaert, 2010
ABCB1	MDR1, P-gp	Ritonavir	15.7		Cyclosporine	MDR1 expressing LLC-PK1 cells	Kumar, 2003
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Ritonavir		0.32	Dichlorofluorescein	HEK-OATP1B1	Izumi, 2016
ABCB1	MDR1, P-gp	Ritonavir	3.8		Digoxin	Caco-2 cells	Choo, 2000
ABCB1	MDR1, P-gp	Ritonavir	28.2		Digoxin	MDCKII-MDR1	Keogh, 2006
ABCB1	MDR1, P-gp	Ritonavir	5		Digoxin	Caco-2 cells	Cook, 2010
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Ritonavir	0.71		Estradiol-17beta-glucuronide	HeLa-OATP1B1	Tirona, 2003
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Ritonavir	1.3	1.3	Estradiol-17beta-glucuronide	HEK-OATP1B1	Karlgren, 2012
SLCO1B3	OATP1B3, OATP8	Ritonavir	4.4	4	Estradiol-17beta-glucuronide	HEK293-OATP1B3	Karlgren, 2012
ABCC3	MRP3	Ritonavir	11.1		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Ritonavir	34		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Ritonavir	0.68		Estradiol-17beta-glucuronide	HEK-OATP1B1	Vermeer, 2016
ABCC2	MRP2, cMOAT	Ritonavir	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLCO2B1	OATP2B1, OATP-B	Ritonavir	6.3	4.8	Estrone sulfate	Caco-2	Annaert, 2010
SLCO2B1	OATP2B1, OATP-B	Ritonavir	2.2		Estrone sulfate	MDCK II-OATP2B1	Kis, 2010
SLCO1A2	OATP1A2, OATP-A	Ritonavir	<10		Fexofenadine	HeLa-OATP1A2	Cvetkovic, 1999
SLC22A5	OCTN2	Ritonavir		7.73	L-carnitine	MDCKII-hOCTN2	Diao, 2010
SLC47A1	MATE1	Ritonavir	15.4		Metformin	HeLa-MATE1	Meyer, 2010
SLC47A1	MATE1	Ritonavir	0.08		Metformin	HEK293-MATE1	Wittwer, 2013
SLC47A1	MATE1	Ritonavir	2.1		Metformin	MDCK2- MATE1	Wittwer, 2013
SLC22A1	OCT1	Ritonavir	3.8		Metformin	HEK293-OCT1	Yee, 2021
SLC22A1	OCT1	Ritonavir	14		N-methylpyridinium	HEK293-OCT1	Jung, 2008
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Ritonavir		0.78	Pitavastatin	HEK293-OATP1B1	Hirano, 2006
ABCB11	BSEP	Ritonavir	1.74		Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A1	OCT1	Ritonavir	5.18		Tetraethylammonium	HeLa-OCT1	Zhang, 2000
SLC47A1	MATE1	Ritonavir	13.9		Tetraethylammonium	HeLa-MATE1	Meyer, 2010

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/OATPs	Atazanavir / Ritonavir	Rosuvastatin	3.1	7.0	ND	ND	ND	ND	Busti, 2008	DDI 1
2	ABCB1/OATPs	Indinavir / Ritonavir	Fexofenadine	4.8	2.5	ND	0.2	0.7	ND	Kharasch, 2009	DDI 2
3	OATPs	Lopinavir / Ritonavir	Rosuvastatin	2.1	4.7	ND	0.5	NS	yes	Kiser, 2008	DDI 3
4	ABCB1/OATPs	Ritonavir	Digoxin	1.9	ND	0.6	0.6	2.6	ND	Ding, 2004	DDI 4
5	ABCB1/OATPs	Ritonavir	Saquinavir	29.9	22.5	ND	ND	ND	ND	la, 2007	DDI 5

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