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ABCB1

Synonyms: ABC20, CD243, CLCS, GP170, MDR1, MGC163296, P-GP, PGP, PGY1

Entrez Gene Link

Expression Data
Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

Orthologs in other species

grivet ABCB1
mouse Abcb1a
mouse Abcb1b

Expression Data

Expression data for other tissues could be found in http://pharmacogenetics.ucsf.edu/gtex/index.html

Asterisk indicates important transporters in the organ as identified in the organ diagram.

Organ	Source	Relative Expression
Brain	Nishimura	`0.00913`
Kidney*	Nishimura	`0.0851`
Liver*	Nishimura	`0.0230`
Placenta*	Nishimura	`0.0255`
Small Intestine*	Nishimura	`0.0337`
Kidney*	Mean across all PMT Samples	`0.471`
Liver*	Mean across all PMT Samples	`0.256`

Note that relative expression values should only be compared between entries of the same source.

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In Vitro Substrates

Substrate	Km (μM)	Cell System	Reference
Acetochlor	25	Sf9 cell membranes	Oosterhuis, 2008
Alachlor	35	Sf9 cell membranes	Oosterhuis, 2008
Berberine	>300	Caco-2	Maeng, 2002
Biotin	13	MDCK-MDR1	Luo, 2006
Chlorpromazine	27.4	MDR1-expressing insect vesicles	Boulton, 2002
Clozapine	58	MDR1-expressing insect vesicles	Boulton, 2002
Colchicine	45	MDR1-containing proteoliposomes	Ambudkar, 1992
Colchicine	1.33	MDR1-expressing CEM/VLB100 vesicles	Bebawy, 1999
Colchicine	1640	Caco-2	Troutman, 2003
Cyclosporine²	8.4	MDR1-expressing LLC-PK1 cells	Saeki, 1993
Cyclosporine²	3.8	MDR1-expressing Caco-2 cells	Fricker, 1996
Dactinomycin	10	MDR1-containing proteoliposomes	Ambudkar, 1992
Damgo	43	MDR1-expressing SW1573/S1 vesicles	Oude, 2001
Dexamethasone	826	ATPase assay of Sf9-MDR1 liposomes	Kimura, 2007
Digoxin^1,3	177	Caco-2	Troutman, 2003
Digoxin^1,3	73	Caco-2	Collett, 2004
Digoxin^1,3	181	ATPase assay of Sf9-MDR1 liposomes	Kimura, 2007
Dolastatin-10	0.9	MDR1-containing proteoliposomes	Borgnia, 1996
Doxorubicin	3	MDR1-containing proteoliposomes	Ambudkar, 1992
Doxorubicin	ND	MDR1 transfected LLC-PK1	Woodahl, 2009
Emetine	6	MDR1-containing proteoliposomes	Borgnia, 1996
Estradiol-17beta-glucuronide	62	MDR1-expressing Sf9 vesicles	Huang, 1998
Etoposide	255	MDCK II-MDR1	Guo, 2002
Etoposide	461	Caco-2	Troutman, 2003
Fexofenadine^1,3	150	Caco-2	Petri, 2004
Grepafloxacin	580	MDR1-expressing Caco-2 cells	Yamaguchi, 2000
Haloperidol	33	MDR1-expressing insect vesicles	Boulton, 2002
Hydroxyrubicin	2	MDR1-expressing K562 cells	Borrel, 1994
Indinavir	0.47	ATPase assay of High Five-MDR1 membranes	Lee, 1998
Irinotecan	45.5	MDCK II-MDR1	Luo, 2002
Irinotecan	116.1	Caco-2	Luo, 2002
Levofloxacin	3000	MDR1-expressing LLC-PK1 cells	Ito, 1997
Levofloxacin	5600	MDR1-expressing Caco-2 cells	Yamaguchi, 2000
Loperamide¹	11.4	Sf9-MDR1 ATPase assay	Feng, 2008
Losartan	100	MDR1-containing proteoliposomes	Borgnia, 1996
Losartan	232	MDR1-expressing Caco-2 cells	Soldner, 2000
Losartan	403.2	MDR1-expressing MDCK cells	Soldner, 2000
Metolachlor	10	Sf9 cell membranes	Oosterhuis, 2008
Nicardipine	2.6	ATPase assay of Sf9-MDR1 liposomes	Kimura, 2007
Olanzapine	8.3	MDR1-expressing insect vesicles	Boulton, 2002
Oseltamivir	4200	MDR1-expressing LLC-PK1 cells	Hoffmann, 2009
Paclitaxel	16.5	MDR1-expressing Caco-2 cells	Walle, 1998
Paclitaxel	0.014	MDR1-expressing MCF7 cells	Jang, 2001
Paclitaxel	65	Caco-2	Collett, 2004
Paclitaxel	0.7	MDR1-expressing Sf9 vesicles	Takahashi, 2005
Paclitaxel	1.4	ATPase assay of Sf9-MDR1 liposomes	Kimura, 2007
Prazosin	20	MDR1-expressing insect vesicles	Dey, 1997
Progesterone	30	MDR1-containing proteoliposomes	Borgnia, 1996
Quetiapine	12.3	MDR1-expressing insect vesicles	Boulton, 2002
Quinidine^1,2,4	18.2	MDR1-expressing insect vesicles	Smith, 2001
Quinine	10	MDR1-containing proteoliposomes	Borgnia, 1996
Rhodamine 123	21	ATPase assay of Sf9-MDR1 liposomes	Kimura, 2007
Risperidone	12.4	MDR1-expressing insect vesicles	Boulton, 2002
Ritonavir^2,4	0.8	MDR1 transfected LLC-PK1	Woodahl, 2005
Saquinavir	15.4	Caco-2	Collett, 2004
Saquinavir	14.5	MDR1 transfected LLC-PK1	Woodahl, 2005
Topotecan	78.3	Caco-2	Li, 2008
Topotecan	102	MDCK II-MDR1	Li, 2008
Valinomycin	1	MDR1-containing proteoliposomes	Borgnia, 1996
Valinomycin	2.5	ATPase assay of Sf9-MDR1 liposomes	Kimura, 2007
Verapamil^2,4	2	MDR1-containing proteoliposomes	Borgnia, 1996
Verapamil^2,4	2	MDR1-expressing Sf9 vesicles	Takahashi, 2005
Verapamil^2,4	4.1	ATPase assay of Sf9-MDR1 liposomes	Kimura, 2007
Verapamil^2,4	1.9	Sf9 cell membranes	Bircsak, 2013
Vinblastine¹	18.99	MDR1-expressing Caco-2 cells	Hunter, 1993
Vinblastine¹	19	Caco-2	Hunter, 1993
Vinblastine¹	0.8	MDR1-containing proteoliposomes	Borgnia, 1996
Vinblastine¹	99.4	MDR1-expressing LLC-PK1 cells	Lecureur, 2000
Vinblastine¹	89.2	Caco-2	Tang, 2002
Vinblastine¹	253	MDCK-MDR1	Tang, 2002
Vinblastine¹	1.7	ATPase assay of Sf9-MDR1 liposomes	Kimura, 2007
Vinblastine¹	146	MDR1-expressing oocytes	Jutabha, 2010
Vincristine	3.7	ATPase assay of Sf9-MDR1 liposomes	Kimura, 2007

ND = not determined
1 denotes drugs that can potentially be used as in vitro substrates for studies of the transporter as defined by the FDA as of March 2022
2 denotes drugs that can potentially be used as in vitro inhibitors for studies of the transporter as defined by the FDA as of March 2022
3 denotes drugs that can potentially be used as clinical substrates for studies of the transporter as defined by the FDA as of March 2022
4 denotes drugs that can potentially be used as clinical inhibitors for studies of the transporter as defined by the FDA as of March 2022

In Vitro Inhibitors

Inhibitor	IC50 (μM)	Ki (μM)	Substrate used	Cell System	Reference
(+)-citronellal	167		Digoxin^1,3	LLC-PK1 cells	Yoshida, 2006
(+)-devapamil	1		Vinblastine¹	F4-6P cells	Hollt, 1992
(+)-emopamil	2.4		Vinblastine¹	F4-6P cells	Hollt, 1992
(+)-felodipine	6.3		Vinblastine¹	F4-6P cells	Hollt, 1992
(+)-isradipine	9.2		Vinblastine¹	F4-6P cells	Hollt, 1992
(+)-niguldipine	1.2		Vinblastine¹	F4-6P cells	Hollt, 1992
(+)-nimodipine	12.6		Vinblastine¹	F4-6P cells	Hollt, 1992
(+)-nitrendipine	10.3		Vinblastine¹	F4-6P cells	Hollt, 1992
(+)-verapamil	2.6		Vinblastine¹	F4-6P cells	Hollt, 1992
(-)-beta-pinene	608		Digoxin^1,3	LLC-PK1 cells	Yoshida, 2006
(-)-citronellol	504		Digoxin^1,3	LLC-PK1 cells	Yoshida, 2006
(-)-devapamil	2.1		Vinblastine¹	F4-6P cells	Hollt, 1992
(-)-emopamil	3		Vinblastine¹	F4-6P cells	Hollt, 1992
(-)-felodipine	8.6		Vinblastine¹	F4-6P cells	Hollt, 1992
(-)-isradipine	4.7		Vinblastine¹	F4-6P cells	Hollt, 1992
(-)-niguldipine	1.3		Vinblastine¹	F4-6P cells	Hollt, 1992
(-)-nimodipine	15.8		Vinblastine¹	F4-6P cells	Hollt, 1992
(-)-nitrendipine	9.4		Vinblastine¹	F4-6P cells	Hollt, 1992
(-)-verapamil	2.9		Vinblastine¹	F4-6P cells	Hollt, 1992
Abietic acid	172		Digoxin^1,3	LLC-PK1 cells	Yoshida, 2006
Alfentanil	112		Digoxin^1,3	Caco-2 cells	Wandel, 2002
Alpha-hydroxy-propiconazole	366.4		N-methyl-quinidine	Human "K" cell inverted vesicles	Mazur, 2015
Alpha-terpinene	414		Digoxin^1,3	LLC-PK1 cells	Yoshida, 2006
Amiodarone⁴	12.8		Calcein AM	CEM cells	Tiberghien, 1996
Amiodarone⁴		5.78	Calcein AM	MDR1-expressing LLC-PK1 cells	Baltes, 2007
Amiodarone⁴	65.4		Calcein AM	MDCK-II cells	Georgantzopoulou, 2014
Amiodarone⁴	22.5		Daunorubicin	MDR1 transfected LLC-PK1	Katoh, 2001
Amiodarone⁴	45.6		Digoxin^1,3	MDR1 transfected LLC-PK1	Katoh, 2001
Amiodarone⁴	5.48		Digoxin^1,3	MDR1 transfected LLC-PK1	Kakumoto, 2002
Amlodipine	22		Daunorubicin	MDR1 expressing LLC-PK1 cells	Katoh, 2000
Aripiprazole	0.8		Rhodamine 123	MDR1 expressing L5178 cells	Broccatelli, 2011
Astemizole	1.3		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Astemizole	2.73		Digoxin^1,3	MDCKII-MDR1	Keogh, 2006
Atorvastatin	271		Daunorubicin	MDR1 expressing 3T3-G185 cells	Wang, 2001
Atorvastatin	307		Rhodamine 123	MDR1 expressing 3T3-G185 cells	Wang, 2001
Atorvastatin lactone	14		Calcein AM	MDR1 expressing MDCK cells	Chen, 2005
Azelastine	16		Daunorubicin	MDR1 transfected LLC-PK1	Katoh, 2001
Azelastine	30		Digoxin^1,3	MDR1 transfected LLC-PK1	Katoh, 2001
Azinphos-ethyl	129		Doxorubicin	B16/F10 cells	Bain, 1997
Azithromycin	21.8		Digoxin^1,3	Caco-2 cells	Eberl, 2007
B869-60	58		Vinblastine¹	F4-6P cells	Hollt, 1992
B869-61	50		Vinblastine¹	F4-6P cells	Hollt, 1992
Barnidipine	8.6		Daunorubicin	MDR1 expressing LLC-PK1 cells	Katoh, 2000
Barnidipine	12.6		Digoxin^1,3	MDR1 expressing LLC-PK1 cells	Takara, 2002
Bay K 8644	79		Vinblastine¹	F4-6P cells	Hollt, 1992
Benidipine	9.5		Daunorubicin	MDR1 expressing LLC-PK1 cells	Katoh, 2000
Benidipine	5		Digoxin^1,3	MDR1 expressing LLC-PK1 cells	Takara, 2002
Beta-hydroxy-propiconazole	456.3		N-methyl-quinidine	Human "K" cell inverted vesicles	Mazur, 2015
Bromocriptine		2.81	Calcein AM	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Bromocriptine		3.96	Vinblastine¹	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Carvedilol⁴	4.6		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
Carvedilol⁴	6		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Carvedilol⁴	6.6		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
Celiprolol		313	Paclitaxel	MDR1-expressing Caco-2 cells	Gao, 2001
Celiprolol	730		Verapamil^2,4	Caco-2 cells	Doppenshmitt, 1998
Cepharanthin	2.1		Daunorubicin	MDR1 expressing LLC-PK1 cells	Hirai, 1995
Chloropromazine	196		Calcein AM	Caco-2 cells	Eneroth, 2001
Chloropromazine	1.2		Verapamil^2,4	Caco-2 cells	Doppenshmitt, 1998
Chlorpyrifos	140.6		Doxorubicin	B16/F10 cells	Bain, 1996
Cholesterol	8.2		Daunorubicin	NIH-G185 cells	Wang, 2000
Cimetidine	>50		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Cimetidine	6500		Verapamil^2,4	Caco-2 cells	Doppenshmitt, 1998
Clarithromycin⁴	56.1		Calcein AM	NIH-3T3-G185 cells	Wang, 2001
Clarithromycin⁴	3.8		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
Clarithromycin⁴	4.1		Digoxin^1,3	Caco-2 cells	Eberl, 2007
Clarithromycin⁴	86.7		Fluo-3	NIH-3T3-G185 cells	Wang, 2001
Clarithromycin⁴	50.2		JC-1	NIH-3T3-G185 cells	Wang, 2001
Clarithromycin⁴	7.2		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Clarithromycin⁴	15.1		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
Clarithromycin⁴	23.8		Tetramethylrosamine	NIH-3T3-G185 cells	Wang, 2001
Clofazimine	0.6		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
Clofazimine	1.1		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Clofazimine	1		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
Clotrimazole		44	Calcein AM	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Clotrimazole	6.7		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Clotrimazole	16.6		Doxorubicin	B16/F10 cells	Bain, 1996
Clotrimazole		29.92	Vinblastine¹	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Cnidiadin	26.4		Vinblastine¹	MDCK-II cells	Barthomeuf, 2005
Colchicine	>50		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Coumaphos	26.9		Doxorubicin	B16/F10 cells	Bain, 1997
Cucurbitacin I	181		Digoxin^1,3	LLC-PK1 cells	Yoshida, 2006
Cyclosporine²	3.4		Calcein AM	CEM cells	Tiberghien, 1996
Cyclosporine²		1.8	Calcein AM	MDR1-expressing CEM/VLB100 cells	Wigler, 1999
Cyclosporine²	7		Calcein AM	Caco-2 cells	Eneroth, 2001
Cyclosporine²	1.7		Calcein AM	NIH-3T3-G185 cells	Wang, 2001
Cyclosporine²		4.66	Calcein AM	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Cyclosporine²	0.8		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Cyclosporine²	9.3		Calcein AM	MDR1 expressing MDCK2 cells	Tong, 2007
Cyclosporine²	1.4		Calcein AM	MDR1 expressing A2780/ADR cells	Muller, 2007
Cyclosporine²	1.4		Calcein AM	MDR1 expressing A2780/ADR cells	Muller, 2008
Cyclosporine²	1.4		Calcein AM	MDR1 expressing A2780/ADR cells	Klinkhammer, 2009
Cyclosporine²	0.9		Calcein AM	Doxorubicin-resistant A2780 adr cells	Juvale, 2013
Cyclosporine²	0.9		Calcein AM	MDR1 expressing A2780/ADR cells	Kohler, 2015
Cyclosporine²	1.2		Calcein AM	MDR1 expressing A2780/ADR cells	Krapf, 2017
Cyclosporine²	1.36		Colchicine	MDCK II-MDR1	Rautio, 2006
Cyclosporine²	1.4		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
Cyclosporine²	0.1		Daunorubicin	MDR1 exressing CCRF-cEM/VCR 1000 cells	Jabeen, 2012
Cyclosporine²	3.7		Digoxin^1,3	MDR1 expressing LLC-PK1 cells	Kusunoki, 1998
Cyclosporine²	1.3		Digoxin^1,3	Caco-2 cells	Choo, 2000
Cyclosporine²		0.46	Digoxin^1,3	Caco-2	Tang, 2002
Cyclosporine²		2.18	Digoxin^1,3	MDCK-MDR1	Tang, 2002
Cyclosporine²		0.35	Digoxin^1,3	MDR1-expressing Caco-2 cells	Horie, 2003
Cyclosporine²	1.6		Digoxin^1,3	MDCK II-MDR1	Rautio, 2006
Cyclosporine²	2.4		Fluo-3	NIH-3T3-G185 cells	Wang, 2001
Cyclosporine²	1.4		Hoechst 33342	MDR1 expressing A2780/ADR cells	Muller, 2008
Cyclosporine²	1.4		Hoechst 33342	MDR1 expressing A2780/ADR cells	Pick, 2008
Cyclosporine²	4.3		JC-1	NIH-3T3-G185 cells	Wang, 2001
Cyclosporine²	1.8		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Cyclosporine²	1.4		Rhodamine 123	MDR1 transfected NIH3T3-G185	Wang, 2001
Cyclosporine²	1.7		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
Cyclosporine²	0.7		Rhodamine 123	MDR1 expressing L5178 cells	Broccatelli, 2011
Cyclosporine²	2.1		Tetramethylrosamine	NIH-3T3-G185 cells	Wang, 2001
Cyclosporine²		0.02	Verapamil^2,4	MDR1-expressing Sf9 vesicles	Rao, 1994
Cyclosporine²	0.7		Verapamil^2,4	Sf9 cell membranes	Bircsak, 2013
Cyclosporine²		1.3	Vinblastine¹	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Cyclosporine²	6.18		Vinblastine¹	MDCK II-MDR1	Rautio, 2006
Daunorubicin		111	Digoxin^1,3	MDR1-expressing MDCK cells	Tang, 2002
Daunorubicin		2.5	Paclitaxel	MDR1-expressing Caco-2 cells	Gao, 2001
Desethylamiodarone	15.4		Daunorubicin	MDR1 transfected LLC-PK1	Katoh, 2001
Desethylamiodarone	25.2		Digoxin^1,3	MDR1 transfected LLC-PK1	Katoh, 2001
Desethylamiodarone	1.27		Digoxin^1,3	MDR1 transfected LLC-PK1	Kakumoto, 2002
Desmethylazelastine	11.8		Daunorubicin	MDR1 transfected LLC-PK1	Katoh, 2001
Desmethylazelastine	11.8		Daunorubicin	MDR1 transfected LLC-PK1	Kakumoto, 2002
Desmethylazelastine	41.8		Digoxin^1,3	MDR1 transfected LLC-PK1	Katoh, 2001
Dexamethasone	>50		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Dexniguldipine		2.3	Calcein AM	MDR1-expressing CEM/VLB100 cells	Wigler, 1999
Diazinon	58.4		Calcein AM	NIH 3T3 cells	Pivcevic, 2006
Dicapthon	191.7		Doxorubicin	B16/F10 cells	Bain, 1996
Digoxin^1,3	>50		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Dihydroergocristine		511	Calcein AM	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Dihydroergocristine		16	Vinblastine¹	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Dihydroergocryptine		360.5	Calcein AM	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Dihydroergocryptine		19.82	Vinblastine¹	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Dihydroergotamine		1000	Calcein AM	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Dihydroergotamine		119.94	Vinblastine¹	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Diltiazem	42.7		Calcein AM	MDR1 expressing A2780/ADR cells	Muller, 2007
Diltiazem	49		Calcein AM	MDR1 expressing A2780/ADR cells	Klinkhammer, 2009
Diltiazem	77.7		Digoxin^1,3	MDR1 expressing LLC-PK1 cells	Takara, 2002
Diltiazem	42.7		Hoechst 33342	MDR1 expressing A2780/ADR cells	Pick, 2008
Dipyridamole	22.7		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
Dipyridamole	40		Digoxin^1,3	MDR1 transfected LLC-PK1	Kakumoto, 2002
Dipyridamole	23.7		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Dipyridamole	34.3		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
Domperidone	106		Calcein AM	Caco-2 cells	Eneroth, 2001
Doxorubicin		8.5	Paclitaxel	MDR1-expressing Caco-2 cells	Gao, 2001
Doxorubicin	990		Verapamil^2,4	Caco-2 cells	Doppenshmitt, 1998
DPDE (enkephalin)	>50		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Ebastine	1.5		Rhodamine 123	MDR1 expressing L5178 cells	Broccatelli, 2011
Efonidipine	17.3		Daunorubicin	MDR1 expressing LLC-PK1 cells	Katoh, 2000
Efonidipine	20.6		Daunorubicin	MDR1 expressing LLC-PK1 cells	Katoh, 2000
Efonidipine	13		Digoxin^1,3	MDR1 expressing LLC-PK1 cells	Takara, 2002
Elacridar	0.2		Calcein AM	MDR1 expressing Kb-V1 cells	Puentes, 2011
Elacridar	0.1		Daunorubicin	MDR1 exressing CCRF-cEM/VCR 1000 cells	Jabeen, 2012
Elacridar (GF120918)²	0.027		Colchicine	MDCK II-MDR1	Rautio, 2006
Elacridar (GF120918)²		0.39	Digoxin^1,3	Caco-2	Tang, 2002
Elacridar (GF120918)²		0.44	Digoxin^1,3	MDCK-MDR1	Tang, 2002
Elacridar (GF120918)²	0.18		Digoxin^1,3	MDCKII-MDR1	Keogh, 2006
Elacridar (GF120918)²	0.055		Digoxin^1,3	MDCK II-MDR1	Rautio, 2006
Elacridar (GF120918)²	0.043		Vinblastine¹	MDCK II-MDR1	Rautio, 2006
Elacridar Hydrochloride		0.04	Digoxin^1,3	MDR1-expressing Caco-2 cells	Horie, 2003
Emetine	35.1		Calcein AM	NIH-3T3-G185 cells	Wang, 2001
Emetine	9.2		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
Emetine	130.3		Fluo-3	NIH-3T3-G185 cells	Wang, 2001
Emetine	115.6		JC-1	NIH-3T3-G185 cells	Wang, 2001
Emetine	2.4		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Emetine	9.6		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
Emetine	207.1		Tetramethylrosamine	NIH-3T3-G185 cells	Wang, 2001
Endosulfan	2.8		Calcein AM	NIH 3T3 cells	Pivcevic, 2006
Endosulfan	34.1		Doxorubicin	B16/F10 cells	Bain, 1996
Endosulfan	33.6		Verapamil^2,4	Sf9 cell membranes	Bircsak, 2013
Ergocornine		105.2	Calcein AM	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Ergocornine		24.5	Vinblastine¹	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Ergocristine		42.8	Calcein AM	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Ergocristine		13.33	Vinblastine¹	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Ergocryptine		12.2	Calcein AM	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Ergocryptine		6.43	Vinblastine¹	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Ergonovine		115.5	Calcein AM	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Ergonovine		100	Vinblastine¹	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Ergotamine		98.9	Calcein AM	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Ergotamine		14.25	Vinblastine¹	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Erlotinib	2		Vincristine	MDR1-expressing K562 vesicles	Noguchi, 2009
Erythromycin		1000	Calcein AM	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Erythromycin	>50		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Erythromycin	10		Digoxin^1,3	Caco-2 cells	Ekins, 2002
Erythromycin	22.7		Digoxin^1,3	Caco-2 cells	Eberl, 2007
Erythromycin		37.79	Vinblastine¹	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Erythromycin	119		Ximelagatran	Caco-2 cells	Eriksson, 2006
Erythromycin A	145.1		N-methyl-quinidine	Human "K" cell inverted vesicles	Mazur, 2015
Erythromycin A	119		Ximelagatran	Caco-2 cells	Eriksson, 2006
Etoposide	>50		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Etoposide		768	Digoxin^1,3	MDR1-expressing MDCK cells	Tang, 2002
Etoposide		276	Paclitaxel	MDR1-expressing Caco-2 cells	Gao, 2001
Felodipine	26.3		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
Felodipine	32.3		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Felodipine	60		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
Fentanyl	6.5		Digoxin^1,3	Caco-2 cells	Wandel, 2002
Fluconazole		1000	Calcein AM	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Fluconazole		400	Vinblastine¹	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Fluphenazine	6.5		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
Fluphenazine	5.7		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Fluphenazine	10.4		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
Forskolin	80.2		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
Forskolin	188.2		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Gallopamil	3.2		Daunorubicin	NIH-G185 cells	Wang, 2001
Gallopamil	2.5		Vinblastine¹	F4-6P cells	Hollt, 1992
Gamma-hydroxy-propiconazole	350.8		N-methyl-quinidine	Human "K" cell inverted vesicles	Mazur, 2015
Glycyrrhetic acid	80.8		Digoxin^1,3	LLC-PK1 cells	Yoshida, 2006
Gpv005	0.6		Daunorubicin	MDR1 exressing CCRF-cEM/VCR 1000 cells	Jabeen, 2012
Gpv062	0.1		Daunorubicin	MDR1 exressing CCRF-cEM/VCR 1000 cells	Jabeen, 2012
Haloperidol	5.3		Verapamil^2,4	Caco-2 cells	Doppenshmitt, 1998
Hydramethylnon	7.3		Doxorubicin	B16/F10 cells	Bain, 1996
Hydrocortisone	>50		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Imatinib	7.2		Calcein AM	MDR1 expressing A2780/ADR cells	Muller, 2007
Imatinib	7.2		Hoechst 33342	MDR1 expressing A2780/ADR cells	Pick, 2008
Indinavir	44		Digoxin^1,3	Caco-2 cells	Choo, 2000
Itraconazole⁴	2.1		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Itraconazole⁴	1.7		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
Itraconazole⁴	1.7		Daunorubicin	G185 cells	Wang, 2002
Itraconazole⁴	0.95		Digoxin^1,3	MDCKII-MDR1	Keogh, 2006
Itraconazole⁴	2		Digoxin^1,3	Caco-2 cells	Cook, 2010
Itraconazole⁴	2.4		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Ivermectin	9		Calcein AM	Caco-2 cells	Eneroth, 2001
Ivermectin	0.1		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Ivermectin	10.9		Doxorubicin	B16/F10 cells	Bain, 1996
Ivermectin	0.1		Rhodamine 123	Caco-2 cells	Griffin, 2005
Ivermectin	-	0.06	Verapamil^2,4	Sf9 cell membranes	Lespine, 2006
Ketoconazole²	36		Calcein AM	Caco-2 cells	Eneroth, 2001
Ketoconazole²		24.9	Calcein AM	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Ketoconazole²	4.8		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Ketoconazole²	5.49		Colchicine	MDCK II-MDR1	Rautio, 2006
Ketoconazole²	5.6		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
Ketoconazole²	5.6		Daunorubicin	G185 cells	Wang, 2002
Ketoconazole²	1.2		Digoxin^1,3	Caco-2 cells	Choo, 2000
Ketoconazole²	1.4		Digoxin^1,3	Caco-2 cells	Wandel, 2000
Ketoconazole²	1.34		Digoxin^1,3	MDCKII-MDR1	Keogh, 2006
Ketoconazole²	3.07		Digoxin^1,3	MDCK II-MDR1	Rautio, 2006
Ketoconazole²	23.4		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Ketoconazole²	5.6		Rhodamine 123	MDR1 transfected NIH3T3-G185	Wang, 2001
Ketoconazole²	53.4		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
Ketoconazole²	13		Verapamil^2,4	Caco-2 cells	Doppenshmitt, 1998
Ketoconazole²		5.27	Vinblastine¹	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Ketoconazole²	6.34		Vinblastine¹	MDCK II-MDR1	Rautio, 2006
Lansoprazole	62.8		Digoxin^1,3	Caco-2 cells	Pauli-Magnus, 2001
Loperamide¹	16		Calcein AM	Caco-2 cells	Eneroth, 2001
Loperamide¹	2.5		Digoxin^1,3	Caco-2 cells	Wandel, 2002
Lopinavir	1.7		Rhodamine 123	MDR1 expressing Caco-2 cells	Vishnuvardhan, 2003
Lovastatin	26		Daunorubicin	MDR1 expressing 3T3-G185 cells	Wang, 2001
Lovastatin	32.7		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Lovastatin	67		Rhodamine 123	MDR1 expressing 3T3-G185 cells	Wang, 2001
Lovastatin Lactone	10		Calcein AM	MDR1 expressing MDCK cells	Chen, 2005
Lovastatin Lactone	114.4		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
Lsn335984, 42	0.9		Calcein AM	MDR1 expressing MDCK2 cells	Gannon, 2009
Manidipine	4.6		Daunorubicin	MDR1 expressing LLC-PK1 cells	Katoh, 2000
Manidipine	4.7		Digoxin^1,3	MDR1 expressing LLC-PK1 cells	Takara, 2002
Methadone	7.5		Rhodamine 123	Caco-2 cells	Stormer, 2001
Methoxyfenozide	44.3		Quinidine^1,2,4	LLC-PK1 cells	Miyata, 2016
Metoprolol	1440		Calcein AM	Caco-2 cells	Eneroth, 2001
Metoprolol	1300		Verapamil^2,4	Caco-2 cells	Doppenshmitt, 1998
Mibefradil	1.8		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Mibefradil	1.6		Digoxin^1,3	Caco-2 cells	Wandel, 2000
Mibefradil	1.2		Digoxin^1,3	Caco-2 cells	Ekins, 2002
Miconazole		55.5	Calcein AM	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Miconazole	3.5		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Miconazole		26.36	Vinblastine¹	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Midazolam	>50		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Morphine	>50		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Moxidectin	10		Rhodamine 123	Caco-2 cells	Griffin, 2005
N-norgallopamil	3.6		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
N-norgallopamil	4.9		LDS-751	NIH-3T3-G185 cells	Wang, 2001
N-norgallopamil	8.6		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
Nefazodone	4.7		Rhodamine 123	NIH-3T3-G185 cells	Stormer, 2001
Nelfinavir	3.4		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Nelfinavir	1.4		Daunorubicin	Caco-2 cells	Choo, 2000
Nicardipine	6.6		Calcein AM	NIH-3T3-G185 cells	Wang, 2001
Nicardipine	2.3		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Nicardipine	4.8		Calcein AM	MDR1 expressing A2780/ADR cells	Muller, 2007
Nicardipine	17.5		Daunorubicin	MDR1 expressing LLC-PK1 cells	Katoh, 2000
Nicardipine	3.2		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
Nicardipine	4.5		Digoxin^1,3	MDR1 expressing LLC-PK1 cells	Takara, 2002
Nicardipine	14.6		Fluo-3	NIH-3T3-G185 cells	Wang, 2001
Nicardipine	4.8		Hoechst 33342	MDR1 expressing A2780/ADR cells	Pick, 2008
Nicardipine	7.1		JC-1	NIH-3T3-G185 cells	Wang, 2001
Nicardipine	5.6		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Nicardipine	25.8		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
Nicardipine	11.7		Tetramethylrosamine	NIH-3T3-G185 cells	Wang, 2001
Nifedipine	113		Daunorubicin	NIH-G185 cells	Wang, 2001
Nifedipine	472		Digoxin^1,3	MDR1 expressing LLC-PK1 cells	Takara, 2002
Nifedipine	73		Vinblastine¹	F4-6P cells	Hollt, 1992
Niguldipine	0.7		Daunorubicin	MDR1 exressing CCRF-cEM/VCR 1000 cells	Jabeen, 2012
Nilvadipine	18		Digoxin^1,3	MDR1 expressing LLC-PK1 cells	Takara, 2002
Nisoldipine	44.1		Digoxin^1,3	MDR1 expressing LLC-PK1 cells	Takara, 2002
Nitrendipine	68.2		Digoxin^1,3	MDR1 expressing LLC-PK1 cells	Takara, 2002
Nobiletin	11.5		Daunorubicin	NIH-G185 cells	Wang, 2001
Norverapamil	0.9		Daunorubicin	NIH-G185 cells	Wang, 2001
Norverapamil	0.3		Digoxin^1,3	Caco-2 cells	Pauli-Magnus, 2000
o,p'-DDT	7.8		Verapamil^2,4	Sf9 cell membranes	Bircsak, 2013
Ophiobolin A	7.86		Digoxin^1,3	LLC-PK1 cells	Yoshida, 2006
Paclitaxel	54		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
Paclitaxel	53.9		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Paclitaxel	54		Rhodamine 123	MDR1 transfected NIH3T3-G185	Wang, 2001
Paclitaxel	70.2		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
Pantoprazole	17.9		Digoxin^1,3	Caco-2 cells	Pauli-Magnus, 2001
Parathion	229.8		Doxorubicin	B16/F10 cells	Bain, 1996
Pentachlorophenol	1.6		Calcein AM	MDCK-II cells	Georgantzopoulou, 2014
Phosalone	3		Calcein AM	NIH 3T3 cells	Pivcevic, 2006
Phosalone	96.4		Doxorubicin	B16/F10 cells	Bain, 1997
Pimozide	2.9		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Pindolol	1950		Verapamil^2,4	Caco-2 cells	Doppenshmitt, 1998
Piperine	74.1		Cyclosporine²	Caco-2 cells	Bhardwaj, 2002
Piperine	15.5		Digoxin^1,3	Caco-2 cells	Bhardwaj, 2002
p,p'-DDD	10.7		Verapamil^2,4	Sf9 cell membranes	Bircsak, 2013
p,p'-DDT	3.8		Verapamil^2,4	Sf9 cell membranes	Bircsak, 2013
Progesterone	121		Calcein AM	Caco-2 cells	Eneroth, 2001
Progesterone	47.9		Calcein AM	MDR1 expressing A2780/ADR cells	Muller, 2007
Progesterone	96.2		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
Progesterone	47.9		Hoechst 33342	MDR1 expressing A2780/ADR cells	Pick, 2008
Progesterone	88.1		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Progesterone	192.2		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
Propafenone⁴	0.3		Daunorubicin	MDR1 exressing CCRF-cEM/VCR 1000 cells	Jabeen, 2012
Propiconazole	3.6		Calcein AM	NIH 3T3 cells	Pivcevic, 2006
Propiconazole	122.9		N-methyl-quinidine	Human "K" cell inverted vesicles	Mazur, 2015
Propranolol	429		Calcein AM	Caco-2 cells	Eneroth, 2001
Propranolol	350		Verapamil^2,4	Caco-2 cells	Doppenshmitt, 1998
Quinacrine	14.4		Calcein AM	CEM cells	Tiberghien, 1996
Quinidine^1,2,4	30.5		Calcein AM	CEM cells	Tiberghien, 1996
Quinidine^1,2,4	157		Calcein AM	Caco-2 cells	Eneroth, 2001
Quinidine^1,2,4	5.6		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Quinidine^1,2,4	51.7		Colchicine	MDCK II-MDR1	Rautio, 2006
Quinidine^1,2,4	18.8		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
Quinidine^1,2,4	2.2		Digoxin^1,3	Caco-2 cells	Choo, 2000
Quinidine^1,2,4		3.23	Digoxin^1,3	Caco-2	Tang, 2002
Quinidine^1,2,4		8.59	Digoxin^1,3	MDCK-MDR1	Tang, 2002
Quinidine^1,2,4	9.52		Digoxin^1,3	MDR1 transfected LLC-PK1	Kakumoto, 2002
Quinidine^1,2,4		0.43	Digoxin^1,3	MDR1-expressing Caco-2 cells	Horie, 2003
Quinidine^1,2,4	9.4		Digoxin^1,3	MDCKII-MDR1	Keogh, 2006
Quinidine^1,2,4	14.9		Digoxin^1,3	MDCK II-MDR1	Rautio, 2006
Quinidine^1,2,4	1		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Quinidine^1,2,4		1.5	Paclitaxel	MDR1-expressing Caco-2 cells	Gao, 2001
Quinidine^1,2,4	33.9		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
Quinidine^1,2,4	340		Verapamil^2,4	Caco-2 cells	Doppenshmitt, 1998
Quinidine^1,2,4	22.9		Vinblastine¹	MDCK II-MDR1	Rautio, 2006
Quinidine^1,2,4	1.8		Ximelagatran	Caco-2 cells	Eriksson, 2006
Quinine	280		Calcein AM	Caco-2 cells	Eneroth, 2001
Quinine	167.8		Calcein AM	NIH-3T3-G185 cells	Wang, 2001
Quinine	22.6		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
Quinine	22.4		Digoxin^1,3	MDCKII-MDR1	Keogh, 2006
Quinine	112.4		Fluo-3	NIH-3T3-G185 cells	Wang, 2001
Quinine	159.3		JC-1	NIH-3T3-G185 cells	Wang, 2001
Quinine	74.4		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Quinine	87.6		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
Quinine	184.9		Tetramethylrosamine	NIH-3T3-G185 cells	Wang, 2001
Quinine	430		Verapamil^2,4	Caco-2 cells	Doppenshmitt, 1998
Ranitidine	>50		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Reserpine²	2.6		Calcein AM	NIH-3T3-G185 cells	Wang, 2001
Reserpine²		12.2	Calcein AM	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Reserpine²	3.2		Calcein AM	MDR1 expressing A2780/ADR cells	Muller, 2007
Reserpine²	0.5		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
Reserpine²		1.38	Digoxin^1,3	Caco-2	Tang, 2002
Reserpine²		11.5	Digoxin^1,3	MDCK-MDR1	Tang, 2002
Reserpine²		2.31	Digoxin^1,3	MDR1-expressing Caco-2 cells	Horie, 2003
Reserpine²	2.1		Fluo-3	NIH-3T3-G185 cells	Wang, 2001
Reserpine²	3.2		Hoechst 33342	MDR1 expressing A2780/ADR cells	Pick, 2008
Reserpine²	6.1		JC-1	NIH-3T3-G185 cells	Wang, 2001
Reserpine²	2.1		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Reserpine²	3.9		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
Reserpine²	5.3		Tetramethylrosamine	NIH-3T3-G185 cells	Wang, 2001
Reserpine²		0.97	Vinblastine¹	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Reversan	6.8		Calcein AM	KBV1 cells	Obreque-Balboa, 2016
Rhodamine 123	0.5		Verapamil^2,4	Caco-2 cells	Doppenshmitt, 1998
Ritonavir^2,4	12		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Ritonavir^2,4	15.7		Cyclosporine²	MDR1 expressing LLC-PK1 cells	Kumar, 2003
Ritonavir^2,4	3.8		Digoxin^1,3	Caco-2 cells	Choo, 2000
Ritonavir^2,4	28.2		Digoxin^1,3	MDCKII-MDR1	Keogh, 2006
Ritonavir^2,4	5		Digoxin^1,3	Caco-2 cells	Cook, 2010
Roxithromycin	15.4		Digoxin^1,3	Caco-2 cells	Eberl, 2007
Saquinavir	12		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Saquinavir	6.5		Digoxin^1,3	Caco-2 cells	Choo, 2000
SDZ 280-446	0.22		Calcein AM	CEM cells	Tiberghien, 1996
Selamectin	0.12		Rhodamine 123	Caco-2 cells	Griffin, 2005
Sertindole	6.5		Rhodamine 123	MDR1 expressing L5178 cells	Broccatelli, 2011
Simvastatin	9		Daunorubicin	MDR1 expressing 3T3-G185 cells	Wang, 2001
Simvastatin	8.9		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
Simvastatin	26.1		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Simvastatin	46		Rhodamine 123	MDR1 expressing 3T3-G185 cells	Wang, 2001
Simvastatin	56.8		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
Simvastatin lactone	10		Calcein AM	MDR1 expressing MDCK cells	Chen, 2005
Sirolimus	1.3		Rhodamine 123	Caco-2 cells	Wacher, 2002
Spironolactone	23.6		Daunorubicin	NIH-G185 cells	Wang, 2001
Sulfentanil	4.5		Digoxin^1,3	Caco-2 cells	Wandel, 2002
Talinolol¹	830		Verapamil^2,4	Caco-2 cells	Doppenshmitt, 1998
Tamoxifen	6.4		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
Tamoxifen	12.1		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Tamoxifen	7.1		Rhodamine 123	MDR1 transfected NIH3T3-G185	Wang, 2001
Tamoxifen	31.4		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
Tariquidar	0.2		Calcein AM	MDR1 expressing Kb-V1 cells	Puentes, 2011
Tariquidar	0.2		Calcein AM	KBV1 cells	Obreque-Balboa, 2016
Tebufenozide	21.5		Quinidine^1,2,4	LLC-PK1 cells	Miyata, 2016
Telithromycin	1.8		Digoxin^1,3	Caco-2 cells	Eberl, 2007
Terfenadine	1.4		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Terfenadine	1.8		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
Terfenadine	2.5		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Terfenadine	2.7		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
Terpinolene	481		Digoxin^1,3	LLC-PK1 cells	Yoshida, 2006
Tetrabromobisphenol A	22.9		[3H]N-methylquinidine	HEK293 cell membrane vesicles	Dankers, 2013
Tetraphenylphosphonium	490		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
Tetraphenylphosphonium	426.6		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Tranylcypromine	14000		Verapamil^2,4	Caco-2 cells	Doppenshmitt, 1998
Trifluoperazine	7.2		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
Trifluoperazine	6.3		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Trifluoperazine	10.9		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
Trimethoxybenzoylyohimbine		2.1	Verapamil^2,4	MDR1-expressing CEM/VLB100 cells	Shepard, 1998
Troleandomycin		483.3	Calcein AM	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Troleandomycin	68.3		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
Troleandomycin	78.2		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Troleandomycin	86.3		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
Troleandomycin		87.64	Vinblastine¹	MDR1-expressing LLC-PK1 cells	Ekins, 2002
Valinomycin	3.2		Daunorubicin	NIH-G185 cells	Wang, 2001
Valspodar²	0.41		Calcein AM	CEM cells	Tiberghien, 1996
Valspodar²		1.3	Calcein AM	CEM/VBL 100	Wigler, 1999
Valspodar²	3.2		Calcein AM	MDCK-II cells	Georgantzopoulou, 2014
Valspodar²	0.5		Daunorubicin	MDR1 exressing CCRF-cEM/VCR 1000 cells	Jabeen, 2012
Valspodar²	0.11		Digoxin^1,3	Caco-2 cells	Choo, 2000
Valspodar²	0.11		Digoxin^1,3	Caco-2 cells	Wandel, 2000
Verapamil^2,4	22.5		Calcein AM	CEM cells	Tiberghien, 1996
Verapamil^2,4	70		Calcein AM	Caco-2 cells	Eneroth, 2001
Verapamil^2,4	28.9		Calcein AM	NIH-3T3-G185 cells	Wang, 2001
Verapamil^2,4	6.3		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Verapamil^2,4	4.6		Calcein AM	MDR1 expressing A2780/ADR cells	Muller, 2007
Verapamil^2,4	4.6		Calcein AM	MDR1 expressing A2780/ADR cells	Muller, 2008
Verapamil^2,4	5.2		Calcein AM	MDR1 expressing A2780/ADR cells	Klinkhammer, 2009
Verapamil^2,4	14		Calcein AM	MDR1 expressing MDCK2 cells	Gannon, 2009
Verapamil^2,4	1.5		Calcein AM	NIH 3T3 cells	Pivcevic, 2006
Verapamil^2,4	0.5		Calcein AM	MDR1 expressing MDCK cells	Pellicani, 2012
Verapamil^2,4	63.9		Calcein AM	MDCK-II cells	Georgantzopoulou, 2014
Verapamil^2,4	17.3		Colchicine	MDCK II-MDR1	Rautio, 2006
Verapamil^2,4	4.2		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
Verapamil^2,4	2.1		Digoxin^1,3	Caco-2 cells	Choo, 2000
Verapamil^2,4	224		Digoxin^1,3	MDR1 expressing LLC-PK1 cells	Kawahara, 2000
Verapamil^2,4		8.11	Digoxin^1,3	Caco-2	Tang, 2002
Verapamil^2,4		15.1	Digoxin^1,3	MDCK-MDR1	Tang, 2002
Verapamil^2,4		0.88	Digoxin^1,3	MDR1-expressing Caco-2 cells	Horie, 2003
Verapamil^2,4	10.7		Digoxin^1,3	MDCK II-MDR1	Rautio, 2006
Verapamil^2,4	237		Digoxin^1,3	LLC-PK1 cells	Yoshida, 2006
Verapamil^2,4	3.2		Doxorubicin	B16/F10 cells	Bain, 1996
Verapamil^2,4	8.44		Fexofenadine^1,3	Caco-2	Petri, 2004
Verapamil^2,4	446.5		Fluo-3	NIH-3T3-G185 cells	Wang, 2001
Verapamil^2,4	6.6		Hoechst 33342	MDR1 expressing A2780/ADR cells	Muller, 2008
Verapamil^2,4	4.6		Hoechst 33342	MDR1 expressing A2780/ADR cells	Pick, 2008
Verapamil^2,4	1.7		Hoechst 33342	Hela cells	Cortes-Ciriano, 2013
Verapamil^2,4		29	Irinotecan	MDCK II-MDR1	Luo, 2002
Verapamil^2,4	42		JC-1	NIH-3T3-G185 cells	Wang, 2001
Verapamil^2,4	4.7		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Verapamil^2,4	1.8		N-methyl-quinidine	Human "K" cell inverted vesicles	Mazur, 2015
Verapamil^2,4		3	Paclitaxel	MDR1-expressing Caco-2 cells	Gao, 2001
Verapamil^2,4	4.2		Rhodamine 123	MDR1 transfected NIH3T3-G185	Wang, 2001
Verapamil^2,4	6.5		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
Verapamil^2,4	9.8		Rhodamine 123	MDR1 expressing MDCK cells	Pick, 2011
Verapamil^2,4	38.2		Tetramethylrosamine	NIH-3T3-G185 cells	Wang, 2001
Verapamil^2,4	1.5		Verapamil^2,4	Caco-2 cells	Doppenshmitt, 1998
Verapamil^2,4	33.5		Vinblastine¹	MDCK II-MDR1	Rautio, 2006
Verapamil^2,4	0.2		Vincristine	MDR1-expressing K562 vesicles	Noguchi, 2009
Verapamil^2,4	1.7		Ximelagatran	Caco-2 cells	Eriksson, 2006
Verapamil (R)	2.6		Paclitaxel	HCT15/CL02 cells	Lee, 2003
Verapamil (R)	5.5		Paclitaxel	MES-SA/DX5 cells	Lee, 2003
Verapamil (Racemic)	4.8		Paclitaxel	MES-SA/DX5 cells	Lee, 2003
Verapamil (S)	2.4		Paclitaxel	HCT15/CL02 cells	Lee, 2003
Verapamil (S)	5.3		Paclitaxel	MES-SA/DX5 cells	Lee, 2003
Vinblastine¹	34		Calcein AM	CEM cells	Tiberghien, 1996
Vinblastine¹	>50		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
Vinblastine¹	29		Calcein AM	MDR1 expressing MDCK cells	Chen, 2005
Vinblastine¹	10.5		Calcein AM	MDR1 expressing A2780/ADR cells	Muller, 2007
Vinblastine¹	30.1		Colchicine	MDCK II-MDR1	Rautio, 2006
Vinblastine¹	17.7		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
Vinblastine¹		140	Digoxin^1,3	MDR1-expressing MDCK cells	Tang, 2002
Vinblastine¹		15	Digoxin^1,3	MDR1-expressing Caco-2 cells	Horie, 2003
Vinblastine¹	17.8		Digoxin^1,3	MDCK II-MDR1	Rautio, 2006
Vinblastine¹	19.9		LDS-751	NIH-3T3-G185 cells	Wang, 2001
Vinblastine¹		36.5	Paclitaxel	MDR1-expressing Caco-2 cells	Gao, 2001
Vinblastine¹	18		Rhodamine 123	MDR1 transfected NIH3T3-G185	Wang, 2001
Vinblastine¹	29.5		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
Vinblastine¹	34		Verapamil^2,4	Caco-2 cells	Doppenshmitt, 1998
Vinblastine¹		2.1	Verapamil^2,4	MDR1-expressing CEM/VLB100 cells	Shepard, 1998
Vinblastine¹	89.7		Vinblastine¹	MDCK II-MDR1	Rautio, 2006
Vincristine	345		Calcein AM	Caco-2 cells	Eneroth, 2001
Vincristine		213	Digoxin^1,3	MDR1-expressing MDCK cells	Tang, 2002
Vincristine	86		Verapamil^2,4	Caco-2 cells	Doppenshmitt, 1998
Wk-X-50	0.8		Calcein AM	MDR1 expressing A2780/ADR cells	Muller, 2007
Zosuquidar²	0.07		Abacavir	MDCKII-MDR1	Shaik, 2007
Zosuquidar²	0.1		Daunorubicin	MDR1 exressing CCRF-cEM/VCR 1000 cells	Jabeen, 2012
Zosuquidar²	0.024		Digoxin^1,3	Caco-2 cells	Choo, 2000

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 (ABCB1/ABCG2)	Atazanavir/ritonavir	Glecaprevir	6.53	4.51	ND	ND	ND	ND	Yu, 2019	DDI 1
2	MDR1	Breviscapine	Fexofenadine^1,3	0.86	0.98		1.03	0.99	ND	Zhao, 2021	DDI 2
3	ABCB1/OATP1B1 (CYP3A4)	Cyclosporine²	Atorvastatin	15.3	13.7	ND	ND	ND	NS	Lemahieu, 2005	DDI 3
4	ABCB1/OATPs	Cyclosporine²	Docetaxel	7.3	5.7	ND	ND	ND	ND	Malingre, 2001	DDI 4
5	ABCB1/ABCG2/OATP1B1/OATP1B3	Cyclosporine²	Glecaprevir	5.08	4.51	ND	ND	ND	ND	Yu, 2019	DDI 5
6	ABCB1/OATPs	Cyclosporine²	Paclitaxel	8.5	2.0	ND	ND	ND	ND	Meerum, 1999	DDI 6
7	ABCB1/ABCG2/OATP1B1/OATP1B3	Cyclosporine²	Voxilaprevir	9.73	14.29	ND	ND	ND	ND	Yu, 2019	DDI 7
8	ABCB1	Dronedarone⁴	Digoxin^1,3	2.3	1.7	0.5	ND	ND	ND	Dronedarone Drug Label	DDI 8
9	ABCB1/ABCG2	Elacridar (GF120918)²	Topotecan	2.4	2.8	ND	ND	NS	ND	Kruijtzer, 2002	DDI 9
10	ABCB1/OATPs	Erythromycin	Simvastatin	6.2	3.5	ND	ND	NS	ND	Kantola, 1998	DDI 10
11	ABCB1/OATPs	Indinavir / Ritonavir^2,4	Fexofenadine^1,3	4.8	2.5	ND	0.2	0.7	ND	Kharasch, 2009	DDI 11
12	ABCB1	Itraconazole⁴	Digoxin^1,3	1.7	NS	0.8	ND	NS	ND	Jalava, 1997	DDI 12
13	ABCB1	Itraconazole⁴	Quinidine^1,2,4	2.4	1.6	0.5	ND	1.6	yes	Kaukonen, 1997	DDI 13
14	ABCB1	Lovastatin	Verapamil^2,4	1.6	1.3	ND	ND	NS	ND	Choi, 2010	DDI 14
15	ABCB1	Quinidine^1,2,4	Digoxin^1,3	ND	ND	0.7	0.6	ND	ND	Rameis, 1985; Hager, 1979	DDI 15
16	ABCB1	Ranolazine⁴	Digoxin^1,3	1.6	1.5	ND	ND	ND	ND	Jerling, 2006	DDI 16
17	ABCB1/OATPs	Ritonavir^2,4	Digoxin^1,3	1.9	ND	0.6	0.6	2.6	ND	Ding, 2004	DDI 17
18	ABCB1/OATPs	Ritonavir^2,4	Saquinavir	29.9	22.5	ND	ND	ND	ND	la, 2007	DDI 18
19	ABCB1/OATP1B1/OATP1B3 (CYP3A)	Simeprevir	Atorvastatin	2.12	1.7	ND	ND	ND	ND	Simeprevir NDA application	DDI 19
20	ABCB1	Valspodar²	Digoxin^1,3	3.0	2.4	0.2	0.3	ND	no	Kovarik, 1999	DDI 20
21	ABCB1	Verapamil^2,4	(R)-fexofenadine	2.9	2.2	ND	0.4	NS	ND	Sakugawa, 2009	DDI 21
22	ABCB1	Verapamil^2,4	(S)-fexofenadine	2.2	2.2	ND	0.5	NS	ND	Sakugawa, 2009	DDI 22
23	ABCB1/OATPs	Verapamil^2,4	Simvastatin	4.6	2.6	ND	ND	NS	ND	Kantola, 1998	DDI 23

The transporters are implicated by in vitro data and/or studies in humans with genetic polymorphisms of the transporter
DDI = Drug Drug Interaction
PK = pharmacokinetic
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
1 denotes drugs that can potentially be used as in vitro substrates for studies of the transporter as defined by the FDA as of March 2022
2 denotes drugs that can potentially be used as in vitro inhibitors for studies of the transporter as defined by the FDA as of March 2022
3 denotes drugs that can potentially be used as clinical substrates for studies of the transporter as defined by the FDA as of March 2022
4 denotes drugs that can potentially be used as clinical inhibitors for studies of the transporter as defined by the FDA as of March 2022