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Cyclosporine

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	8.4	MDR1-expressing LLC-PK1 cells	Saeki, 1993
ABCB1	MDR1, P-gp	3.8	MDR1-expressing Caco-2 cells	Fricker, 1996

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
SLCO1B3	OATP1B3, OATP8	Cyclosporine	0.3		Amanitin	MDCK II-OATP1B3	Letschert, 2006
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Cyclosporine	1.88	0.82	Atorvastatin	HEK-OATP1B1	Karlgren, 2012
ABCG2	BCRP, MXR	Cyclosporine	1.4		Basal activity	High Five insect cell crude membranes	Pawarode, 2007
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Cyclosporine	0.3		Bosentan	CHO-OATP1B1	Treiber, 2007
SLCO1B3	OATP1B3, OATP8	Cyclosporine	0.8		Bosentan	CHO-OATP1B1	Treiber, 2007
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Cyclosporine	3.5		Bromsulphthalein	MDCK II-OATP1B1	Letschert, 2006
SLCO1B3	OATP1B3, OATP8	Cyclosporine	0.3		Bromsulphthalein	MDCK II-OATP1B3	Letschert, 2006
SLCO2B1	OATP2B1, OATP-B	Cyclosporine	20		Bromsulphthalein	MDCK II-OATP2B1	Letschert, 2006
ABCB1	MDR1, P-gp	Cyclosporine	3.4		Calcein AM	CEM cells	Tiberghien, 1996
ABCB1	MDR1, P-gp	Cyclosporine		1.8	Calcein AM	MDR1-expressing CEM/VLB100 cells	Wigler, 1999
ABCB1	MDR1, P-gp	Cyclosporine	7		Calcein AM	Caco-2 cells	Eneroth, 2001
ABCB1	MDR1, P-gp	Cyclosporine	1.7		Calcein AM	NIH-3T3-G185 cells	Wang, 2001
ABCB1	MDR1, P-gp	Cyclosporine		4.66	Calcein AM	MDR1-expressing LLC-PK1 cells	Ekins, 2002
ABCB1	MDR1, P-gp	Cyclosporine	0.8		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
mouse_Abcb1a	Mdr, Pgp, Pgy, Mdr3, P-gp, Abcb4, Mdr1a	Cyclosporine	4.8		Calcein AM	Mouse mdr1a expressing LLC-PK1 cells	Schwab, 2003
mouse_Abcb1b	mdr, Mdr1, Pgy1, Abcb1, Mdr1b, Pgy-1	Cyclosporine	0.7		Calcein AM	Mouse mdr1b expressing LLC-PK1 cells	Schwab, 2003
ABCC2	MRP2, cMOAT	Cyclosporine	10		Calcein AM	MDCK II-MRP2	Wortelboer, 2003
ABCB1	MDR1, P-gp	Cyclosporine	9.3		Calcein AM	MDR1 expressing MDCK2 cells	Tong, 2007
ABCB1	MDR1, P-gp	Cyclosporine	1.4		Calcein AM	MDR1 expressing A2780/ADR cells	Muller, 2007
ABCB1	MDR1, P-gp	Cyclosporine	1.4		Calcein AM	MDR1 expressing A2780/ADR cells	Muller, 2008
ABCC2	MRP2, cMOAT	Cyclosporine	13.6		Calcein AM	MRP2-expressing MDCK-II cells	Leyers, 2008
ABCB1	MDR1, P-gp	Cyclosporine	1.4		Calcein AM	MDR1 expressing A2780/ADR cells	Klinkhammer, 2009
ABCB1	MDR1, P-gp	Cyclosporine	0.9		Calcein AM	Doxorubicin-resistant A2780 adr cells	Juvale, 2013
ABCB1	MDR1, P-gp	Cyclosporine	0.9		Calcein AM	MDR1 expressing A2780/ADR cells	Kohler, 2015
ABCC2	MRP2, cMOAT	Cyclosporine	20		Calcein AM	MRP2-expressing MDCK-II cells	Baiceanu, 2016
ABCC2	MRP2, cMOAT	Cyclosporine	25.6		Calcein AM	MRP2-expressing MDCK-II cells	Baiceanu, 2016
ABCB1	MDR1, P-gp	Cyclosporine	1.2		Calcein AM	MDR1 expressing A2780/ADR cells	Krapf, 2017
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Cyclosporine		0.238	Cerivastatin	MDCK II-OAT1B1	Shitara, 2003
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Cyclosporine		2.32	Cilostazol	HEK-OATP1B1	Wang, 2017
ABCB1	MDR1, P-gp	Cyclosporine	1.36		Colchicine	MDCK II-MDR1	Rautio, 2006
ABCB1	MDR1, P-gp	Cyclosporine	1.4		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
ABCB1	MDR1, P-gp	Cyclosporine	0.1		Daunorubicin	MDR1 exressing CCRF-cEM/VCR 1000 cells	Jabeen, 2012
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Cyclosporine	0.5	0.051	Demethylphalloin	HEK293 cells	Fehrenbach, 2003
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Cyclosporine		0.116	Dichlorofluorescein	HEK-OATP1B1	Izumi, 2016
ABCB1	MDR1, P-gp	Cyclosporine	3.7		Digoxin	MDR1 expressing LLC-PK1 cells	Kusunoki, 1998
ABCB1	MDR1, P-gp	Cyclosporine	1.3		Digoxin	Caco-2 cells	Choo, 2000
ABCB1	MDR1, P-gp	Cyclosporine		0.46	Digoxin	Caco-2	Tang, 2002
ABCB1	MDR1, P-gp	Cyclosporine		2.18	Digoxin	MDCK-MDR1	Tang, 2002
ABCB1	MDR1, P-gp	Cyclosporine		0.35	Digoxin	MDR1-expressing Caco-2 cells	Horie, 2003
ABCB1	MDR1, P-gp	Cyclosporine	1.6		Digoxin	MDCK II-MDR1	Rautio, 2006
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Cyclosporine	0.37		Estradiol-17beta-glucuronide	HeLa-OATP1B1	Tirona, 2003
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Cyclosporine	0.05		Estradiol-17beta-glucuronide	HEK-OATP1B1	Hinton, 2008
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Cyclosporine	1.4	1.3	Estradiol-17beta-glucuronide	HEK-OATP1B1	Karlgren, 2012
SLCO1B3	OATP1B3, OATP8	Cyclosporine	1.3	1.2	Estradiol-17beta-glucuronide	HEK293-OATP1B3	Karlgren, 2012
ABCC2	MRP2, cMOAT	Cyclosporine	14.5		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Cyclosporine	23		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Cyclosporine	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCG2	BCRP, MXR	Cyclosporine	13.4	6.7	Estrone sulfate	BCRP membrane vesicles	Xia, 2007
ABCB1	MDR1, P-gp	Cyclosporine	2.4		Fluo-3	NIH-3T3-G185 cells	Wang, 2001
ABCB11	BSEP	Cyclosporine	0.93		Glycocholate	BSEP-expressing Sf9 vesicles	Kis, 2009
ABCB1	MDR1, P-gp	Cyclosporine	1.4		Hoechst 33342	MDR1 expressing A2780/ADR cells	Muller, 2008
ABCB1	MDR1, P-gp	Cyclosporine	1.4		Hoechst 33342	MDR1 expressing A2780/ADR cells	Pick, 2008
ABCB1	MDR1, P-gp	Cyclosporine	4.3		JC-1	NIH-3T3-G185 cells	Wang, 2001
ABCB1	MDR1, P-gp	Cyclosporine	1.8		LDS-751	NIH-3T3-G185 cells	Wang, 2001
ABCC1	MRP1	Cyclosporine	5		Leukotriene C4	MRP1-expressing HeLa vesicles	Leier, 1994
ABCC2	MRP2, cMOAT	Cyclosporine		4.7	Leukotriene C4	MRP2-expressing LLC-PK1 vesicles	Chen, 1999
ABCG2	BCRP, MXR	Cyclosporine		7.8	Methotrexate	BCRP membrane vesicles	Xia, 2007
ABCC2	MRP2, cMOAT	Cyclosporine		21	Monoglucuronosyl bilirubin	MRP2-expressing HEK vesicles	Kamisako, 1999
ABCB4	MDR3	Cyclosporine	ND		Not applicable	nucleotide trapping with MDR3-expressing Sf9 membranes	Smith, 2000
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Cyclosporine		0.24	Pitavastatin	HEK293-OATP1B1	Hirano, 2006
ABCB1	MDR1, P-gp	Cyclosporine	1.4		Rhodamine 123	MDR1 transfected NIH3T3-G185	Wang, 2001
ABCB1	MDR1, P-gp	Cyclosporine	1.7		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
ABCB1	MDR1, P-gp	Cyclosporine	0.7		Rhodamine 123	MDR1 expressing L5178 cells	Broccatelli, 2011
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Cyclosporine	2.2		Rosuvastatin	OATP1B1-expressing oocytes	Simonson, 2004
SLC10A1	NTCP	Cyclosporine	0.37		Rosuvastatin	HeLa-NTCP	Ho, 2006
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Cyclosporine	0.31		Rosuvastatin	HeLa-OATP1B1	Ho, 2006
SLCO1B3	OATP1B3, OATP8	Cyclosporine	0.06		Rosuvastatin	HeLa-OATP1B3	Ho, 2006
SLCO2B1	OATP2B1, OATP-B	Cyclosporine	0.07		Rosuvastatin	HEK293-OATP2B1	Ho, 2006
ABCG2	BCRP, MXR	Cyclosporine	3.7		Rosuvastatin	polarized Caco-2 monolayer	Elsby, 2016
ABCB11	BSEP	Cyclosporine	0.94		Taurochenodeoxycholate	BSEP-expressing Sf9 vesicles	Kis, 2009
SLC10A1	NTCP	Cyclosporine	1		Taurocholate	HeLa-NTCP	Kim, 1999
ABCB11	BSEP	Cyclosporine	8.4		Taurocholate	BSEP-expressing Sf9 vesicles	Kis, 2009
ABCB11	BSEP	Cyclosporine	18.9		Taurocholate	BSEP-expressing Sf9 vesicles	Kis, 2009
ABCB11	BSEP	Cyclosporine	0.5		Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013
ABCB1	MDR1, P-gp	Cyclosporine	2.1		Tetramethylrosamine	NIH-3T3-G185 cells	Wang, 2001
ABCB1	MDR1, P-gp	Cyclosporine		0.02	Verapamil	MDR1-expressing Sf9 vesicles	Rao, 1994
ABCB1	MDR1, P-gp	Cyclosporine	0.7		Verapamil	Sf9 cell membranes	Bircsak, 2013
ABCB1	MDR1, P-gp	Cyclosporine		1.3	Vinblastine	MDR1-expressing LLC-PK1 cells	Ekins, 2002
ABCC2	MRP2, cMOAT	Cyclosporine		8.11	Vinblastine	MDCK II-MRP2	Tang, 2002
ABCB1	MDR1, P-gp	Cyclosporine	6.18		Vinblastine	MDCK II-MDR1	Rautio, 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/OATP1B1 (CYP3A4)	Cyclosporine	Atorvastatin	15.3	13.7	ND	ND	ND	NS	Lemahieu, 2005	DDI 1
2	ABCB1/OATPs	Cyclosporine	Docetaxel	7.3	5.7	ND	ND	ND	ND	Malingre, 2001	DDI 2
3	OATP1B1/OATP1B3 (CYP3A4)	Cyclosporine	Fluvastatin	3.55	4.1	ND	0.31	NS	ND	Park, 2001	DDI 3
4	ABCB1/ABCG2/OATP1B1/OATP1B3	Cyclosporine	Glecaprevir	5.08	4.51	ND	ND	ND	ND	Yu, 2019	DDI 4
5	ABCB1/OATPs	Cyclosporine	Paclitaxel	8.5	2.0	ND	ND	ND	ND	Meerum, 1999	DDI 5
6	ABCG2/OATPs	Cyclosporine	Pitavastatin	4.6	6.6	ND	ND	ND	ND	Livalo Drug Label	DDI 6
7	OATP1B1, OATP1B3,OATP2B1	Cyclosporine	Pitavastatin	4.60	ND	ND	ND	ND		Gessner, 2019	DDI 7
8	ABCC2/OATP1B1	Cyclosporine	Pravastatin	9.93	7.78	ND	ND	0.75	ND	Hedman, 2004	DDI 8
9	OATP1B1 (CYP3A4)	Cyclosporine	Repaglinide	2.44	1.72	NS	ND	NS	NS	Kajosaari, 2005	DDI 9
10	ABCG2/OATPs	Cyclosporine	Rosuvastatin	5.0	10.6	ND	ND	ND	ND	Simonson, 2004	DDI 10
11	ABCG2/OATPs	Cyclosporine	Rosuvastatin	6.4	18.2	ND	ND	ND	ND	Simonson, 2004	DDI 11
12	ABCB1/ABCG2/OATP1B1/OATP1B3	Cyclosporine	Voxilaprevir	9.73	14.29	ND	ND	ND	ND	Yu, 2019	DDI 12

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