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Vinblastine

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	18.99	MDR1-expressing Caco-2 cells	Hunter, 1993
ABCB1	MDR1, P-gp	19	Caco-2	Hunter, 1993
ABCB1	MDR1, P-gp	0.8	MDR1-containing proteoliposomes	Borgnia, 1996
ABCB1	MDR1, P-gp	99.4	MDR1-expressing LLC-PK1 cells	Lecureur, 2000
ABCB4	MDR3	ND	Nucleotide trapping assay with Sf9-MDR3 membranes	Smith, 2000
ABCB1	MDR1, P-gp	89.2	Caco-2	Tang, 2002
ABCB1	MDR1, P-gp	253	MDCK-MDR1	Tang, 2002
ABCC2	MRP2, cMOAT	137.3	MDCK II-MRP2	Tang, 2002
ABCB1	MDR1, P-gp	1.7	ATPase assay of Sf9-MDR1 liposomes	Kimura, 2007
ABCB1	MDR1, P-gp	146	MDR1-expressing oocytes	Jutabha, 2010

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
ABCB1	MDR1, P-gp	Vinblastine	34		Calcein AM	CEM cells	Tiberghien, 1996
ABCB1	MDR1, P-gp	Vinblastine	>50		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
mouse_Abcb1a	Mdr, Pgp, Pgy, Mdr3, P-gp, Abcb4, Mdr1a	Vinblastine	>50		Calcein AM	Mouse mdr1a expressing LLC-PK1 cells	Schwab, 2003
mouse_Abcb1b	mdr, Mdr1, Pgy1, Abcb1, Mdr1b, Pgy-1	Vinblastine	8		Calcein AM	Mouse mdr1b expressing LLC-PK1 cells	Schwab, 2003
ABCB1	MDR1, P-gp	Vinblastine	29		Calcein AM	MDR1 expressing MDCK cells	Chen, 2005
ABCC2	MRP2, cMOAT	Vinblastine	21		Calcein AM	MRP2-expressing MDCK cells	Chen, 2005
ABCB1	MDR1, P-gp	Vinblastine	10.5		Calcein AM	MDR1 expressing A2780/ADR cells	Muller, 2007
ABCB1	MDR1, P-gp	Vinblastine	30.1		Colchicine	MDCK II-MDR1	Rautio, 2006
ABCB1	MDR1, P-gp	Vinblastine	17.7		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
ABCB1	MDR1, P-gp	Vinblastine		140	Digoxin	MDR1-expressing MDCK cells	Tang, 2002
ABCB1	MDR1, P-gp	Vinblastine		15	Digoxin	MDR1-expressing Caco-2 cells	Horie, 2003
ABCB1	MDR1, P-gp	Vinblastine	17.8		Digoxin	MDCK II-MDR1	Rautio, 2006
ABCC4	MRP4	Vinblastine	35.1		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC2	MRP2, cMOAT	Vinblastine	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Vinblastine	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A5	OCTN2	Vinblastine		4.85	L-carnitine	MDCKII-hOCTN2	Diao, 2009
ABCB1	MDR1, P-gp	Vinblastine	19.9		LDS-751	NIH-3T3-G185 cells	Wang, 2001
ABCB4	MDR3	Vinblastine	ND		Not applicable	nucleotide trapping with MDR3-expressing Sf9 membranes	Smith, 2000
ABCB1	MDR1, P-gp	Vinblastine		36.5	Paclitaxel	MDR1-expressing Caco-2 cells	Gao, 2001
ABCB1	MDR1, P-gp	Vinblastine	18		Rhodamine 123	MDR1 transfected NIH3T3-G185	Wang, 2001
ABCB1	MDR1, P-gp	Vinblastine	29.5		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
ABCB11	BSEP	Vinblastine	>133		Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013
ABCB1	MDR1, P-gp	Vinblastine	34		Verapamil	Caco-2 cells	Doppenshmitt, 1998
ABCB1	MDR1, P-gp	Vinblastine		2.1	Verapamil	MDR1-expressing CEM/VLB100 cells	Shepard, 1998
ABCB1	MDR1, P-gp	Vinblastine	89.7		Vinblastine	MDCK II-MDR1	Rautio, 2006

Clinical Drug-Drug Interactions

No drug-drug interaction information.