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Doxorubicin

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	3	MDR1-containing proteoliposomes	Ambudkar, 1992
ABCG2	BCRP, MXR	5	ATP hydrolysis assay of BCRP-expressing Sf9 vesicles	Ozvegy, 2001
ABCB1	MDR1, P-gp	ND	MDR1 transfected LLC-PK1	Woodahl, 2009

* 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	Doxorubicin	160	150	Estradiol-17beta-glucuronide	HEK-OATP1B1	Karlgren, 2012
SLCO1B3	OATP1B3, OATP8	Doxorubicin	41	38	Estradiol-17beta-glucuronide	HEK293-OATP1B3	Karlgren, 2012
ABCC4	MRP4	Doxorubicin	19		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC2	MRP2, cMOAT	Doxorubicin	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Doxorubicin	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCB1	MDR1, P-gp	Doxorubicin		8.5	Paclitaxel	MDR1-expressing Caco-2 cells	Gao, 2001
ABCB11	BSEP	Doxorubicin	>133		Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A4	OCTN1	Doxorubicin	0.00931		Tetraethylammonium	KB-3-3-hOCTN1	Okabe, 2008
ABCB1	MDR1, P-gp	Doxorubicin	990		Verapamil	Caco-2 cells	Doppenshmitt, 1998

No drug-drug interaction information.