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Levofloxacin

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	3000	MDR1-expressing LLC-PK1 cells	Ito, 1997
ABCB1	MDR1, P-gp	5600	MDR1-expressing Caco-2 cells	Yamaguchi, 2000
SLCO1A2	OATP1A2, OATP-A	136	OATP1A2-expressing oocytes	Maeda, 2007

* 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	Levofloxacin	30.3		1-methyl-4-phenylpyridinium (MPP+)	HEK293-OCT1	Parvez, 2016
SLC47A1	MATE1	Levofloxacin	17.9		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-MATE1	Wittwer, 2013
ABCC2	MRP2, cMOAT	Levofloxacin	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Levofloxacin	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Levofloxacin	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A5	OCTN2	Levofloxacin	6800		L-carnitine	Caco-2 cells expressing OCTN2	Hirano, 2006
SLC22A5	OCTN2	Levofloxacin		3000	L-carnitine	BeWo cells expressing OCTN2	Hirano, 2008
SLC22A5	OCTN2	Levofloxacin		1900	L-carnitine	MDCKII-hOCTN2	Diao, 2009
SLC22A5	OCTN2	Levofloxacin		1890	L-carnitine	MDCKII-hOCTN2	Diao, 2010
SLC22A1	OCT1	Levofloxacin	22.6		Metformin	HEK293-OCT1	Parvez, 2016
ABCB11	BSEP	Levofloxacin	>133		Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013

No drug-drug interaction information.