UCSF home page | About UCSF | UCSF Medical Center

Skip to TransPortal content

Enlarge Text
Click to increase the text size. Restore Text
Click to restore original text size. Reduce Text
Click to decrease the text size.


Decrease the text size \| Restore text size \| Increase the text size

Furosemide

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
SLC22A8	OAT3	ND	S2-OAT3	Hasannejad, 2004

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
ABCC2	MRP2, cMOAT	Furosemide	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Furosemide	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Furosemide	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A11	OAT4	Furosemide	44.5		Estrone sulfate	S2-OAT4	Hasannejad, 2004
SLC22A8	OAT3	Furosemide	7.31		Estrone sulfate	S2-OAT3	Hasannejad, 2004
SLC22A5	OCTN2	Furosemide		1350	L-carnitine	MDCKII-hOCTN2	Diao, 2010
SLC22A6	OAT1	Furosemide	18		Para-aminohippurate	S2-OAT1	Hasannejad, 2004
SLC22A7	OAT2	Furosemide	603		Prostaglandin F2-alpha	S2-OAT2	Hasannejad, 2004
SLC22A8	OAT3	Furosemide	1.7		Sitagliptin	CHO-OAT3	Chu, 2007
SLC10A1	NTCP	Furosemide	15		Taurocholate	HeLa-NTCP	Kim, 1999
ABCB11	BSEP	Furosemide	>133		Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013

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	OATs	Cefiderocol	Furosemide	1.01	1.00	ND	ND	1.25	ND	Katsube, 2018	DDI 1
2	OATs	Furosemide	Lomefloxacin	1.1	NS	0.7	0.9	NS	ND	Sudoh, 1994	DDI 2
3	OATs	Nitisinone	Furosemide	1.72	1.12	ND	ND	ND	ND	Huledal, 2019	DDI 3
4	OATs/MRPs	Probenecid	Furosemide	2.7	1.5	0.3	0.4	1.7	ND	Vree, 1995	DDI 4

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