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

Irbesartan

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
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	0.695	HEK-OATP1B1	Chapy, 2015
SLCO1B3	OATP1B3, OATP8	11.9	HEK293-OATP1B3	McFeely, 2019

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
SLC22A6	OAT1	Irbesartan	0.039		Bestatin	HEK293-OAT1	Huo, 2014
SLC22A8	OAT3	Irbesartan	0.41		Bestatin	HEK293-OAT3	Huo, 2014
SLCO2B1	OATP2B1, OATP-B	Irbesartan	1.3		Dibromofluorescein	HEK293-OATP2B1	Unger, 2020
ABCC3	MRP3	Irbesartan	21.1		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Irbesartan	83.2		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Irbesartan	4.65		Estrone sulfate	HEK-OATP1B1	Pei, 2018
SLC15A1	PEPT1	Irbesartan		230	Glycylsarcosine	Caco-2	Knutter, 2009
ABCB11	BSEP	Irbesartan	7.31		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	OATP1B1	Irbesartan	Repaglinide	1.33	1.84	ND	ND	NS	Yes	Pei, 2018	DDI 1

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