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Rifampin

Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

In Vitro Substrates

No substrate information.

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
SLC22A8	OAT3	Rifampin	30.2		Estrone sulfate	HEK293-OAT3	Parvez, 2016
SLC22A5	OCTN2	Rifampin		1150	L-carnitine	MDCKII-hOCTN2	Diao, 2009
SLC22A6	OAT1	Rifampin		62.2	Olmesartan	OAT1-expressing oocytes	Choi, 2011
SLC22A6	OAT1	Rifampin	48.1		PAH	HEK293-OAT1	Parvez, 2016
SLC22A6	OAT1	Rifampin	79.1		Para-aminohippurate	OAT1-expressing oocytes	Choi, 2011

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	OCTs	Rifampin	Metformin	1.13	1.10	1.16	NR	0.92	Yes	Cho, 2011	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