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Zidovudine

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
SLC22A7	OAT2	26.8	S2-OAT2	Takeda, 2002
SLC22A6	OAT1	45.9	S2-OAT1	Takeda, 2002
SLC22A8	OAT3	145	S2-OAT3	Takeda, 2002
SLC22A11	OAT4	152	S2-OAT4	Takeda, 2002

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
SLC22A1	OCT1	Zidovudine	0.0002		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT1	Minuesa, 2009
ABCC2	MRP2, cMOAT	Zidovudine	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Zidovudine	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Zidovudine	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A5	OCTN2	Zidovudine		2140	L-carnitine	MDCKII-hOCTN2	Diao, 2009
SLC22A5	OCTN2	Zidovudine		2140	L-carnitine	MDCKII-hOCTN2	Diao, 2010
ABCB11	BSEP	Zidovudine	>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/OCTs	Cotrimoxazole (trimethoprim/sulfamethoxazole)	Zidovudine	NS	ND	0.4	NS	NS	ND	Chatton, 1992	DDI 1
2	OCTs	Trimethoprim	Zidovudine	NS	ND	0.5	NS	NS	ND	Chatton, 1992	DDI 2

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