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Lopinavir

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
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Lopinavir	0.74	0.32	Atorvastatin	HEK-OATP1B1	Karlgren, 2012
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Lopinavir	0.5	0.5	Cholyl-glycylamido-fluorescein (CGamF)	CHO-OATP1B1	Annaert, 2010
SLCO1B3	OATP1B3, OATP8	Lopinavir	2	1.4	Cholyl-glycylamido-fluorescein (CGamF)	CHO-OATP1B3	Annaert, 2010
ABCC3	MRP3	Lopinavir	21		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Lopinavir	47		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC2	MRP2, cMOAT	Lopinavir	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLCO2B1	OATP2B1, OATP-B	Lopinavir	0.72		Estrone sulfate	MDCK II-OATP2B1	Kis, 2010
ABCG2	BCRP, MXR	Lopinavir	7.66		Pheophorbide A	MDCK II-BCRP	Weiss, 2007
ABCB1	MDR1, P-gp	Lopinavir	1.7		Rhodamine 123	MDR1 expressing Caco-2 cells	Vishnuvardhan, 2003
ABCG2	BCRP, MXR	Lopinavir	8.7		Rosuvastatin	polarized Caco-2 monolayer	Elsby, 2016
ABCB11	BSEP	Lopinavir	17.3		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	OATPs	Lopinavir / Ritonavir	Rosuvastatin	2.1	4.7	ND	0.5	NS	yes	Kiser, 2008	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