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Lovastatin

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)	Substrate used	Cell System	Reference
ABCB1	MDR1, P-gp	Lovastatin	26	Daunorubicin	MDR1 expressing 3T3-G185 cells	Wang, 2001
SLCO2B1	OATP2B1, OATP-B	Lovastatin	9.92	Dibromofluorescein	HEK293-OATP2B1	Unger, 2020
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Lovastatin	4	Estradiol-17beta-glucuronide	HEK-OATP1B1	Chen, 2005
ABCC2	MRP2, cMOAT	Lovastatin	>133	Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Lovastatin	>133	Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Lovastatin	>133	Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCB1	MDR1, P-gp	Lovastatin	32.7	LDS-751	NIH-3T3-G185 cells	Wang, 2001
ABCB1	MDR1, P-gp	Lovastatin	67	Rhodamine 123	MDR1 expressing 3T3-G185 cells	Wang, 2001
ABCB11	BSEP	Lovastatin	19.3	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	OATP1B1	Gemfibrozil	Lovastatin	2.79	2.81	ND	ND	ND	ND	Kyrklund, 2001	DDI 1
2	ABCB1	Lovastatin	Verapamil	1.6	1.3	ND	ND	NS	ND	Choi, 2010	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