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Saquinavir

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
ABCB1	MDR1, P-gp	15.4	Caco-2	Collett, 2004
SLCO1A2	OATP1A2, OATP-A	36.4	OATP1A2-expressing oocytes	Su, 2004
ABCB1	MDR1, P-gp	14.5	MDR1 transfected LLC-PK1	Woodahl, 2005

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	Saquinavir	37		1-methyl-4-phenylpyridinium (MPP+)	HEK293-OCT1	Jung, 2008
ABCB1	MDR1, P-gp	Saquinavir	12		Calcein AM	MDR1 expressing LLC-PK1 cells	Schwab, 2003
mouse_Abcb1a	Mdr, Pgp, Pgy, Mdr3, P-gp, Abcb4, Mdr1a	Saquinavir	>50		Calcein AM	Mouse mdr1a expressing LLC-PK1 cells	Schwab, 2003
mouse_Abcb1b	mdr, Mdr1, Pgy1, Abcb1, Mdr1b, Pgy-1	Saquinavir	>50		Calcein AM	Mouse mdr1b expressing LLC-PK1 cells	Schwab, 2003
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Saquinavir	2.1	1.8	Cholyl-glycylamido-fluorescein (CGamF)	CHO-OATP1B1	Annaert, 2010
SLCO1B3	OATP1B3, OATP8	Saquinavir	4.1	2.8	Cholyl-glycylamido-fluorescein (CGamF)	CHO-OATP1B3	Annaert, 2010
ABCB1	MDR1, P-gp	Saquinavir	6.5		Digoxin	Caco-2 cells	Choo, 2000
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Saquinavir	1.23		Estradiol-17beta-glucuronide	HeLa-OATP1B1	Tirona, 2003
SLCO1B3	OATP1B3, OATP8	Saquinavir	0.47		Estradiol-17beta-glucuronide	HEK-OATP1B3	Chiou, 2014
ABCC3	MRP3	Saquinavir	42		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Saquinavir	59		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC2	MRP2, cMOAT	Saquinavir	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLCO2B1	OATP2B1, OATP-B	Saquinavir	5.3	4	Estrone sulfate	Caco-2	Annaert, 2010
SLCO2B1	OATP2B1, OATP-B	Saquinavir	4.6		Estrone sulfate	MDCK II-OATP2B1	Kis, 2010
SLCO1A2	OATP1A2, OATP-A	Saquinavir	<10		Fexofenadine	HeLa-OATP1A2	Cvetkovic, 1999
ABCG2	BCRP, MXR	Saquinavir	27.4		Pheophorbide A	MDCK II-BCRP	Weiss, 2007
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Saquinavir		1.59	Pitavastatin	HEK293-OATP1B1	Hirano, 2006
ABCB11	BSEP	Saquinavir	4.9		Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A1	OCT1	Saquinavir	8.26		Tetraethylammonium	HeLa-OCT1	Zhang, 2000

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	ABCB1/OATPs	Ritonavir	Saquinavir	29.9	22.5	ND	ND	ND	ND	la, 2007	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