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Paclitaxel

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	16.5	MDR1-expressing Caco-2 cells	Walle, 1998
ABCB4	MDR3	ND	Nucleotide trapping assay with Sf9-MDR3 membranes	Smith, 2000
ABCB1	MDR1, P-gp	0.014	MDR1-expressing MCF7 cells	Jang, 2001
ABCB1	MDR1, P-gp	65	Caco-2	Collett, 2004
ABCB1	MDR1, P-gp	0.7	MDR1-expressing Sf9 vesicles	Takahashi, 2005
SLC22A7	OAT2	0.1428	OAT2-expressing oocytes	Kobayashi, 2005
SLCO1B3	OATP1B3, OATP8	6.79	OATP1B3-expressing oocytes	Smith, 2005
ABCB1	MDR1, P-gp	1.4	ATPase assay of Sf9-MDR1 liposomes	Kimura, 2007
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	0.6	OATP1B1-expressing oocytes	Svoboda, 2011

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
SLCO1B3	OATP1B3, OATP8	Paclitaxel	2	Amanitin	MDCK II-OATP1B3	Letschert, 2006
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Paclitaxel	50	Bromsulphthalein	MDCK II-OATP1B1	Letschert, 2006
SLCO1B3	OATP1B3, OATP8	Paclitaxel	4	Bromsulphthalein	MDCK II-OATP1B3	Letschert, 2006
SLCO2B1	OATP2B1, OATP-B	Paclitaxel	25	Bromsulphthalein	MDCK II-OATP2B1	Letschert, 2006
ABCB1	MDR1, P-gp	Paclitaxel	54	Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Paclitaxel	0.03	Estradiol-17beta-glucuronide	CHO-OATP1B1	Gui, 2008
SLCO1B3	OATP1B3, OATP8	Paclitaxel	0.5	Estradiol-17beta-glucuronide	CHO-OATP1B3	Gui, 2008
ABCC2	MRP2, cMOAT	Paclitaxel	>133	Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Paclitaxel	>133	Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Paclitaxel	>133	Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCB1	MDR1, P-gp	Paclitaxel	53.9	LDS-751	NIH-3T3-G185 cells	Wang, 2001
ABCB4	MDR3	Paclitaxel	ND	Not applicable	nucleotide trapping with MDR3-expressing Sf9 membranes	Smith, 2000
ABCB1	MDR1, P-gp	Paclitaxel	54	Rhodamine 123	MDR1 transfected NIH3T3-G185	Wang, 2001
ABCB1	MDR1, P-gp	Paclitaxel	70.2	Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
ABCB11	BSEP	Paclitaxel	24.4	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	ABCB1/OATPs	Cyclosporine	Paclitaxel	8.5	2.0	ND	ND	ND	ND	Meerum, 1999	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