Inhibitor |
IC50 (μM) |
Ki (μM) |
Substrate used |
Cell System |
Reference |
5-fluorodeoxyuridine monophosphate |
|
1163 |
Carboxydichlorofluorescein |
MRP5-expressing HEK293 vesicles |
Pratt, 2006 |
5-nitro-2-(3-phenylpropylamino)-benzoic acid (NPPB) |
2 |
|
5-fluorodeoxyuridine monophosphate |
MRP5-expressing HEK293 vesicles |
Pratt, 2005 |
5-nitro-2-(3-phenylpropylamino)-benzoic acid (NPPB) |
0.102 |
|
Carboxydichlorofluorescein |
MRP5-expressing HEK293 vesicles |
Pratt, 2006 |
Benzbromarone |
150 |
|
9-(2-phosphonomethoxyethyl)adenine (PMEA) |
MRP4-expressing HEK293 vesicles |
Reid, 2003 |
Cyclic GMP |
960 |
|
5-fluorodeoxyuridine monophosphate |
MRP5-expressing HEK293 vesicles |
Pratt, 2005 |
Cyclic GMP |
4855.5 |
|
Carboxydichlorofluorescein |
MRP5-expressing HEK293 vesicles |
Pratt, 2006 |
Dipyridamole |
30 |
|
9-(2-phosphonomethoxyethyl)adenine (PMEA) |
MRP4-expressing HEK293 vesicles |
Reid, 2003 |
Glyburide |
15 |
|
5-fluorodeoxyuridine monophosphate |
MRP5-expressing HEK293 vesicles |
Pratt, 2005 |
Methotrexate |
780 |
|
5-fluorodeoxyuridine monophosphate |
MRP5-expressing HEK293 vesicles |
Pratt, 2005 |
Methotrexate |
|
1059 |
Carboxydichlorofluorescein |
MRP5-expressing HEK293 vesicles |
Pratt, 2006 |
MK-571 |
17 |
|
5-fluorodeoxyuridine monophosphate |
MRP5-expressing HEK293 vesicles |
Pratt, 2005 |
MK-571 |
200 |
|
9-(2-phosphonomethoxyethyl)adenine (PMEA) |
MRP4-expressing HEK293 vesicles |
Reid, 2003 |
MK-571 |
15.9 |
|
Carboxydichlorofluorescein |
MRP5-expressing HEK293 vesicles |
Pratt, 2006 |
Pemetrexed |
2110 |
|
5-fluorodeoxyuridine monophosphate |
MRP5-expressing HEK293 vesicles |
Pratt, 2005 |
Pemetrexed |
442 |
|
Carboxydichlorofluorescein |
MRP5-expressing HEK293 vesicles |
Pratt, 2006 |
Pemetrexed |
|
300 |
Carboxydichlorofluorescein |
MRP5-expressing HEK293 vesicles |
Pratt, 2006 |
Probenecid |
70 |
|
5-fluorodeoxyuridine monophosphate |
MRP5-expressing HEK293 vesicles |
Pratt, 2005 |
Probenecid |
200 |
|
9-(2-phosphonomethoxyethyl)adenine (PMEA) |
MRP4-expressing HEK293 vesicles |
Reid, 2003 |
Probenecid |
34 |
|
Carboxydichlorofluorescein |
MRP5-expressing HEK293 vesicles |
Pratt, 2006 |
Sildenafil |
580 |
|
5-fluorodeoxyuridine monophosphate |
MRP5-expressing HEK293 vesicles |
Pratt, 2005 |
Sildenafil |
80 |
|
9-(2-phosphonomethoxyethyl)adenine (PMEA) |
MRP4-expressing HEK293 vesicles |
Reid, 2003 |
Sildenafil |
|
0.267 |
Cyclic GMP |
MRP5-expressing V79 vesicles |
Jedlitschky, 2000 |
Sulfinpyrazone |
300 |
|
9-(2-phosphonomethoxyethyl)adenine (PMEA) |
MRP4-expressing HEK293 vesicles |
Reid, 2003 |
Sulfinpyrazone |
103.2 |
|
Carboxydichlorofluorescein |
MRP5-expressing HEK293 vesicles |
Pratt, 2006 |
Trequinsin |
580 |
|
5-fluorodeoxyuridine monophosphate |
MRP5-expressing HEK293 vesicles |
Pratt, 2005 |
Trequinsin |
30 |
|
9-(2-phosphonomethoxyethyl)adenine (PMEA) |
MRP4-expressing HEK293 vesicles |
Reid, 2003 |
Trequinsin |
218 |
|
Carboxydichlorofluorescein |
MRP5-expressing HEK293 vesicles |
Pratt, 2006 |
Trequinsin |
|
0.24 |
Cyclic GMP |
MRP5-expressing V79 vesicles |
Jedlitschky, 2000 |
Zaprinast |
20 |
|
5-fluorodeoxyuridine monophosphate |
MRP5-expressing HEK293 vesicles |
Pratt, 2005 |
Zaprinast |
250 |
|
9-(2-phosphonomethoxyethyl)adenine (PMEA) |
MRP4-expressing HEK293 vesicles |
Reid, 2003 |
Zaprinast |
32.3 |
|
Carboxydichlorofluorescein |
MRP5-expressing HEK293 vesicles |
Pratt, 2006 |
The transporters are implicated by in vitro data and/or studies in humans with genetic polymorphisms of the transporter
DDI = Drug Drug Interaction
PK = pharmacokinetic
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
1 denotes drugs that can potentially be used as in vitro substrates for studies of the transporter as defined by the FDA as of March 2022
2 denotes drugs that can potentially be used as in vitro inhibitors for studies of the transporter as defined by the FDA as of March 2022
3 denotes drugs that can potentially be used as clinical substrates for studies of the transporter as defined by the FDA as of March 2022
4 denotes drugs that can potentially be used as clinical inhibitors for studies of the transporter as defined by the FDA as of March 2022