. 2015 Apr 4;17(4):802–812. doi: 10.1208/s12248-015-9757-1

Table II.

Summary of Novel Modulators Against MRPs

Name	Target	Drug classification	Effects on target MRPs		Mechanism of inhibition on target MRPs
Name	Target	Drug classification	In vitro	In vivo	Transcription	Expression	Function
Ibrutinib	MRP1	Bruton’s tyrosine kinase inhibitor	+(11)	+(11)	↔^a	↔	↓^b
Nilotinib	MRP7	BCR-Abl inhibitor	+(12)	+(12)	N/A	↔	↓
Imatinib	MRP7	BCR-Abl inhibitor	+(12)	N/A	N/A	↔	↓
Erlotinib	MRP7	EGFR and HER2 inhibitor	+(13,14)	N/A	N/A	↔	↓
Lapatinib	MRP7	EGFR inhibitor	+(14)	N/A	N/A	↔	↓
Tandutinib	MRP7	FLT3 inhibitor	+(15)	N/A	N/A	↔	↓
Masitinib	MRP7	c-Kit inhibitor, PDGFR inhibitor	+(16)	+(16)	N/A	↔	↓
Sildenafil and vardenafil	MRP7	PDE5 inhibitor	+(17)	N/A	N/A	↔	↓
Tariquidar	MRP7	P-gp (ABCB1) inhibitor	+(18)	N/A	↔	↓ (>24 h treatment)	↓
NVP-BHG712	MRP7	EphB4 inhibitor	+(19)	+(19)	N/A	↔	↓
GSH-conjugated catechol metabolite	MRP1 and MRP2	GSH-conjugated catechol metabolites	+(20)	N/A	N/A	N/A	↓
3ATA	MRP1-4, preferred selectivity for MRP1	Triterpene	+(21)	N/A	N/A	N/A	↓
miR-326	MRP1	miRNA	+(22)	N/A	↓	↓	↓
miR-297	MRP2	miRNA	+(23)	+(23)	↓	↓	↓

N/A study not conducted, MRP multidrug resistance proteins, EGFR epidermal growth factor receptor, PDGFR platelet-derived growth factor, PDE5 phosphodiesterase type 5, GSH glutathione

(+): this compound shows reversal activity on the targeted MRPs, superscript number showing the relevant reference

^a(↔): no significant alterations

^b(↓) downregulation or inhibition