Table 2. The reversal of ABC transporter-mediated multidrug resistance (MDR) by TKIs.

TKIs that reverse MDR	Alternative name(s)	MDR-related ABC transporters involved	Clinical applications	Reference(s)
Imatinib	Gleevec, STI571	ABCB1/P-gp/MDR1, ABCG2/BCRP, ABCC1/MRP1, ABCC10/MRP7	CML, GISTs, Ph+ ALL, and others	[8], [42]-[46], [48]
Nilotinib	Tasigna, AMN107	ABCB1/P-gp/MDR1, ABCG2/BCRP, ABCC10/MRP7	Newly diagnosed CML, imatinib-resistant or -intolerant CML	[9], [47], [48]
Sunitinib	Sutent, SU11248	ABCB1/P-gp/MDR1, ABCG2/BCRP	RCC, imatinib-resistant GISTs, pNET	[11], [49], [50]
Erlotinib	Tarceva, OSI-774	ABCB1/P-gp/MDR1, ABCG2/BCRP, ABCC10/MRP7	Advanced NSCLC and pancreatic cancer	[12], [51], [53], [66]
Lapatinib	Tykerb, GW572016	ABCB1/P-gp/MDR1, ABCG2/BCRP, ABCC10/MRP7	HER2-positive advanced or metastatic breast cancer	[13], [52], [53]
Gefitinib	Iressa, ZD1839	ABCB1/P-gp/MDR1, ABCG2/BCRP	Advanced NSCLC	[14], [54]-[57]
Vandetanib	ZD6474	ABCB1/P-gp/MDR1, ABCG2/BCRP, ABCC1/MRP1	Metastatic medullary thyroid cancer	[15], [58], [59]
Sorafenib	Nexavar	ABCB1/P-gp/MDR1	Advanced RCC, advanced HCC	[16], [60], [61]
Apatinib	YN968D1	ABCB1/P-gp/MDR1, ABCG2/BCRP	-	[62]
BIBF 1120	-	ABCB1/P-gp/MDR1	-	[64]
AG1478	-	ABCB1/P-gp/MDR1, ABCG2/BCRP	-	[65], [66]
Cediranib	Recentin, AZD2171	ABCB1/P-gp/MDR1, ABCC1/MRP1	-	[67]
Canertinib	CI1033	ABCG2/BCRP	-	[28]

CML, chronic myelogenous leukemia; GISTs, gastrointestinal stromal tumors; ALL, acute lymphocytic leukemia; RCC, renal cell carcinoma; PNET, primitive neuroectodemal tumor; NSCLC, non-small cell lung cancer; HCC, hepatocellular carcinoma.