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Table 3 TKIs function as inhibitors of ABC transporters

From: Tyrosine kinase inhibitors enhanced the efficacy of conventional chemotherapeutic agent in multidrug resistant cancer cells

TKIs Target ABC transporter inhibitor Applications Approved by FDA Reference
Afatinib EGFR,HER2 ABCG2 NSCLC 2013 [107]
AG1478 EGFR ABCB1, ABCG2 NA Not approved [108]
Alectinib ALK ABCB1, ABCG2 NSCLC 2015 [90]
Apatinib VEGFR ABCB1, ABCG2 Gastric carcinoma Not approved [109]
AST1306 EGFR ABCG2 NA Not approved [110]
Axitinib VEGFR, PDGFR ABCG2 RCC 2012 [111]
Bosutinib BCR-ABL,Src ABCG2 CML 2012 [82]
Cabozantinib VEGFR, Kit ABCG2 Thyroid cancer 2011 [112]
Canertinib EGFR ABCB1, ABCG2 NA Not approved [113]
Cediranib VEGFR ABCB1, ABCC1 NA Not approved [114]
CEP-33779 JAK ABCB1 NA Not approved [115]
Ceritinib ALK ABCB1, ABCG2 NSCLC 2014 [116]
Crizotinib ALK ABCB1 NSCLC 2011 [117]
Dasatinib BCR-ABL, Src ABCB1, ABCG2 CML 2006 [81]
EKI785 EGFR ABCB1, ABCC1 NA Not approved [94]
Erlotinib EGFR ABCB1, ABCG2, ABCC10 NSCLC 2004 [84, 87]
Gefitinib EGFR ABCB1, ABCG2 NSCLC 2003 [75, 118]
GW2974 EGFR ABCB1, ABCG2 NA Not approved [119]
GW583340 EGFR ABCB1, ABCG2 NA Not approved [119]
Ibrutinib BTK ABCC1 Lymphoma 2013 [91]
Icotinib EGFR ABCG2 NSCLC 2011 [120]
Imatinib BCR-ABL ABCB1, ABCC1, ABCG2, ABCC10 CML, GIST 2001 [76, 77, 88, 94]
Lapatinib HER2, EGFR ABCB1, ABCC1, ABCG2, ABCC10 Breast cancer 2007 [84,85,86]
Linsitinib IGF ABCG2, ABCC10 NA Not approved [121]
Masitinib Kit ABCG2, ABCC10 Mast cell tumor Not approved [122, 123]
Motesanib VEGFR ABCB1, ABCG2 NA Not approved [124]
Neratinib HER2, EGFR ABCB1 Breast cancer 2017 [92]
Nilotinib BCR-ABL ABCB1, ABCG2, ABCC10 CML 2007 [78]
Nintedanib VEGFR, PDGFR ABCB1 NSCLC 2014 [125]
Osimertinib EGFR ABCB1, ABCG2 NSCLC 2015 [93]
PD173074 VEGFR ABCB1, ABCC10 NA Not approved [126, 127]
Ponatinib BCR-ABL ABCB1, ABCG2, ABCC10 CML 2012 [128, 129]
Quizartinib FLT3 ABCG2 AML Not approved [130]
Regorafenib VEGFR ABCB1 GIST 2012 [131]
Saracatinib Src ABCB1 NA Not approved [132]
Sorafenib VEGFR, PDGFR ABCB1, ABCC2, ABCC4, ABCG2 RCC, HCC 2005 [133]
Sunitinib VEGFR, PDGFR ABCB1, ABCG2 GIST, RCC 2006 [16, 89]
Tandutinib FLT3 ABCG2 NA Not approved [134]
Telatinib VEGFR ABCG2 NA Not approved [135]
Trametinib MEK ABCB1 Melanoma 2013 [136]
Vandetanib VEGFR, EGFR ABCB1, ABCC1, ABCG2 Thyroid cancer 2011 [137, 138]
Vatalanib VEGFR ABCB1, ABCG2 Colorectal cancer Not approved [139]
WHI-P154 JAK ABCG2 NA Not approved [140]