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 | |
Gefitinib | EGFR | ABCB1, ABCG2 | NSCLC | 2003 | |
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 | |
Lapatinib | HER2, EGFR | ABCB1, ABCC1, ABCG2, ABCC10 | Breast cancer | 2007 | |
Linsitinib | IGF | ABCG2, ABCC10 | NA | Not approved | [121] |
Masitinib | Kit | ABCG2, ABCC10 | Mast cell tumor | Not approved | |
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 | |
Ponatinib | BCR-ABL | ABCB1, ABCG2, ABCC10 | CML | 2012 | |
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 | |
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 | |
Vatalanib | VEGFR | ABCB1, ABCG2 | Colorectal cancer | Not approved | [139] |
WHI-P154 | JAK | ABCG2 | NA | Not approved | [140] |