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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]