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Table 1 Fibroblast growth factor targeting therapies in clinical development

From: Challenges and opportunities in the targeting of fibroblast growth factor receptors in breast cancer

Drug class

Drug name

Target

Stage of clinical development

First-generation TKIs

TKI258 (dovitinib) [64]

FGFR, PDGFR and VEGFR

Phase III

 

BMS540215 (brivanib) [71]

FGFR and VEGFR

Phase II

 

BIBF 1120 [72]

FGFR, PDGFR and VEGFR

Phase III

 

Ponatinib [73]

ABL, FGFR, VEGFR2, PDGFRα, FLT3

Phase II

 

E7080 [74]

VEFGR, PDGFR, FGFR, KIT and RET

Phase I

 

E3810 [75]

VEGFR1 to VEGFR3 and FGFR1 inhibitor

Phase I

 

Sulfatinib [76]

VEGFR and FGFR inhibitor

Phase I

Second-generation TKIs

AZD 4547 [77, 78]

Selective FGFR1, FGFR2 and FGFR3 inhibitor

Phase II

 

BGJ398 [79]

Selective pan-FGFR inhibitor

Phase I

FGFR antibodies

IMC-A1 [62]

FGFR1-IIIc-specific antibody

Preclinical

 

GP369 [35]

FGFR2 blocking antibody

Preclinical

 

PRO-001 [80]

FGFR3-specific blocking antibody

Preclinical

 

R3Mab [61]

FGFR3-specific antibody

Preclinical

FGFR ligand traps

FP-1039 [81]

FGF ligand trap (blocks multiple FGFs)

Phase I

  1. ABL, c-abl oncogene 1, non-receptor tyrosine kinase; FGF, fibroblast growth factor; FGFR, fibroblast growth factor receptor; FLT3, fms-related tyrosine kinase 3; KIT, Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog; PDGFR, platelet-derived growth factor receptor; RET, ret proto-oncogene; TKI, tyrosine kinase inhibitor; VEGFR, vascular endothelial growth factor receptor.