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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.