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 | 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 |