Table 1.

Current clinical development status of FGF/FGFR-targeting anticancer agents

CompoundCompanyTargetClinical development (indication)
Small-molecule tyrosine kinase inhibitors: mixed pharmacology
BrivanibBristol-Myers SquibbFGFR, VEGFRPhase III (CRC, HCC, liver)
DovitinibNovartisFGFR, PDGFR, VEGFR, FLT3, c-KITPhase III (RCC)
LenvatinibEisaiFGFR, PDGFR, VEGFRPhase III (melanoma, thyroid)
MasitinibAB ScienceFGFR3, PDGFR, c-KITPhase III (GIST, melanoma, MM, pancreatic)
NintedanibBoehringer IngelheimFGFR, PDGFR, VEGFRPhase III (NSCLC, ovarian)
PazopanibGlaxoSmithKlineFGFR1, FGFR3, VEGFR, PDGFR, c-KITPhase III (breast, lung, ovarian, RCC, STS)
PI-88ProgenFGF1, FGF2, VEGFPhase III (HCC, liver)
RegorafenibBayerFGFR, PDGFR, VEGFR, c-KIT, RETPhase III (GIST, CRC)
TSU 68PfizerFGFR, KDR, PDGFR, VEGFR2Phase III (HCC)
ENMD-2076EntremedFGFR1, KDR, FGFR2, PDGFR, VEGFR, FLT3, c-KIT, Aurora K, FLT3Phase II (ovarian)
PonatinibAriadFGFR, PDGFR, VEGFRPhase II (AML, CML)
E3810EisaiFGFR1, VEGFRPhase I (solid tumors)
PBI-05204Phoenix BioFGF2, AKT, NF-κB, p70S6KPhase I (solid tumors)
Small-molecule tyrosine kinase inhibitors: FGFR selective
AZD4547AstraZenecaFGFR1–3Phase II (breast, gastric)
BGJ398NovartisFGFR1–3Phase I (solid tumors)
LY2874455Eli LillyFGFR1–4Phase I (solid tumors)
FGFR antibodies
RG7444RocheFGFR3Phase I (MM)
FGF-ligand traps
FP-1039Five Prime TherapeuticsFGF1, FGF2, FGF4Phase II (endometrial)

Abbreviations: AML, acute myeloid leukemia; CML, chronic myeloid leukemia; CRC, colorectal cancer; FLT3, fms-like tyrosine kinase receptor-3; GIST, gastrointestinal stromal tumor; KDR, kinase insert domain receptor; MM, multiple myeloma; RCC, renal cell carcinoma; RET, REarranged during Transfection; STS, soft tissue sarcoma.

Source: www.ClinicalTrials.gov (accessed December 15, 2011).