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. Author manuscript; available in PMC: 2013 Jun 17.
Published in final edited form as: Nat Rev Drug Discov. 2009 Mar;8(3):235–253. doi: 10.1038/nrd2792

Table 1.

Selected inhibitors of FGF signalling

Drug structure Function refs
Sunitinib graphic file with name nihms472127t1.jpg

  • A tyrosine kinase inhibitor that acts on FGFR in addition to many other RTKs

  • Inhibition occurs at concentrations in the low nanomolar range in vitro

  • 800 ng per ml plasma concentration inhibits FGFR, but only 50–100 ng per ml is needed for efficacy

 62
Suramin graphic file with name nihms472127t2.jpg

  • Mimics heparin and interferes with FGF–FGFR binding

  • Efficacious in a range of cancers but also has the dangerous side effect of coagulopathy

 103–107
Thalidomide graphic file with name nihms472127t3.jpg

  • Interferes with FGF2-induced angiogenesis

  • Phase II trials demonstrated its efficacy in treating cancer, including prostate and renal malignancies

 100–102
SU5402 graphic file with name nihms472127t4.jpg

  • SU5402, PD173074 and NDGA have shown efficacy against multiple myeloma cell lines through inhibition of the FGFR3 kinase domain

  • PD173074 has also shown in vitro efficacy against FGFR2-deregulated endometrial cancers

 63–65
PD173074 graphic file with name nihms472127t5.jpg
NDGA graphic file with name nihms472127t6.jpg

FGF, fibroblast growth factor; FGFR, fibroblast growth factor receptor; NDGA, norhydroguaiaretic acid; RTK, receptor tyrosine kinase.