Table 5. Agents target FGF2/FGFR in cancer.

Agent	Company	Target	Agent Type	Characteristics	Clinical Trial	Indication/Tested on	Ref.
FGF2 inhibitors
FP-1039/GSK3052230	Five Prime Pharmaceuticals (CA, USA)	FGF2	Protein	Ligand trap: prevents FGF2 from binding to receptors	Phase I (Ongoing) NCT01868022	Squamous non-small cell lung cancer, mesothelioma	[86]
Interferon-α	−	FGF2	Protein	Inhibits FGF2 expression and production	Phase II (ongoing) NCT00049530	Bladder cancer, melanoma	[87, 187]
miRNA 646	−	FGF2	miRNA	Downregulates FGF2	−	Osteosarcoma	[188]
Sm27	−	FGF2	Small molecule	Binds to heparin-binding site on FGF2 and prevents FGF2 interaction with receptors	−	Endothelial cells	[189]
Anvirzel	Nerium Biotechnology (Canada)	FGF2	Glycoside	Inhibits FGF2 export by affecting Na+/K+ pump	−	Prostate cancer	[190]
Pentraxin-3	−	FGF2	Protein	Inhibits FGF2 binding to FGFR	−	Pancreatic cancer	[191]
TNP-470/AGM-1470	−	FGF2	Antibiotic	Suppresses expression and production of FGF2	−	Bladder cancer	[192]
Pentosan Polysulfate (Elmiron)	Ortho-McNeil Pharmaceutical (NJ, USA)	FGF2	Small molecule	Blocks and inhibits activity of FGF2	−	Various advanced cancers	[193]
PI-88	Progen Pharmaceuticals (Australia)	FGF2	Small molecule	Binds and inhibits FGF2 associated angiogenesis	−	Liver cancer	[194]
Thalidomide	Celgene (NJ, USA)	FGF2	Small molecule	Inhibits FGF2 induced angiogenesis	−	Multiple cancers	[195]
PAMPS, PAS, PSS, PVS	−	FGF2	Sulfonic acid polymers	FGF2 Antagonists	−	Endothelial cells	[196]
Sirolimus (Rapamycin)	Pfizer (NY, USA)	FGF2	Small molecule	Inhibits FGF2 dependent angiogenesis and proliferation	−	Fibroblasts and endothelial cells	[197]
Suramin (Germanin)	Bayer (Germany)	FGF2	Small Molecule	FGF2 antagonist/reduced FGF2 expression	−	Multiple cancers	[198]
Platelet Factor 4	−	FGF2	Protein	FGF2 antagonist	−	Endothelial cells	[199]
Non-specific Tyrosine Kinase Inhibitors
Lenvatinib (Lenvima)	Eisai (Japan)	FGFR1, PDGFR, VEGFR	Small molecule	Tyrosine kinase and angiogenesis inhibitor	Approved	Progressive, radioactive iodine-refractory thyroid cancer	[200]
AP 24534 (Ponatinib, Iclusig)	ARIAD Pharmaceuticals (MA, USA)	BCR-ABL, FGFR1-4	Small molecule	Tyrosine kinase inhibitor	Approved	CML, ALL	[89]
Pazopanib (Votrient)	GlaxoSmithKline (England)	FGFR, PDGFR, VEGFR	Small molecule	Tyrosine kinase and angiogenesis inhibitor	Approved	Renal cell carcinoma, soft tissue sarcoma	[90]
Nintedanib (Vargatef, Ofev)	Boehringer Ingelheim (Germany)	FGFR1-3, PDGFR, VEGFR	Small molecule	Tyrosine kinase and angiogenesis inhibitor	Approved (EU)	Non-small-cell lung cancer	[201]
BMS582664 (Brivanib)	Bristol-Myers Squibb (NY, USA)	FGFR1, VEGFR1, VEGFR2	Small molecule	Tyrosine kinase and angiogenesis inhibitor	Phase I/II/III trials NCT00633789 NCT00355238 NCT00435669	Liver cancer, solid tumors	[202]
SU6668, TSU-68 (Orantinib)	SUGEN/Pfizer/Taiho Pharmaceutical (CA, USA/NY, USA/Japan)	FGFR, PDGFR, VEGFR2	Small molecule	Tyrosine kinase and angiogenesis inhibitor	Phase I/II NCT00024206 NCT00784290	Advanced solid tumors, liver cancer	[203, 204]
TKI-258, CHIR-258 (Dovitinib)	Novartis (Switzerland)	FGFR1-3, PDGFR, VEGFR	Small molecule	Tyrosine kinase and angiogenesis inhibitor	Phase II trials NCT01058434 NCT01831726 NCT01861197 NCT01732107 NCT01719549	Multiple cancers including relapsed MM, non-small cell lung cancer, bladder cancer, gastric cancer	[205]
E3810 (Lucitanib)	EOS/Clovis Oncology (India/CO, USA)	FGFR1-3, VEGFR	Small molecule	Tyrosine kinase inhibitor	PhaseI/II NCT01283945	Solid tumors	[206]
Specific FGFR inhibitors
Debio 1347	Debiopharm (Switzerland)	FGFR1-3	Small molecule	Inhibits FGFR autophosphorylation	Phase I NCT01948297	Advanced solid tumors	[97]
AZD 4547	AstraZeneca (England)	FGFR1-3	Small molecule	Tyrosine kinase inhibitor	Phase II NCT01795768	Gastric cancer, esophageal cancer, breast cancer	[98]
BGJ 398	Novartis (Switzerland)	FGFR1-3	Small molecule	Tyrosine kinase and angiogenesis inhibitor	Phase I NCT01004224	Advanced solid tumors	[207]
JNJ-42756493	Janssen Oncology (Belgium)	FGFR	Small molecule	Tyrosine kinase inhibitor	Phase I/II NCT01703481 NCT02365597	Urothelial cancer, glioma	[208]
ARQ 087	Arqule (MA, USA)	FGFR	Small molecule	Tyrosine kinase inhibitor	Phase I NCT01752920	Solid tumors	[209]
LY287445	LKT Laboratories (MN, USA)	FGFR1-4	Small molecule	Tyrosine kinase inhibitor	Phase I NCT01212107	Advanced tumors	[210]
TAS-120	Taiho Pharmaceuticals (Japan)	FGFR	Small molecule	Irreversible FGFR inhibitor	Phase I/II NCT02052778	Advanced solid tumors, multiple myeloma	[211]
MFGR1877S	Genentech/Roche (CA, USA/Switzerland)	FGFR3	Antibody	Inhibits FGFR3 mediated cell proliferation	Phase I NCT01363024 NCT01122875	Solid tumors, multiple myeloma	[212, 213]
BAY 1179470	Bayer (NJ, USA)	FGFR2	Antibody	Inhibits FGFR2 mediated cell proliferation	Phase I NCT01881217	Advanced, refractory solid tumors	[100]
PD 161570	Parke-Davis/Pfizer (NY, USA)	FGFR	Small molecule	Tyrosine kinase and receptor phosphorylation inhibitor	−	Ovarian cancer	[214]
PD 173074	Parke-Davis/Pfizer (NY, USA)	FGFR	Small molecule	Tyrosine kinase and angiogenesis inhibitor	−	Urothelial carcinoma	[215]
PD 166285 dihydrochloride	Parke-Davis/Pfizer (NY, USA)	FGFR	Small molecule	Tyrosine kinase and angiogenesis inhibitor	−	Small cell lung cancer	[215, 216]
PD 166866	Parke-Davis/Pfizer (NY, USA)	FGFR1	Small molecule	Tyrosine kinase and angiogenesis inhibitor	−	Small cell lung cancer	[217, 218]
FIIN hydrochloride	−	FGFR1-4	Small molecule	Irreversible FGFR inhibitor	−	Cancer cell lines	[219]
SU 5402	−	FGFR, VEGFR	Small molecule	Tyrosine kinase and angiogenesis inhibitor	−	Urothelial carcinoma	[215]
SSR128129E	−	FGFR	Small molecule	Binds extracellular domain. Inhibits FGFR signaling	−	Endothelial cells, cancer cell lines	[220, 221]