Table 3 Therapeutics targeting FGF signaling
Class | Drug | Targets | Diseases | Drug development |
|---|---|---|---|---|
Recombinant FGFs or FGF analogs | rmFGF1 | FGF1 receptor | T2DM | Preclinical |
rhFGF1 | FGF1 receptor | T2DM | Preclinical | |
rhFGF2 (trafermin) | FGF2 receptor | Skin ulcers Periodontitis | Approved Japan P3 (NCT01015404) | |
FGF7 (palifermin) | FGF7 receptor | Oral mucositis | Approved USA | |
FGF10 (repifermin) | FGF10 receptor | Mucositis | Clinical trials was terminated in 2004 | |
rhFGF18 (sprifermin) | FGF18 receptor | Osteoarthritis | P2 (NCT01919164) | |
FGF19-4/5/6 | FGF19 receptor | Tumorigenicity | Preclinical | |
FGF19 variant (FGF19v) | FGF19 receptor | Mitogenic | Preclinical | |
NGM282 (M70) | FGF19 receptor | T2DM PSC | P2 (NCT01943045) P2 (NCT02704364) | |
Obeticholic acid and Px-104 | FGF19 receptor | Primary/secondary bile acid malabsorption Obesity NAFLD | P2 (NCT01585025) P2 (NCT01625026) P2 (NCT01265498) P2 (NCT01999101) | |
LY2405319 | FGF21 receptor | T2DM | P1 (NCT01869959) | |
FGF21variant (PEG-FGF21G71C, Fc-FGF21(RG)) | FGF21 receptor | T2DM | Preclinical | |
PF-05231023 (CVX-343) | FGF21 receptor | T2DM | P1 (NCT01285518) | |
Non-selective TKIs | Lucitanib (E3810) | FGFR1/2, VEGFR1/2/3, and PDGFRα/β | Cancer with FGFR alteration | P2 (NCT02747797) P3 (NCT00165672) |
Nintedanib (BIBF1120) | FGFR1/2/3, VEGFR1/2/3, and PDGFRα/β | Cancer with FGFR alteration | Submitted P3 | |
Dovitinib (CHIR258 or TKI258) | VEGFR1/2/3, FGFR1/2/3, PDGFRβ, c-Kit, RET, TrkA, CSF-1R, and FLT3 | Cancer with FGFR alteration | P2 (NCT01719549) P2 (NCT01732107) | |
Regorafenib | Â | Â | P2 (NCT01929616) | |
Brivanib | Â | Â | P2 (NCT03516071) | |
Ponatinib | Â | Â | Approved for market | |
Lenvatinib | FGFR1/2/3 | Cancer with FGFR | P2 (NCT03609359) | |
Pazopanib | Â | alteration | P2 (NCT01253369) | |
Orantinib | Â | Â | P3 (NCT01465464) | |
Sunitinib | Â | Â | P2 (NCT00768144) | |
Cediranib | Â | Â | P3 (NCT00399035) | |
Selective TKIs | AZD4547 | FGFR1/2/3 | Cancer with FGFR alteration | P2 (NCT01824901) P2 (NCT01791985) P2 (NCT02824133) P2 (NCT01213160) |
BGJ398 (NVP-BGJ398) | FGFR1/2/3 | Cancer with FGFR alteration | P2 (NCT01975701) P2 (NCT02150967) P2 (NCT02160041) | |
JNJ-42756493 (erdafitinib) | FGFR1/2/3/4 | Cancer with FGFR alteration | P2 (NCT02365597) P2 (NCT02699606) | |
LY287445, Debio-1347, TAS-120, and BAY-1163877 | FGFR1/2/3/4 | Cancer with FGFR alteration | Preclinical | |
Neutralizing monoclonal antibodies (mAbs) | KRN23 | FGF23 | XLH | P3 (NCT02537431) |
Bemarituzumab (FPA144) | FGFR2b | Neoplasms | P1 (NCT02318329) | |
BAY1179470 | FGFR2 | Neoplasms | P1 (NCT01881217) | |
MFGR1877S | FGFR3 | Neoplasms | P1 (NCT01122875) | |
hIgG1-1A2 | FGF2 | Â | Â | |
GAL-F2 | FGF2 | Â | Â | |
3F12E7 | FGF2 | Â | Â | |
KM1334 | FGF8b | Neoplasms | Preclinical | |
FGF10 mAb | FGF10 | Â | Â | |
FN1 and FC1 | FGF23 | Â | Â | |
R1MAb1 | FGFR1 | Â | Â | |
FGF traps | FP-1039 (GSK3052230) | FGF1/2/4 | Neoplasms | P1 (NCT01868022) |
SM27 | FGF2 | Angiogenesis | Preclinical | |
NSC12 | FGF2 | Lung tumors | Preclinical | |
sFGFR2IIIc (S252W) | FGFR2 | AS | Preclinical | |
sFGFR3 | FGF2/9/18 | Chondrodysplasia | Preclinical | |
Peptide P3 | FGFR3 | Chondrodysplasia | Preclinical | |
Gene therapy | XRP0038 (NV1FGF) | FGF1 receptor | Peripheral vascular diseases | P2 (NCT00566657) |
Expression of FGF18 cDNA | FGF18 receptor | Murine models | Preclinical | |
AAV9-Fgfr2-shRNA | Fgfr2-P253R allele | AS | Preclinical | |
CRISPR/Cas9 | Fgfr3-G374R | Achondroplasia | Preclinical |
