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. 2019 Mar 21;8(3):270. doi: 10.3390/cells8030270

Table 2.

Therapeutic agents for the inhibition of VEGF-C/VEGFR3 signaling.

Agents Agent Description Developer Current Status Ref.
Sorafenib Small molecule TKI
(VEGFRs, PDGFRs,
c-kit, RET)
Bayer and Onyx FDA-approved [138]
Sunitinib Small molecule TKI
(VEGFRs, PDGFRs,
c-kit, Flt3, RET)
Pfizer Inc. FDA-approved [140]
Pazopanib Small molecule TKI
(VEGFRs, PDGFRs,
c-kit)
GlaxoSmithKline FDA-approved [141]
Axitinib Small molecule TKI
(VEGFRs, PDGFRs,
c-kit)
Pfizer Inc. FDA-approved [142,143]
Cediranib Small molecule TKI
(VEGFRs, PDGFRs,
c-kit)
AstraZeneca Phase III [137]
Brivanib Small molecule TKI
(VEGFRs, PDGFRs,
FGFRs)
Bristol-Myers Squibb Phase III [144]
Vandetanib Small molecule TKI
(VEGFRs, PDGFRs,
EGFR, RET)
AstraZeneca Phase II [145,146]
Motesanib Small molecule TKI
(VEGFRs, PDGFRs,
c-kit, RET)
Amgen Phase III [147]
SAR131675 Small molecule TKI
(more selective for VEGFR3 than VEGFR1/2)
Sanofi Preclinical [148,149]
Bevacizumab Humanized
anti-VEGF-A mAb
Genentech FDA-approved [150]
IMC-3C5 Humanized
anti-VEGFR3 mAb
ImClone Systems/Eli Lilly Phase I [153]
VGX-100 Humanized
anti-VEGF-C mAb
Circadian Technologies Phase I [154]
Diabody Anti-VEGFR2/
VEGFR3 mAb
- Preclinical [155]
sVEGFR3-Fc Soluble VEGFR3 decoy receptor - Preclinical [156]
Single-chain fragment (scFv) Anti-VEGF-C
mAb fragment
- Preclinical [157]
VEGFR3-Ig Anti-VEGF-C/A Receptor-Ig
fusion protein
- Preclinical [158]
Anti-VEGFR3 peptide Anti-VEGFR3 peptide - Preclinical [92]