Table 4 Inhibitors of lymphangiogenesis and applications

From: Lymphatic vessel: Origin, heterogeneity, biological functions and therapeutic targets

Inhibitor name

Target of action

Application

Antibody drugs

Bevacizumab

VEGF

Inhibition of Corneal inflammatory lymphangiogenesis Inhibition of melanoma-associated lymphangiogenesis

1E9

VEGFC

Inhibition of lymphangiogenesis in clear cell renal cell carcinoma

VGX-100

VEGFC

Suppression of lymphangiogenesis in corneal graft rejection response Inhibition of lymphangiogenesis in colorectal cancer

Single-chain fragment of VEGFC antibody

VEGFC

Blockage the lymphangiogenic activity of VEGFC

VEGFR3-immunoglobulin

VEGFC

Suppression of lung cancer-associated lymphangiogenesis

VEGFR3 antagonist antibody

VEGFR3

Suppression of lung cancer-associated lymphangiogenesis

MEDI3617

ANG2

Reduction of lung cancer-associated lymphangiogenesis

AZD5180

ANG2

Inhibition of lymphangiogenesis in infection-mediated inflammation

18E5

ANG2

Suppression of lymphangiogenesis in corneal graft rejection response

Small molecular inhibitors

Pazopanib

VEGFR1, VEGFR2, VEGFR3

Inhibition of lymphangiogenesis in colorectal cancer

Sunitinib

VEGFR1, VEGFR2, VEGFR3, PDGFRs, c-Kit

Suppression of pathologic corneal lymphangiogenesis, Suppression of cancer-associated lymphangiogenesis

Synthesized preclinical candidate agents

VEGFC siRNA

VEGFC

Suppression of lymphangiogenesis

ANG2 siRNA

ANG2

Suppression of pathologic corneal lymphangiogenesis

Inhibitors naturally existed in the host

WNT1

VEGFC

Inhibition of melanoma-associated lymphangiogenesis

TSP-1

VEGFC

Suppression of corneal lymphangiogenesis Inhibition of lymphangiogenesis in mouse atherosclerotic aortic tissue

Semaphorins

Plexins and NRPs

Suppression of corneal lymphangiogenesis Suppression of HNSCC-associated lymphangiogenesis

IFN-γ

 

Promotion of LEC apoptosis

Other inhibitors

Rapamycin

mTOR

Inhibition of cancer-associated lymphangiogenesis Suppression of lymphangiogenesis in corneal graft rejection response

Celecoxib

COX2

Suppression of lymphangiogenesis in breast cancer

Aspirin

COXs

Suppression of lymphangiogenesis in lung cancer

Phomaketide A

VEGFR3 PKCδ, eNOS

Inhibition of cancer-associated lymphangiogenesis

Fucoxanthin

-

Suppression of lymphangiogenesis in breast cancer

Shikonin

NF-κB

Inhibition of lymphangiogenesis in an in vitro model

Curcumin

VEGFR3

Suppression of cancer-associated lymphangiogenesis

  1. VEGF vascular endothelial growth factor, VEGFR vascular endothelial growth factor receptor, ANG angiopoietin, PDGFR platelet-derived growth factor receptor, NRP neuropilin, mTOR mammalian target of rapamycin, COX cyclooxygenase, PKC δ protein kinase C δ, eNOS endothelial nitric oxide synthase