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 |