Table 1.
VEGF and Ang-2 axis targeted agents in the clinic and preclinical settings. (Due to the scope of this review, this table only shows the VEGF/VEGFR axis targeted agents that have been FDA approved.).
| Agent | Target | Clinical Status | Tumor Setting |
|---|---|---|---|
| VEGF Targeted | |||
| Bevacizumab (Avastin®) | VEGF | FDA Approved | mCRC, RCC, NSCLC, Glioblastoma |
| Sorafenib (Nexavar®) | VEGFR, PDGFR, Raf, RET, cKIT, Flt3 | FDA Approved | RCC, HCC |
| Sunitinib (Sutent®) | VEGFR, PDGFR, Flt3, RET, CSF-1 | FDA Approved | RCC, GIST, Pancreatic cancer |
| Pazopanib (Votrient®) | VEGFR, PDGFR, cKIT | FDA Approved | RCC, Sarcoma |
| Vandetanib (Caprelsa®) | VEGFR, EGFR, RET | FDA Approved | Medullary thyroid cancer |
| Cabozantinib (Cometriq®) | cMET, VEGFR-2 | FDA Approved | Medullary thyroid cancer |
| Axitinib (Inlyta®) | VEGFR, PDGFR, cKIT | FDA Approved | RCC |
| Ziv-Aflibercept (Zaltrap®) | VEGF | FDA Approved | mCRC |
| Ramucirumab (Cyramza®) | VEGFR-2 | FDA Approved | Stomach cancer |
| Angiopoietin Targeted | |||
| Trebananib (AMG386) | Ang-1/Ang-2 | Phase III | Ovarian cancer |
| Phase I | AML, CNS | ||
| AMG780 | Ang-2 | Phase I | Solid tumors |
| MEDI3617 | Ang-2 | Phase I | Solid tumors |
| Nesvacumab (REGN910) | Ang-2 | Phase I | Solid tumors |
| CVX-060 | Ang-2 | Phase I | Solid tumors |
| DX-2240 | Tie1 | Preclinical | |
| scFv-Ang-2 | Ang-2 | Preclinical | |
| LC-06 | Ang-2 | Preclinical | |
| VEGF and angiopoietin targeted | |||
| Regorafenib (Stivarga®) | VEGFR-2, PDGFR, Tie2, KIT, RET, Raf | FDA Approved | mCRC, GIST |
| CEP-11981 | Tie2, VEGFR | Phase I | Solid tumors |
| ARRY-614 | Tie2, VEGFR-2, p38, Abl | Phase I | Myelodysplastic syndromes |
| CVX-241 | Ang-2, VEGF | Phase I | Solid tumors |
| RO5520985/RG7221 | Ang-2-VEGF CrossMab | Phase I | Solid tumors |
| ACTB-1003 | Tie2, VEGFR-2, FGFR-1, RSK, S6K A | Preclinical | |
| DAAP | Ang-2, VEGF | Preclinical |
mCRC: metastatic colorectal cancer, RCC: renal cell carcinoma, NSCLC: non-small cell lung cancer, HCC: hepatocellular carcinoma, GIST: gastrointestinal stromal tumor, AML: acute myeloid leukemia, CNS: central nervous system tumor.