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. Author manuscript; available in PMC: 2017 Oct 1.
Published in final edited form as: Cancer Lett. 2014 Oct 12;380(2):525–533. doi: 10.1016/j.canlet.2014.09.035

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.