Table I.
FDA-approved anti-angiogenic therapeutics.
| Anti-angiogenic agent | Targeted Pathway | Clinical Indications (year approved) |
|---|---|---|
| Afatinib | Receptor tyrosine kinase inhibitor (epidermal growth factor receptor [EGFR], human epidermal growth factor receptor 2 [HER2]) | Non-small cell lung cancer (2013); squamous cell lung carcinoma (2016) |
| Aflibercept | VEGFR1/VEGR2/IgG chimeric protein (VEGF-A, VEGF-B, and placental growth factor [PIGF]) | Wet age-related macular degeneration (2011); metastatic colorectal cancer (2012) |
| Axitinib | Receptor tyrosine kinase inhibitor (VEGFR, platelet-derived growth factor receptor [PDGFR], c-KIT) | Renal cell carcinoma (2012) |
| Bevacizumab | Humanized monoclonal antibody (VEGF-A) | Metastatic colorectal cancer (2004); lung cancer (2006) |
| Cabozantinib | Receptor tyrosine kinase inhibitor (c-MET, VEGFR2, AXL, RET) | Metastatic medullary thyroid cancer (2012) |
| Cetuximab | Chimeric monoclonal antibody (EGFR) | Metastatic colorectal cancer (2012); recurrent or metastatic head and neck cancer (2011) |
| Erlotinib | Receptor tyrosine kinase inhibitor (EGFR) | Lung cancer (2004) |
| Gefitinib | Receptor tyrosine kinase inhibitor (EGFR) | Metastatic non-small cell lung cancer (2015) |
| Lapatinib | Receptor tyrosine kinase inhibitor (EGFR, HER2) | HER2+ breast cancer (2007) |
| Lenalidomide | Small molecule that binds to cerublon and thereby reduces the level of certain transcription factors | Myelodysplastic syndrome (2005) |
| Necitumumab | human IgG1 monoclonal antibody (EGFR) | Metastatic squamous non-small cell lung cancer, in combination with gemcitabine and cisplatin (2015) |
| Nintedanib | Receptor tyrosine kinase inhibitor (VEGFR, fibroblast growth factor receptor [FGFR], PDGFR) | Idiopathic pulmonary fibrosis (2014) |
| Panitumumab | Human IgG2 monoclonal antibody (EGFR) | Colorectal cancer (2006) |
| Pazopanib | Receptor tyrosine kinase inhibitor (c-KIT, FGFR, PDGFR, VEGFR) | Renal cell carcinoma (2009); soft tissue sarcoma (2012) |
| Pegaptanib | RNA aptamer (VEGF-A165 isoform) | Wet age-related macular degeneration (2004) |
| Pertuzumab | Humanized monoclonal antibody (HER2) | Neoadjuvant treatment of HER2+ breast cancer in combination with Trastuzamab and Docetaxel (2012) |
| Pomalidomide | Small molecule that binds to cerublon and thereby reduces the level of certain transcription factors | Multiple myeloma (2013) |
| Ramucirumab | IgG1 monoclonal antibody (VEGFR2) | Metastatic gastric or gastroesophageal junction adenocarcinoma and platinum-resistant metastatic non-small cell lung cancer (2014); metastatic colorectal cancer (2015) |
| Ranibizumab | Fab fragment of bevacizumab (VEGF-A) | Neovascular age-related macular degeneration (2006) |
| Regorafenib | Receptor tyrosine kinase inhibitor (VEGFR2, TIE2) | Metastatic colorectal cancer (2012); GIST (2013); and hepatocellular carcinoma (2017) |
| Sorafenib | Kinase inhibitor (VEGFR, PDGFR, RAF family) | Renal cell carcinoma (2005); hepatocellular carcinoma (2007) |
| Sunitinib | Receptor tyrosine kinase inhibitor (PDGFR, VEGFR, c-KIT, RET, granulocyte colony-stimulating factor receptor [G-CSFR], FLT3) | Metastatic renal cell carcinoma and gastrointestinal stromal tumor (2006); pancreatic neuroendocrine tumors (2011) |
| Temsirolimus | Small molecule inhibitor (mammalian target of rapamycin [mTOR]) | Multiple myeloma in combination with dexamethasone (2006) |
| Thalidomide | Small molecule that binds to cerublon and thereby reduces the level of certain transcription factors | Multiple myeloma (2003) |
| Trastuzumab | Humanized monoclonal antibody (HER2) | HER2+ breast cancer (2006); HER2-overexpressing metastatic gastric or gastroesophageal (GE) junction adenocarcinoma (2010) |
| Vandetanib | Receptor tyrosine kinase inhibitor (VEGFR, EGFR, RET) | Unresectable, locally advanced, or metastatic medullary thyroid cancer (2011) |