Table 1.
Anti-VEGF drugs currently used/tested in the clinics
| Drugs | Company | Mode of Action | Tumor Types Treated | Status |
|---|---|---|---|---|
| Bevacizumab | Genentech Inc. | Monoclonal anti-VEGF antibody | Metastatic Colorectal Cancer in Combination with Fluoropyrimidine-based Chemotherapy, Metastatic Renal Cell Carcinoma, Second-Line Treatment of Glioblastoma, First-Oine Treatment of Non-Small Cell Lung Cancer (NSCLC), Second-Line Treatment of Metastatic Colorectal Cancer, First-Line Treatment of Metastatic Colorectal Cancer, | FDA approved |
| Sorafenib | Bayer Healthcare and Onyx Pharmaceuticals | Small molecule multi-TKi including VEGFR | Liver cancer, Thyroid cancer and RCC, | FDA approved |
| Sunitinib | Pfizer Inc | Small molecule multi-TKi including VEGFR | Pancreatic neuroendocrine tumor, Gastrointestinal stromal tumor, Kidney cancer | FDA approved |
| Pazopanib | Glaxo SmithKline | Small molecule multi-TKi including VEGFR | Advanced soft tissue sarcoma, Advanced renal cell carcinoma | FDA approved |
| Vatalanib | Bayer Schering and Novartis | Small molecule multi-TKi including VEGFR | Colorectal cancer Non-Small Cell Lung Cancer (NSCLC) | (Phase I) (Phase II) |
| Axitinib | Pfizer Inc. | Small molecule Inhibitor of VEGFR1, VEGFR2, VEGFR3, c-KIT, PDGFT | Advanced renal cell carcinoma (after failure of one prior systemic therapy) Progressive, Recurrent/Metastatic Adenoid Cystic Carcinoma Advanced carcinoid tumor | FDA approved (Phase II) (Phase II) |
| Aflibercept | Regeneron Pharmaceuticals | Chimeric VEGF/PGF neutralizing receptor; vascular endothelial growth factor trap Functions as a soluble decoy receptor, binds to pro-angiogenic vascular endothelial growth factors (VEGFs) | Metastatic Colorectal Cancer K-RAS Mutant Patients With Resectable Liver Metastates (Phase II/III) Metastatic colorectal Cancer Myelodysplastic Syndromes Stage III-IV Melanoma Esophageal and Gastric Cancer Breast Cancer | FDA approved (Phase III) (Phase II) (Phase II) (Phase II) (Phase I) |
| Vandetanib | AstraZeneca | Small molecule dual TKi for VEGFR/EGFR | Medullary thyroid cancer Precancerous Head and Neck Lesions, Gastrointestinal Stroma Tumors | FDA Approved (Phase II) |
| Cediranib | AstraZeneca | Small molecule TKi for VEGFR | Alveolar Soft Part Sarcoma Recurrent Glioblastoma Ovarian cancer | (Phase II) (Phase III) (Phase III) |
| Nintedanib (BIBF 1120) | Boehringer Ingelheim | Small molecule inhibitor of angiokinase (inhibits VEGFR, FGFR, PDGFR) | Ovarian Neoplasms Peritoneal Neoplasms | (Phase III) |
| Ponatinib | ARIAD Pharmaceuticals | BCR-ABL inhibitor that also selectively inhibits certain other tyrosine kinases in preclinical studies, including FLT3, RET, KIT and the members of the FGFR PDGFR and VEGFR families of kinases. | Chronic myeloid leukemia or Philadelphia chromosome-positive acute lymphoblastic leukemia | FDA Approved |
| Brivanib | Vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor | Recurrent or Persistent Endometrial Cancer and Cervical Cancer | (Phase I) | |
| Regorafenib | Bayer Healthcare | Inhibits vascular endothelial growth factor receptors (VEGFRs) 2 and 3, and Tie2, Ret, Kit, PDGFR and Raf kinases, | Colorectal cancer (metastasized) Gastrointestinal stromal tumor (locally advanced, cannot be removed by surgery, or has metastasized) | FDA Approved FDA Approved |
| Ramucirumab | Eli Lilly and Company | Binds to vascular endothelial growth factor receptor-2 (VEGFR-2) | Gastric or gastro-esophageal junction adenocarcinoma | FDA Approved |