Table 8.
Antiangiogenics, target and main clinical indications or trials.
| Name (Code) Trade Name | Targets | Approved Clinical Indications or Clinical Trial Study |
|---|---|---|
| Sunitinib (SU011248) Sutent | VEGFR1/2/3, FLT3, Kit, PDFGRβ | GIST, RCC, pNET |
| Pazopanib (GW786034) Votrient | VEGFR1/2/3, PDGFRα/β, FGFR cKIT. | RCC, soft-tissue sarcoma. |
| Tivozanib (AV-951) Fotivda | VEGFR1/2/3 | RCC |
| Axitinib (AG013736) Inlyta | VEGFR1/2/3, c-KIT | RCC |
| Cabozantinib (BMS-907351) Cabometyx, cometriq | c-MET, VEGFR2, RET, TRKA, TRKB and Axl. | RCC, HCC, MTC |
| Lenvatinib (E7080) Lenvima | VEGFR1/2/3, FGFR1/2/3/4, PDGFRα, c-KIT, RET | RCC, DTC, HCC |
| Sorafenib (BAY43-9006), Nexavar | VEGFR1/2/3, PDGFRβ, Flt-3, c-KIT, RET, Raf | HCC, DTC, RCC |
| Regorafenib (BAY73-4506) Stivarga | VEGFR1/2/3, Raf, TIE-2, PDGFR, RET, CSF-1 | CRC, GIST, HCC |
| Nintedanib (BIBF1120) Vargatef | VEGFR1/2/3, PDGFRα/β), FGFR1/2/3, TRK, Flt-3 RET | NSCLC |
| Vandetanib (ZD6474) Caprelsa | VEGFR, EGFR and RET. | MTC |
| Apatinib (YN968D1) | VEGFR2 | Gastric cancer (China) |
| Fruquintinib (HMPL-013) | VEGFR1/2/3 | CRC (China) |
| Anlotinib (AL3818) | VEGFR2/3, c-Kit | NSCLC (China) |
| Motesanib (AMG-706) | VEGFR1/2/3, c-Kit, RET, PDGFR | Under development in several solid tumors |
| Linifanib (ABT-869) | VEGFR1/2, CSF-1R, FLT3, c-Kit | Under development in several solid tumors |
| Glesatinib (MGCD-265) | VEGFR1/2/3, MET, RON, Tie-2 | Under development in NSCLC (NCT02544633) and other solid tumors |
| Cediranib (AZD2171) | VEGFR1/2/3, c-Kit, PDGFRβ, FGFR1 | Under development in several solid tumors |
| Dovitinib (CHIR-258) | FGFR1/2/3, VEGF, c-Kit, FLT3 | Multiple clinical trials mainly in renal cell carcinoma (phase III), breast cancer, hepatocellular cancer, endometrial cancer and GIST |
| Tivozanib (AV-951) | VEGFR1/2/3, EphB2, PDGFR | Under development in several solid tumors |
| Vatalanib (PTK787) | VEGFR1/2/3, PDGFR, c-Kit | Under development in several solid tumors |
| Brivanib (BMS-540215) | VEGFR1/2, FGFR1 | Under development in several solid tumors |
| Apatinib (YN968D1) | VEGFR2, RET | Under development in several solid tumors |
| Ponatinib (AP24534) | VEGFR2, PDGFR, FGFR1 | Under development in several solid tumors |
| LY2874455 | VEGFR2, FGFR1/2/4 | Under development in solid tumors (NCT01212107) |
| Golvatinib (E7050) | VEGFR2, MET | Under development in several solid tumors |
| Telatinib (BAY 57-9352) | VEGFR2/3, c-Kit, PDGFR | Under development in gastric cancer (NCT00952497, NCT03817411) and other solid tumors (NCT03175497) |
| Lucitanib (E-3810) | VEGFR1/2/3, FGFR1/2 | Under development in several solid tumors |
| Sulfatinib | VEGFR1/2/3, FGFR1, CSF1R | Under development in neuroendocrine tumors (NCT04579679), thyroid cancer (NCT04524884), biliary tract carcinoma (NCT03873532) and other solid tumors (NCT04579757, NCT02549937) |