Table 2.
Tyrosine kinase inhibitors (TKI) with VEGF receptor activity. Based on Table 1 from Chu, Expert Opin. Biol. Ther. (2009) 9(2): 263–271. By permission of Quincy Chu).
| Drug | Mechanism of Action | Company | Current Stage of Development |
|---|---|---|---|
| Predominant class III tyrosine kinase inhibitors | |||
| ABT-869 | VEGFR-2/PDGFR beta | Abbott | II |
| Axitinib | VEGFR-1, 2, 3/C-KIT/PDGFR beta | Pfizer | II/III |
| AMG 706 | VEGFR-1, 2, 3/PDGFR alpha/C-KIT/RET | Amgen | II/III |
| BAY 57-9352 | VEGFR-2, 3/PDGFR/C-KIT | Bayer | I |
| Brivanib | VEGFR-1, 2/FGFR-1 | Bristol Meyer Squibb | II/III |
| BIBF 1120 | VEGFR-1,2,3/FGFR-3/PDGFR alpha | Boehringer-Ingelheim | II/III |
| Cediranib | VEGFR-1,2,3/PDGFR alpha/C-KIT | AstraZeneca | II/III |
| Pazopanib | VEGFR-1,2,3/PDGFR alpha/C-KIT | GlaxoSmithKline | II/III |
| Sorafenib | VEGFR-2,3/PDGFR alpha/FLT-3/C-KIT | Bayer | III and FDA approved for renal cell carcinoma and HCC |
| Sunitinib | VEGFR-1,2/C-KIT/FLT-3/PDGFR alpha | Pfizer | III and FDA approved for GIST and renal cell carcinoma |
| Vatalanib | VEGFR-1,2,3/PDGFR alpha/C-KIT/C-FOS | Novartis | III |
| Epidermal growth factor receptor (EGFR) and VEGFR inhibitors | |||
| AEE788 | EGFR/HER-2/VEGFR-2 | Novartis | II |
| BMS-690514 | Pan-HER and VEGFR | Bristol Meyer Squibb | I/II |
| Vandetanib | EGFR/VEGFR-2 | AstraZeneca | III |
| XL-647 | EGFR/VEGFR-2 | Exelixis | I |
| Miscellaneous multi-kinase inhibitors with VEGFR activity | |||
| CYC116 | Aurora kinase/VEGFR-2 | Cyclacel | I |
| MGCD265 | VEGFR/C-MET | MethylGene | I |
| OSI930 | VEGFR-2/C-KIT/LCK/C-RAF | OSI | I |