Table 3.
| Drug | VEGFR1 (IC50) | VEGFR2 (IC50) | VEGFR3 (IC50) | RET (IC50) | Other (IC50) | PR | SD | PFS | Citations |
|---|---|---|---|---|---|---|---|---|---|
| Motesanib | X (2) | X (3) | X (6) | X (59) | c-KIT (8) | 14% | 35% | 40 weeks | Sherman et al73 |
|
| |||||||||
| Axitinib | X (1.2) | X (0.25) | X (0.29) | c-KIT (1.7) | 30% | 38% | 18.1 months | Cohen et al71 | |
|
| |||||||||
| Sorafenib | X (90) | X (20) | X (49) | BRAF (22) c-KIT (68) |
15% | 56% | 15 months | Kloos et al57 | |
| 23% | 53% | 84 weeks | Gupta-Abramson et al56 | ||||||
| 25% | 34% | 58 weeks | Hoftijzer et al58 | ||||||
| 31% | 42% | 18 months | Schneider et al59 | ||||||
| 18% | 79% | n/a | Ahmed et al60 | ||||||
| 20% | 60% | 19 months | Cabanillas et al61 | ||||||
|
| |||||||||
| Sunitinib | X (2) | X (9) | X (17) | X (41) | c-KIT (7) | 28% | 46% | TTP 12.8 months | Carr et al62 |
|
| |||||||||
| Pazopanib | X (10) | X (30) | X (47) | X (2800) | c-KIT (74)95 | 49% | n/a | 11.7 months | Bible et al66 |
|
| |||||||||
| Lenvatinib | X (22) | X (4) | X (5.2) | X (35) | FGFR (46) 96 c-KIT (100)97 |
50% | n/a | 12.6 months | Sherman et al77 |
|
| |||||||||
| Cabozantinib | X (0.035) | X (5.2) | c-MET (1.8) c-KIT (4.6)98 |
53% | 40% | n/a | Cabanillas et al76 | ||
|
| |||||||||
| Vandetanib | X (1600) | X (40) | X (110) | X (100) | EGFR (500) | ≤8% | 56% | 11.1 months | Leboulleux et al68 |
|
| |||||||||
| Selumetenib | MEK (14)99 | 3% | 54% | 8 months | Hayes et al75 | ||||
VEGFR=vascular endothelial growth factor receptor; FGFR= fibroblast growth factor receptor; EGFR= epidermal growth factor receptor; PFS=progression-free survival; PR=partial response; CR=complete response; TTP=time to progression; IC50=half maximal inhibitory concentration in nmol.