Table 1.
Target profiles of Aurora kinase inhibitors currently in clinical investigation in the haematological malignancies
| Drug | Manufacturer | Target kinase inhibited by drug* |
|||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Aurora A |
Aurora B |
FLT3 | ABL1 | ABL1 (T315I) |
KIT | VEGFR | JAK2 | FGFR3 | SYC | LYN | IGF1R | ||
| AZD1152 | Astra Zeneca | 1369 | 0.37 | - | - | - | - | - | - | - | - | - | - |
| MLN8237 | Millennium | 1 | 1100 | - | - | - | - | - | - | - | - | - | - |
| ENMD-2076 | EntreMed | 14 | 290 | 3 | 295 | 81 | 126 | 36 | 120 | 92 | - | - | - |
| AS703569 | Merck Sereno | 4 | 4.8 | 99% inhibition at 100 nM |
92% inhibition at 100 nM |
- | - | - | - | - | - | - | - |
| KW-2449 | Kyowa Hakko Kirin Pharma |
48 | 48 | 6.6 | 14 | 4 | 300 | - | 150 | - | - | - | - |
| AT9283 | Astex Therapeutics |
3 | 3 | 10 | 110 | 4 | - | 10–30 | 1.2 | 10–30 | - | - | - |
| Danusertib | Nerviano | 13 | 70 | - | 21 | 4 | - | - | - | - | - | - | - |
| XL228 | Exelixis | 3.1 | 0.6 | - | 5 | 1.4 | - | - | - | 3 | 6.1 | 5 | 1.2 |
*
Concentration inhibiting target kinase activity by 50% (IC50) shown (nM) unless otherwise indicated.