Table 4.
Inhibition of major carbapenemases by new carbapenemase inhibitors.
| Inhibitor | Carbapenemase | ||||||
|---|---|---|---|---|---|---|---|
| Class A | Class B | Class D | |||||
| KPC | NDM | VIM | IMP | OXA-23 | OXA-24/40 | OXA-48 | |
| Diazabicyclooctane-derived | |||||||
| Relebactam | ✓ | ✗ | ✗ | ✗ | ✗ | ✗ | |
| Avibactam | ✓ | ✗ | ✗ | ✗ | ✗ | ✗ | ✓ |
| Zidebactam | ✓ a | ✗ | ✗ | ✗ | ✗ | ✗ | ✗ |
| Durlobactam | ✓ | ✗ | ✗ | ✓ | ✓ | ✓ | |
| Nacubactam | ✓ b | ✗ | ✗ | ✗ | ✗ | ✗ | |
| ETX1317 | ✓ | ✓ | |||||
| WCK 4234 | ✓ | ✗ | ✗ | ✗ | ✓ c | ✓ d | ✓ |
| Boronic acid derived | |||||||
| Vaborbactam | ✓ | ✗ | ✗ | ✗ | ✗ | ✗ | |
| Taniborbactam | ✓ | ✓ | ✓ | ✗ | ✓ | ||
| VNRX-5236 | ✓ e | ✗ | ✗ | ✗ | ✓ | ||
| QPX7728 | ✓ | ✓ | ✓ | ✓ | ✓ | ✓ | |
| β-lactam-derived | |||||||
| Enmetazobactam | ✓ | ✓ f | |||||
| LN-1-255 | ✓ | ✓ | ✓ | ||||
✓, useful inhibitory activity experimentally demonstrated; ✗, non-inhibition or not useful inhibitory activity demonstrated; blank square, not evaluated. Intermediate inhibition activity: IC50 or Ki values: a Ki = 4.5 µM, b IC50 = 0.87 µM, c Ki = 8 µM, d Ki = 5 µM, e IC50 = 5.2 µM and f IC50 = 1.1 µM.