TABLE 1.
IC50 values (in nM) of β-lactamase inhibition by QPX7728 and comparator BLIsb
| Enzyme | Class | CARB | IC50 (nM) of drug: |
|||
|---|---|---|---|---|---|---|
| Vaborbactam | Avibactam | Relebactam | QPX7728 | |||
| KPC-2 | A | Yes | 110 ± 30 | 22 ± 6 | 82 ± 17 | 2.9 ± 0.4 |
| CTX-M-14 | A | No | 110 ± 40 | 1.4 ± 0.4 | 34 ± 10 | 0.94 ± 0.2 |
| CTX-M-15 | A | No | 92 ± 13 | 0.56 ± 0.25 | ND | 1.2 ± 0.1 |
| SHV-12 | A | No | 56 ± 11 | 0.61 ± 0.19 | 330 ± 50 | 1.9 ± 0.6 |
| TEM-10 | A | No | 470 ± 150 | 4.3 ± 1.2 | 160 ± 20 | 2.2 ± 0.8 |
| TEM-43 | A | No | (2.2 ± 0.4) × 103 | ND | ND | 3.0 ± 0.1 |
| P99 | C | No | 88 ± 38 | 26 ± 7 | 36 ± 4 | 22 ± 6 |
| OXA-48 | D | Yes | (6.9 ± 2.3) × 103 | 180 ± 50 | (9 ± 0.3) × 104 | 1.1 ± 0.4 |
| OXA-23 | D | Yes | (1.2 ± 0.2) × 105 | (3.1 ± 0.6) × 103 | ND | 1.2 ± 0.4 |
| NDM-1a | B | Yes | >1.6 × 105 | >1.6 × 105 | >1.6 × 105 | 55 ± 25 |
| VIM-1 | B | Yes | >1.6 × 105 | >1.6 × 105 | >1.6 × 105 | 14 ± 4 |
| IMP-1a | B | Yes | >1.6 × 105 | >1.6 × 105 | >1.6 × 105 | 610 ± 70 |
| IMP-26a | B | Yes | >1.6 × 105 | >1.6 × 105 | >1.6 × 105 | (4.1 ± 1) × 103 |
a
Imipenem was used as a substrate.
b
Abbreviations: CARB, carbapenemase activity; ND, not done.