TABLE 1.
In vitro and in vivo activities of RWJ-416457, linezolid, and vancomycin against gram-positive pathogens in mouse lethal infection models
| Model and strain (type) | Compound | MIC (μg/ml) | ED50, mg/kg/day (95% fiducial limit)
|
||
|---|---|---|---|---|---|
| p.o. | s.c. | i.v. | |||
| S. aureus systemic infection models | |||||
| ATCC 13709 (MSSA) | RWJ-416457 | 1 | 3.4 (2.7-4.5) | 4.7 (3.2-6.8) | 4.0 (3.0-5.2) |
| Linezolid | 2 | 6.4 (5.2-7.8) | 7.0 (5.4-9.1) | 6.3 (4.2-9.8) | |
| Vancomycin | 1 | NAa | 1.7 (0.9-2.9) | 0.9 (0.6-1.4) | |
| OC8525 (CA-MRSA) | RWJ-416457 | 2 | 2.1 (1.3-3.0) | 3.5 (2.5-4.5) | 1.5 (0.6-2.3) |
| Linezolid | 4 | 5.1 (2.7-7.8) | 3.7 (1.7-5.7) | 8.5 (6.5-11) | |
| Vancomycin | 1 | NA | 12 (10-14) | 5.6 (3.7-11) | |
| S. pneumoniae lung infection model | |||||
| ATCC 6301 (PSSP) | RWJ-416457 | 1 | 3.1 (2.0-4.9) | 9.3 (5.6-31) | 18 (13-26) |
| Linezolid | 2 | 14 (9.5-28) | 20 (13-26) | >40 | |
a
NA, not applicable.