TABLE 1.
Antibacterial activities of DX-619 and reference compounds against gram-positive bacteria
| Organism (no. of strains) and compound | MIC (μg/ml)
|
|||
|---|---|---|---|---|
| Range | 50% | 90% | ||
| Staphylococcus aureus | ||||
| Methicillin susceptible (48) | ||||
| DX-619 | ≦0.004-0.06 | 0.008 | 0.015 | |
| Levofloxacin | 0.12-8 | 0.25 | 0.5 | |
| Sitafloxacin | 0.008-1 | 0.03 | 0.06 | |
| Ciprofloxacin | 0.12-32 | 0.5 | 2 | |
| Moxifloxacin | 0.03-2 | 0.06 | 0.12 | |
| Gatifloxacin | 0.06-4 | 0.12 | 0.25 | |
| Garenoxacin | 0.008-1 | 0.03 | 0.06 | |
| Vancomycin | 1-2 | 1 | 1 | |
| Teicoplanin | 0.25-1 | 0.5 | 0.5 | |
| Quinupristin-dalfopristin | 0.12-0.25 | 0.25 | 0.25 | |
| Linezolid | 2-4 | 2 | 4 | |
| Arbekacin | 4-128 | 8 | 16 | |
| Imipenem | 0.03-0.06 | 0.06 | 0.06 | |
| Ceftriaxone | 2-16 | 4 | 4 | |
| Minocycline | 0.12-16 | 0.12 | 0.12 | |
| Oxacillin | 0.25-1 | 0.5 | 1 | |
| Methicillin resistant, ciprofloxacin susceptible (24) | ||||
| DX-619 | ≦0.004-0.015 | 0.008 | 0.008 | |
| Levofloxacin | 0.12-0.25 | 0.25 | 0.25 | |
| Sitafloxacin | ≦0.004-0.03 | 0.03 | 0.03 | |
| Ciprofloxacin | 0.12-0.5 | 0.5 | 0.5 | |
| Moxifloxacin | 0.015-0.06 | 0.03 | 0.06 | |
| Gatifloxacin | 0.03-0.12 | 0.12 | 0.12 | |
| Garenoxacin | 0.008-0.03 | 0.015 | 0.03 | |
| Vancomycin | 1-2 | 2 | 2 | |
| Teicoplanin | 0.25-2 | 0.5 | 1 | |
| Quinupristin-dalfopristin | 0.12-0.5 | 0.25 | 0.5 | |
| Linezolid | 2 | 2 | 2 | |
| Arbekacin | 4-32 | 16 | 32 | |
| Imipenem | 0.25-64 | 1 | 32 | |
| Ceftriaxone | 32->128 | 128 | >128 | |
| Minocycline | 0.12-16 | 0.12 | 4 | |
| Oxacillin | 16->128 | 64 | >128 | |
| Methicillin resistant, ciprofloxacin resistant (99) | ||||
| DX-619 | 0.03-1 | 0.06 | 0.5 | |
| Levofloxacin | 4->128 | 8 | >128 | |
| Sitafloxacin | 0.25-16 | 0.5 | 8 | |
| Ciprofloxacin | 8->64 | 32 | >64 | |
| Moxifloxacin | 1-64 | 2 | 32 | |
| Gatifloxacin | 1-128 | 4 | 64 | |
| Garenoxacin | 0.25-64 | 1 | 32 | |
| Vancomycin | 0.5-2 | 1 | 2 | |
| Teicoplanin | 0.25-4 | 1 | 1 | |
| Quinupristin-dalfopristin | 0.12-4 | 0.5 | 0.5 | |
| Linezolid | 0.5-2 | 1 | 1 | |
| Arbekacin | 4->128 | 8 | 32 | |
| Imipenem | 1->128 | 32 | 64 | |
| Ceftriaxone | >128 | >128 | >128 | |
| Minocycline | 0.06-16 | 8 | 16 | |
| Oxacillin | 64->128 | >128 | >128 | |
| Coagulase-negative staphylococci | ||||
| Methicillin susceptible (46) | ||||
| DX-619 | ≦0.004-0.12 | 0.008 | 0.015 | |
| Levofloxacin | 0.12-16 | 0.25 | 0.5 | |
| Sitafloxacin | 0.008-0.25 | 0.015 | 0.03 | |
| Ciprofloxacin | 0.12-32 | 0.25 | 0.5 | |
| Moxifloxacin | 0.03-4 | 0.12 | 0.12 | |
| Gatifloxacin | 0.06-4 | 0.12 | 0.25 | |
| Garenoxacin | 0.015-1 | 0.03 | 0.06 | |
| Vancomycin | 0.5-4 | 1 | 2 | |
| Teicoplanin | 0.12-4 | 0.5 | 2 | |
| Quinupristin-dalfopristin | 0.12-0.25 | 0.12 | 0.25 | |
| Linezolid | 0.5-1 | 1 | 1 | |
| Arbekacin | 1-32 | 2 | 8 | |
| Imipenem | 0.015-0.03 | 0.03 | 0.03 | |
| Ceftriaxone | 0.5-8 | 1 | 2 | |
| Minocycline | 0.06-0.5 | 0.06 | 0.12 | |
| Oxacillin | 0.06-0.25 | 0.12 | 0.12 | |
| Methicillin resistant (45) | ||||
| DX-619 | 0.008-0.5 | 0.06 | 0.12 | |
| Levofloxacin | 0.25->128 | 8 | 32 | |
| Sitafloxacin | 0.015-2 | 0.25 | 0.5 | |
| Ciprofloxacin | 0.12->64 | 8 | 64 | |
| Moxifloxacin | 0.06-64 | 1 | 4 | |
| Gatifloxacin | 0.12-64 | 2 | 4 | |
| Garenoxacin | 0.03-32 | 1 | 4 | |
| Vancomycin | 1-4 | 2 | 2 | |
| Teicoplanin | 0.25-8 | 1 | 4 | |
| Quinupristin-dalfopristin | 0.12-0.25 | 0.12 | 0.25 | |
| Linezolid | 1-2 | 1 | 2 | |
| Arbekacin | 2-64 | 16 | 64 | |
| Imipenem | 0.12-128 | 32 | 64 | |
| Ceftriaxone | 8->128 | 32 | >128 | |
| Minocycline | 0.06-16 | 0.25 | 8 | |
| Oxacillin | 2->128 | 32 | >128 | |
| Streptococcus pneumoniae | ||||
| Penicillin susceptible (48) | ||||
| DX-619 | ≦0.004-0.03 | 0.015 | 0.015 | |
| Levofloxacin | 0.5-2 | 1 | 2 | |
| Sitafloxacin | 0.03-0.12 | 0.06 | 0.06 | |
| Ciprofloxacin | 0.5-4 | 1 | 2 | |
| Moxifloxacin | 0.12-0.25 | 0.12 | 0.25 | |
| Gatifloxacin | 0.25-0.5 | 0.25 | 0.5 | |
| Garenoxacin | 0.015-0.25 | 0.06 | 0.12 | |
| Vancomycin | 0.25-1 | 0.5 | 1 | |
| Quinupristin-dalfopristin | 0.5-2 | 1 | 1 | |
| Linezolid | 0.5-2 | 1 | 2 | |
| Imipenem | ≦0.004-0.06 | 0.008 | 0.015 | |
| Ceftriaxone | 0.015-1 | 0.12 | 0.5 | |
| Benzylpenicillin | 0.015-0.06 | 0.03 | 0.06 | |
| Penicillin intermediate and resistant (50) | ||||
| DX-619 | 0.008-0.06 | 0.03 | 0.03 | |
| Levofloxacin | 1-2 | 1 | 2 | |
| Sitafloxacin | 0.03-0.25 | 0.06 | 0.12 | |
| Ciprofloxacin | 1-8 | 2 | 4 | |
| Moxifloxacin | 0.12-0.5 | 0.25 | 0.5 | |
| Gatifloxacin | 0.25-1 | 0.5 | 0.5 | |
| Garenoxacin | 0.03-0.25 | 0.12 | 0.12 | |
| Vancomycin | 0.25-1 | 0.5 | 0.5 | |
| Quinupristin-dalfopristin | 0.5-4 | 1 | 1 | |
| Linezolid | 1-2 | 1 | 2 | |
| Imipenem | 0.12-0.5 | 0.25 | 0.5 | |
| Ceftriaxone | 0.5-2 | 1 | 2 | |
| Benzylpenicillin | 1-4 | 2 | 2 | |
| Ciprofloxacin resistant (19) | ||||
| DX-619 | 0.015-0.12 | 0.03 | 0.12 | |
| Levofloxacin | 8-32 | 16 | 16 | |
| Sitafloxacin | 0.12-0.5 | 0.25 | 0.5 | |
| Ciprofloxacin | 4-32 | 16 | 32 | |
| Moxifloxacin | 1-4 | 2 | 4 | |
| Gatifloxacin | 2-8 | 4 | 8 | |
| arenoxacin | 0.06-2 | 0.5 | 1 | |
| Vancomycin | 0.12-1 | 0.5 | 1 | |
| Quinupristin-dalfopristin | 0.5-2 | 1 | 1 | |
| Linezolid | 0.25-1 | 1 | 1 | |
| Imipenem | ≦0.004-0.5 | 0.06 | 0.25 | |
| Ceftriaxone | 0.008-4 | 0.25 | 1 | |
| Benzylpenicillin | ≦0.004-4 | 0.25 | 4 | |
| Streptococcus pyogenes (49) | ||||
| DX-619 | 0.008-0.015 | 0.008 | 0.015 | |
| Levofloxacin | 0.25-2 | 0.5 | 1 | |
| Sitafloxacin | 0.015-0.06 | 0.03 | 0.06 | |
| Ciprofloxacin | 0.25-2 | 0.5 | 1 | |
| Moxifloxacin | 0.12-0.5 | 0.25 | 0.5 | |
| Gatifloxacin | 0.25-0.5 | 0.25 | 0.5 | |
| Garenoxacin | 0.06-0.25 | 0.12 | 0.25 | |
| Vancomycin | 0.5-1 | 0.5 | 1 | |
| Teicoplanin | 0.12-0.25 | 0.25 | 0.25 | |
| Quinupristin-dalfopristin | 0.25-0.5 | 0.5 | 0.5 | |
| Linezolid | 0.25-1 | 0.5 | 1 | |
| Imipenem | ≦0.004-0.008 | ≦0.004 | 0.008 | |
| Ceftriaxone | ≦0.004-0.03 | 0.03 | 0.03 | |
| Benzylpenicillin | ≦0.004-0.015 | 0.015 | 0.015 | |
| Streptococcus agalactiae (19) | ||||
| DX-619 | 0.008-0.12 | 0.015 | 0.12 | |
| Levofloxacin | 0.5-32 | 1 | 32 | |
| Sitafloxacin | 0.06-1 | 0.06 | 0.5 | |
| Ciprofloxacin | 0.5-32 | 1 | 32 | |
| Moxifloxacin | 0.12-8 | 0.25 | 8 | |
| Gatifloxacin | 0.25-8 | 0.25 | 8 | |
| Garenoxacin | 0.06-4 | 0.12 | 4 | |
| Vancomycin | 0.5-2 | 1 | 1 | |
| Teicoplanin | 0.12-0.5 | 0.5 | 0.5 | |
| Quinupristin-dalfopristin | 0.5 | 0.5 | 0.5 | |
| Linezolid | 1-2 | 1 | 2 | |
| Imipenem | 0.015-0.03 | 0.03 | 0.03 | |
| Ceftriaxone | 0.06-0.25 | 0.12 | 0.12 | |
| Benzylpenicillin | 0.06-0.12 | 0.06 | 0.12 | |
| Enterococcus faecalis | ||||
| Vancomycin susceptible (50) | ||||
| DX-619 | 0.03-0.5 | 0.06 | 0.25 | |
| Levofloxacin | 1-128 | 2 | 32 | |
| Sitafloxacin | 0.06-4 | 0.12 | 2 | |
| Ciprofloxacin | 0.5-64 | 1 | 64 | |
| Moxifloxacin | 0.12-16 | 0.25 | 8 | |
| Gatifloxacin | 0.25-32 | 0.5 | 16 | |
| Garenoxacin | 0.12-8 | 0.25 | 4 | |
| Vancomycin | 1-4 | 1 | 2 | |
| Teicoplanin | 0.12-0.5 | 0.25 | 0.5 | |
| Quinupristin-dalfopristin | 4-32 | 8 | 16 | |
| Linezolid | 1-2 | 2 | 2 | |
| Imipenem | 1-4 | 1 | 4 | |
| Vancomycin resistant (18) | ||||
| DX-619 | 0.015-0.5 | 0.25 | 0.5 | |
| Levofloxacin | 0.5-64 | 32 | 64 | |
| Sitafloxacin | 0.06-4 | 2 | 4 | |
| Ciprofloxacin | 0.25-128 | 32 | 64 | |
| Moxifloxacin | 0.12-32 | 16 | 32 | |
| Gatifloxacin | 0.25-32 | 16 | 32 | |
| Garenoxacin | 0.06-8 | 4 | 8 | |
| Vancomycin | 8->128 | >128 | >128 | |
| Teicoplanin | 0.25-128 | 64 | 128 | |
| Quinupristin-dalfopristin | 0.5-16 | 8 | 16 | |
| Linezolid | 2 | 2 | 2 | |
| Imipenem | 1-128 | 2 | 64 | |
| Enterococcus faecium | ||||
| Vancomycin susceptible (47) | ||||
| DX-619 | 0.03-4 | 1 | 2 | |
| Levofloxacin | 1-128 | 16 | 64 | |
| Sitafloxacin | 0.06-8 | 1 | 4 | |
| Ciprofloxacin | 1->64 | 16 | 64 | |
| Moxifloxacin | 0.25-64 | 8 | 32 | |
| Gatifloxacin | 0.25-32 | 16 | 32 | |
| Garenoxacin | 0.25-64 | 8 | 32 | |
| Vancomycin | 0.5-2 | 1 | 1 | |
| Teicoplanin | 0.25-2 | 0.5 | 1 | |
| Quinupristin-dalfopristin | 0.25-16 | 0.5 | 2 | |
| Linezolid | 2 | 2 | 2 | |
| Imipenem | 2->128 | >128 | >128 | |
| Vancomycin resistant (19) | ||||
| DX-619 | 0.06-4 | 0.25 | 2 | |
| Levofloxacin | 2-64 | 4 | 64 | |
| Sitafloxacin | 0.12-8 | 0.5 | 8 | |
| Ciprofloxacin | 1->128 | 4 | >128 | |
| Moxifloxacin | 0.5-32 | 4 | 32 | |
| Gatifloxacin | 0.5-32 | 4 | 32 | |
| Garenoxacin | 0.25-32 | 8 | 32 | |
| Vancomycin | 32->128 | >128 | >128 | |
| Teicoplanin | 0.5-64 | 32 | 64 | |
| Quinupristin-dalfopristin | 0.5-4 | 0.5 | 2 | |
| Linezolid | 2 | 2 | 2 | |
| Imipenem | 16->128 | >128 | >128 | |
| Enterococcus gallinarum Vancomycin resistant (13) | ||||
| DX-619 | 0.12-2 | 1 | 2 | |
| Levofloxacin | 2-64 | 16 | 64 | |
| Sitafloxacin | 0.25-8 | 2 | 8 | |
| Ciprofloxacin | 2->128 | 128 | >128 | |
| Moxifloxacin | 0.5-32 | 4 | 32 | |
| Gatifloxacin | 0.5-64 | 8 | 32 | |
| Garenoxacin | 0.25-8 | 2 | 8 | |
| Vancomycin | 8->128 | >128 | >128 | |
| Teicoplanin | 0.5->128 | 32 | >128 | |
| Quinupristin-dalfopristin | 0.25-2 | 0.5 | 2 | |
| Linezolid | 2 | 2 | 2 | |
| Imipenem | 1->128 | >128 | >128 | |
| Peptostreptococcus spp. (13) | ||||
| DX-619 | ≦0.004-1 | 0.06 | 0.5 | |
| Levofloxacin | 0.06-32 | 4 | 16 | |
| Sitafloxacin | 0.015-2 | 0.06 | 0.5 | |
| Ciprofloxacin | 0.12-16 | 2 | 8 | |
| Moxifloxacin | 0.03-32 | 0.25 | 2 | |
| Gatifloxacin | 0.03-128 | 0.12 | 32 | |
| Garenoxacin | 0.12-64 | 1 | 8 | |
| Vancomycin | 0.25-4 | 0.25 | 1 | |
| Teicoplanin | 0.06-0.12 | 0.12 | 0.12 | |
| Quinupristin-dalfopristin | 0.25-0.5 | 0.5 | 0.5 | |
| Linezolid | 0.5-1 | 1 | 1 | |
| Imipenem | ≦0.004-1 | 0.03 | 0.12 | |
| Ceftriaxone | 0.06->128 | 0.25 | 4 | |
| Clostridium difficile (17) | ||||
| DX-619 | 0.25-32 | 2 | 2 | |
| Levofloxacin | 4-128 | 64 | 128 | |
| Sitafloxacin | 0.25-32 | 1 | 2 | |
| Ciprofloxacin | 16-64 | 32 | 64 | |
| Moxifloxacin | 2-128 | 32 | 32 | |
| Gatifloxacin | 2-64 | 32 | 32 | |
| Garenoxacin | 1-128 | 32 | 64 | |
| Vancomycin | 1-4 | 2 | 2 | |
| Teicoplanin | 0.06-0.25 | 0.12 | 0.25 | |
| Quinupristin-dalfopristin | 1-2 | 1 | 2 | |
| Linezolid | 0.5-4 | 1 | 4 | |
| Imipenem | 8-32 | 16 | 16 | |
| Ceftriaxone | 16->128 | 128 | >128 | |