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WAP-8294A2 is a major component in a complex of water-soluble depsipeptide antibiotics produced by Lysobator sp.
1. Productivity :
Production of a single entity peak of WAP-8294A2 at a concentration approaching 1000mg/l in 18 hours fermentation, is obtained.
2. Efficacy :
|
WAP-8294A2 |
VCM |
| Bacterial Action |
2 hours
(bactericidal) |
24 hours
(bacteriostatic) |
| Effective Dose (i.v. mice) |
0.5 mg/kg |
40 mg/kg |
| MRSA thigh infection (s.c. mice) |
Effective |
Slightly effective |
| MRSA Aortic-Value endocarditis (rabbit) |
Effective |
Slightly effective |
Acute toxicity mice
(LD50/ED50) |
x 375 |
x 18 |
Acute toxicity beagle dog
(LD50/ED50) |
x 55 |
x 2 |
| Development of resistance |
slow |
slow |
3. WAP-8294A2's Advantages :
- Bacterial at 1MIC within 2 hours:
(Vancomycin more than 2MIC in 24 hours)
- Narrow Spectrum:
- Staphylococcus aureus & Staphylococcis epidermidis
- Bacillus including Bacillus anthracis
- Mycobacterium tuberculosis
- Increased activity in presence of serum
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