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BMY 28100, a new oral cephalosporin
Abstract:
BMY 28100, a new oral cephalosporin with a (Z)-propenyl side chain at the 3 position and a p-hydroxyphenylglycyl substituent at the 7 position, was evaluated in comparison with cefaclor and cephalexin and, when appropriate, ampicillin and vancomycin. In vitro, BMY 28100 was more active than the reference cephalosporins against streptococci, Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, Haemophilus influenzae, Propionibacterium acnes, Clostridium perfringens, and Clostridium difficile. BMY 28100 was comparable to cefaclor and more active than cephalexin against Staphylococcus saprophyticus and ampicillin-susceptible strains of Branhamella catarrhalis; but against ampicillin-resistant strains of B. catarrhalis, BMY 28100 was comparable to cephalexin and more active than cefaclor. Against Neisseria gonorrhoeae, BMY 28100 was comparable to cephalexin, but less active than cefaclor. Members of the family Enterobacteriaceae overall were equally susceptible to BMY 28100 and cefaclor but were less susceptible to cephalexin. In human serum, BMY 28100 was 45% protein bound. After an oral dose to mice, 82% of the drug was recovered in urine. The oral therapeutic efficacy of BMY 28100 in systemically infected mice reflected its activity in vitro.
Insights
BMY 28100, a novel oral cephalosporin, demonstrates superior in vitro activity against various bacteria, including resistant strains. Its efficacy in mice suggests potential as a valuable new antibiotic for treating bacterial infections.
Area of Science:
- Microbiology
- Pharmacology
- Infectious Diseases
Background:
- Cephalosporins are a class of antibiotics widely used to treat bacterial infections.
- Evaluating new cephalosporin derivatives is crucial for combating antibiotic resistance.
- BMY 28100 is a novel oral cephalosporin with unique structural modifications.
Purpose of the Study:
- To assess the in vitro antimicrobial activity of BMY 28100.
- To compare BMY 28100 with established antibiotics like cefaclor and cephalexin.
- To evaluate the in vivo efficacy and pharmacokinetic properties of BMY 28100.
Main Methods:
- In vitro susceptibility testing against a panel of clinically relevant bacteria.
- Comparative analysis with cefaclor, cephalexin, ampicillin, and vancomycin.
- Protein binding, urinary recovery in mice, and oral therapeutic efficacy studies in infected mice.
Main Results:
- BMY 28100 exhibited greater in vitro activity than reference cephalosporins against many Gram-positive and Gram-negative bacteria.
- It showed comparable or superior activity against specific strains, including ampicillin-resistant Branhamella catarrhalis.
- BMY 28100 demonstrated favorable pharmacokinetic properties and therapeutic efficacy in a murine infection model.
Conclusions:
- BMY 28100 possesses a broad spectrum of potent antimicrobial activity.
- Its in vitro and in vivo profiles suggest potential as a valuable therapeutic agent.
- Further clinical evaluation is warranted to establish its role in treating bacterial infections.