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The meaning of the development of flomoxef and clinical experience in Japan
1Product Development Department, Shionogi & Co. Ltd., Osaka, Japan.
Abstract:
Flomoxef is a fourth generation cephem which has the same activity against gram-negative bacteria as the third generation cephems, but is also active against gram-positive organisms, especially most methicillin resistant Staphylococcus aureus (MRSA). As flomoxef induces the smallest amount of PBP-2' among all cephems, it is hoped that this will be the cephem that is able to control the increase of MRSA. High plasma levels in proportion to dosage are seen with flomoxef, the transfer to various body fluids and tissue is good, and the half-life in the plasma is about 50 min. Most of the compound is excreted in the urine in the unchanged form, that is 85% in 6 h. Clinical trials in 2,494 cases with various infections showed an excellent to good response in 77.1%, and an antibacterial effect of 80 to 100%. The efficacy rate against MRSA was 83.3%. The type and incidence of side effects was common to those of other injectable cephems, and no spermatogenic or hematological side effects were observed.
Insights
Flomoxef, a fourth-generation cephem antibiotic, shows broad-spectrum activity, including against methicillin-resistant Staphylococcus aureus (MRSA). Clinical trials demonstrate its efficacy and favorable pharmacokinetic profile for treating various infections.
Area of Science:
- Pharmacology
- Infectious Diseases
- Microbiology
Background:
- Flomoxef is a fourth-generation cephem antibiotic.
- It exhibits activity against Gram-negative bacteria similar to third-generation cephems.
- Notably, it is also effective against Gram-positive organisms, including methicillin-resistant Staphylococcus aureus (MRSA).
Purpose of the Study:
- To evaluate the clinical efficacy and safety of flomoxef.
- To assess its potential in controlling the rise of MRSA infections.
- To characterize its pharmacokinetic properties.
Main Methods:
- Clinical trials involving 2,494 patients with various infections.
- Assessment of treatment response and antibacterial effects.
- Pharmacokinetic analysis of plasma levels, body fluid transfer, and excretion.
- Evaluation of side effects, including spermatogenic and hematological parameters.
Main Results:
- Flomoxef demonstrated an excellent to good response rate of 77.1% in clinical trials.
- Antibacterial effect ranged from 80% to 100%.
- Efficacy rate against MRSA was 83.3%.
- Flomoxef achieves high plasma levels, good tissue distribution, and a half-life of approximately 50 minutes.
- 85% of the drug is excreted unchanged in urine within 6 hours.
- Side effects were comparable to other injectable cephems, with no observed spermatogenic or hematological toxicity.
Conclusions:
- Flomoxef is an effective antibiotic for various infections, including those caused by MRSA.
- Its favorable pharmacokinetic profile and low induction of PBP-2' suggest a role in managing MRSA.
- The safety profile is consistent with other injectable cephems.