Ceftobiprole: an extended-spectrum anti-methicillin-resistant Staphylococcus aureus cephalosporin.
OBJECTIVE
To summarize and evaluate the literature concerning ceftobiprole.


METHODS
Literature identification was conducted through MEDLINE (1966-February 2008) and International Pharmaceutical Abstracts (1970-February 2008) using the terms ceftobiprole, medocaril, BAL 5788, RO-5788, BAL 9141, RO 63-9141, pyrrolidinone cephalosporin, MRSA, complicated skin and skin-structure infections (cSSSIs), community-acquired pneumonia, and nosocomial pneumonia. Additional publications were identified through a review of articles and abstracts from infectious disease meetings.


METHODS
All articles in English were evaluated and all pertinent information was included.


RESULTS
Ceftobiprole medocaril is an extended-spectrum cephalosporin with activity against methicillin-resistant Staphylococcus spp., vancomycin-resistant Staphylococcus aureus, penicillin-resistant Streptococcus pneumoniae, vancomycin-resistant Enterococcus faecalis, Enterobacteriaceae, and Pseudomonas aeruginosa. Inactivity includes extended-spectrum beta-lactamase (ESBL)-producing Enterobacteriaceae and Enterococcus faecium. Preliminary data suggest that ceftobiprole may be effective with a 1-hour infusion of 500 mg every 12 hours for gram-positive infections and 500 mg every 8 hours with a 2-hour infusion for polymicrobial infections. Two clinical trials support these dosing regimens for cSSSIs. Ceftobiprole was noninferior to vancomycin in suspected gram-positive cSSSIs, with cure rates of 93.3% and 93.5%, respectively. Furthermore, ceftobiprole was noninferior to vancomycin and ceftazidime in polymicrobial cSSSIs (cure rates 90.5% vs 90.2%, respectively). Although the total number of adverse effects was similar to those of the comparator, more patients in the ceftobiprole group experienced nausea, vomiting, and dysgeusia.


CONCLUSIONS
The activity of ceftobiprole and limited clinical data suggest that it may be useful as empiric monotherapy for cSSSI and in combination with other antimicrobials in lower respiratory tract infections for which Phase 3 clinical trials are currently exploring. Although not shown in vitro, ceftobiprole may induce resistance due to its broad spectrum of activity. Approval is expected for the treatment of cSSSI.
Anderson
Shawn D
SD
Departments of Pharmacy Practice and Family Medicine, University of Florida, Gainesville, FL 32601, USA. sda2@ufl.edu
Gums
John G
JG
D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D002511:Cephalosporins / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D002986:Clinical Trials as Topic; D004347:Drug Interactions; D006090:Gram-Negative Bacteria / Q000187:drug effects; D016905:Gram-Negative Bacterial Infections / Q000188:drug therapy*; D006094:Gram-Positive Bacteria / Q000187:drug effects; D016908:Gram-Positive Bacterial Infections / Q000188:drug therapy*; D006801:Humans; D008826:Microbial Sensitivity Tests
D000900:Anti-Bacterial Agents; D002511:Cephalosporins; C505439:ceftobiprole medocaril