Category Ranking
98%
Total Visits
921
Avg Visit Duration
2 minutes
Citations
20
Article Abstract
Ceftobiprole medocaril, the most advanced of the anti-MRSA (methicillin-resistant Staphylococcus aureus) beta-lactams in clinical development, has recently completed its first Phase III clinical trial, and has demonstrated non-inferiority to vancomycin. Phase II clinical trials have been initiated with PPI0903, which is, like ceftobiprole medocaril, an injectable pro-drug of a broad-spectrum cephalosporin with anti-MRSA activity, and with RO4908643, a carbapenem with more modest activity against MRSA.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.coph.2006.06.002 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Development of a Cyclodextrin-Based Drug Delivery System to Improve the Physicochemical Properties of Ceftobiprole as a Model Antibiotic.
Int J Mol Sci
June 2025
Department of Synthetic Drugs, National Medicines Institute, Chełmska 30/34, 00-725 Warsaw, Poland.
This study presents a methodology for developing a cyclodextrin-based delivery system for ceftobiprole, a poorly water-soluble and amphoteric drug, chemically stable in acidic conditions. Ceftobiprole is a broad-spectrum cephalosporin antibiotic administered clinically as its water-soluble prodrug, ceftobiprole medocaril, due to limited aqueous solubility of the parent compound. Solubility enhancement was achieved through complexation with anionic sulfobutylether-β-cyclodextrin (SBE-β-CD).
View Article and Find Full Text PDFStability of Ceftobiprole Medocaril in Portable Elastomeric Infusion Devices.
Infect Dis Ther
August 2025
Service of Infectious Diseases, Hospital Universitario Ramón y Cajal, IRYCIS, CIBERINFEC, Madrid, Spain.
Introduction: Ceftobiprole medocaril is a new fifth-generation cephalosporin commercially available as a prodrug. Since it is newly introduced in therapy, there is limited data on its physicochemical stability for outpatient parenteral antimicrobial therapy (OPAT). This work aimed to demonstrate the suitability of ceftobiprole medocaril in OPAT, determining the physicochemical stability within portable elastomeric infusion devices (Accufuser C0100L 10 mL/h 300 mL).
View Article and Find Full Text PDFMedoxomil Prodrug Strategies.
J Med Chem
May 2025
Department of Medicinal Chemistry and Institute for Therapeutics Discovery and Development, University of Minnesota, 717 Delaware Street, SE, Minneapolis, Minnesota 55414, United States.
Drug discovery campaigns often face biopharmaceutical challenges, some of which can be solved by a prodrug approach. Prodrugs are enzymatically or chemically transformed in vivo to produce active drugs. Among these, medoxomil promoieties have been judiciously employed in multiple drug discovery campaigns, leading to three prodrugs gaining FDA approval: azilsartan medoxomil (), olmesartan medoxomil (), and ceftobiprole medocaril (), and one approval in Japan: prulifloxacin ().
View Article and Find Full Text PDFCeftobiprole medocaril for skin and skin-structure infections.
Expert Opin Drug Metab Toxicol
May 2025
Department of Medicine, Weill Cornell Medicine, New York, NY, USA.
Introduction: On 3 April 2024, the United States Food and Drug Administration (FDA) approved ceftobiprole medocaril sodium (Zevtera) for injection for the treatment of adults with acute bacterial skin and skin structure infections (ABSSSI) as well as patients with Staphylococcus aureus bloodstream infections and patients 3 months to less than 18 years old with community-acquired bacterial pneumonia.
Areas Covered: Ceftobiprole is a fifth-generation cephalosporin that exerts antibacterial activity by binding to penicillin-binding proteins and inhibiting transpeptidases and has demonstrated broad antimicrobial activity against both Gram-positive and Gram-negative pathogens, including methicillin-resistant Staphylococcus aureus (MRSA). This manuscript involves a literature review of PubMed from 1 February 2024 through 8 January 2025.
In the first half of 2024, the US FDA approved several new drugs that have relevance for those practicing in primary care. This article, the winter 2025 edition of the journal's biannual Drug Update, highlights the following new medications: sotatercept-csrk (Winrevair), aprocitentan (Tryvio), resmetirom (Rezdiffra), berdazimer (Zelsuvmi), ceftobiprole medocaril sodium (Zevtera), sofpironium (Sofdra), and ensifentrine (Ohtuvayre).
View Article and Find Full Text PDF