Zevtera (ceftobiprole) / Basilea, MedCap AB - LARVOL DELTA

The use of Ceftobiprole in treatment pathways in Spain: an expert panel review. (PubMed, J Glob Antimicrob Resist) - "Experts concluded that ceftobiprole may be a suitable alternative therapy in complex infections caused by Gram-positive and select Gram-negative bacteria. They agreed that use in CAP and HAP could be expanded and that there was potential for use in all unlicensed indications discussed. The panel noted the benefits of its broad spectrum in polymicrobial infections, whilst the ability to administer the drug by continuous perfusion could enable its use in outpatient settings. Further research could highlight its suitability across additional conditions and populations."

Journal • Cardiovascular • Infectious Disease • Pneumonia • Respiratory Diseases

Efficacy of Ceftobiprole and Daptomycin at Bone Concentrations Against Methicillin-Resistant Staphylococcus aureus Biofilm: Results of a Dynamic In Vitro PK/PD Model. (PubMed, Antibiotics (Basel)) - "We assessed whether CTO-DAP outperformed DAP combined with a non-anti-MRSA beta-lactam (cefazolin [CZO]). At clinically relevant concentrations, ceftobiprole and daptomycin showed similar activity against MRSA biofilms. The CTO-DAP combination showed comparable efficacy to DAP-CZO."

Journal • PK/PD data • Preclinical • Infectious Disease

Ceftobiprole in Critically Ill Patients: Proposal for New Dosage Regimens. (PubMed, Ther Drug Monit) - "The proposed dosing regimens can be used to guide ceftobiprole administration in critically ill patients. However, measurement of ceftobiprole plasma concentration remains essential, at least once, to confirm patient exposure."

Journal • Critical care • Infectious Disease • Pneumonia • Respiratory Diseases

Medoxomil Prodrug Strategies. (PubMed, J Med Chem) - "Among these, medoxomil promoieties have been judiciously employed in multiple drug discovery campaigns, leading to three prodrugs gaining FDA approval: azilsartan medoxomil (6), olmesartan medoxomil (20), and ceftobiprole medocaril (29), and one approval in Japan: prulifloxacin (35). The approach has been used for drugs spanning multiple classes to improve oral bioavailability, solubility, tissue localization, efflux, and side effect profiles. This Perspective analyzes the history and application of medoxomil prodrugs and discusses their potential for drug development."

Journal • Review

In Vitro activity of ceftobiprole against 20,255 recent clinical bacterial isolates in Canada (CANWARD 2015-2023). (PubMed, Diagn Microbiol Infect Dis) - "Ceftobiprole demonstrated potent in vitro activity against MRSA, MSSA, S. pneumoniae, S. pyogenes, ESBL-negative E. coli and K. pneumoniae, and P. mirabilis isolated from clinical specimens of patients seeking care at Canadian tertiary-care hospitals."

Journal • Preclinical • Infectious Disease • Pneumococcal Infections • Pneumonia

Management of Staphylococcus aureus Bacteremia: A Review. (PubMed, JAMA) - "Cefazolin or antistaphylococcal penicillins should be used for MSSA and vancomycin, daptomycin, or ceftobiprole for MRSA. Once S aureus susceptibilities are known, MSSA should be treated with cefazolin or an antistaphylococcal penicillin. Additional clinical management consists of identifying sites of metastatic infection and pursuing source control for identified foci of infection."

Journal • Cardiovascular • CNS Disorders • Diabetes • Immunology • Infectious Disease • Inflammation • Metabolic Disorders • Musculoskeletal Pain • Pain • Pulmonary Embolism • Rheumatology

Pharmacokinetic Characteristics and Blood-Brain Barrier Penetration of Ceftobiprole in Patients with Proposed or Confirmed Central Nervous System Infection (ChiCTR) - P=N/A | N=12 | Recruiting | Sponsor: Huashan Hospital, Fudan University; Shenzhen China Resources Gosun Pharmaceuticals Co., Ltd

New trial • Infectious Disease

Evaluation of the efficacy and safety of five generations of cephalosporins in the treatment of Staphylococcus aureus bacteremia (ChiCTR) - P=N/A | N=60 | Completed | Sponsor: Sir Run Run Shaw Hospital, Zhejiang University School of Medicine (SRRSH); Sir Run Run Shaw Hospital, Zhejiang University School of Medicine (SRRSH)

New trial

Impact of obesity on clinical outcomes in patients treated with ceftobiprole: results from Phase 3 clinical trials. (PubMed, J Antimicrob Chemother) - "This analysis further supports the efficacy and safety of ceftobiprole at current recommended doses in obese patients with SAB, ABSSSI or CABP."

Clinical data • Journal • P3 data • Genetic Disorders • Infectious Disease • Obesity • Pneumonia • Respiratory Diseases

Clinical experience with the use of ceftobiprole: study in two hospitals in northern Spain (ESCMID Global 2025) - No abstract available

Clinical

Stability of ceftobiprole medocaril in portable elastomeric infusion devices (ESCMID Global 2025) - No abstract available

Ampicillin and ceftobiprole: a potent duo against Enterococcus faecalis infective endocarditis (ESCMID Global 2025) - No abstract available

Cardiovascular

Ceftobiprole alone versus in combination with ampicillin against borderline penicillin-resistant, vancomycin-resistant Enterococcus faecalis (ESCMID Global 2025) - No abstract available

Combination therapy • Cardiovascular

In vitro activity of ceftobiprole against Staphylococcus aureus: Current experience. (PubMed, Rev Argent Microbiol) - No abstract available

Journal • Preclinical

Phenyl urea based adjuvants for β-lactam antibiotics against methicillin resistant Staphylococcus aureus. (PubMed, Bioorg Med Chem Lett) - "Moreover, PBP4 is also a key determinant of S. aureus resistance to fifth-generation cephalosporins (ceftobiprole and ceftaroline). We screened the previously reported pilot library, and prepared an additional series of phenyl ureas based on compound 1. Lead compounds potentiate multiple β-lactam antibiotics, lowering minimum inhibitory concentrations (MICs) below susceptibility breakpoints, with up to 64-fold reductions in MIC."

Journal • Infectious Disease • Inflammation • Musculoskeletal Diseases • Orthopedics

A Study to Assess the Effect of Ceftobiprole on the PK of Pitavastatin and on Plasma Levels of Coproporphyrin (clinicaltrials.gov) - P1 | N=12 | Completed | Sponsor: Basilea Pharmaceutica | Recruiting ➔ Completed

Biomarker • Trial completion

Ceftobiprole medocaril for skin and skin-structure infections. (PubMed, Expert Opin Drug Metab Toxicol) - "The pharmacokinetics of this drug, coupled with its favorable safety profile, suggest ceftobiprole will be an important addition to the antimicrobial armamentarium. In the future, ceftobiprole may be used alone or in combination to treat antibiotic-resistant infections, which serve as an expanding threat to patients with and without immune impairment."

Journal • Dermatology • Infectious Disease • Pneumonia • Respiratory Diseases

Molecular screening and dynamics simulation reveal potential phytocompounds in Swertia chirayita targeting the UspA1 protein of Moraxella catarrhalis for COPD therapy. (PubMed, PLoS One) - "All of these affinities were stronger than that of the control drug ceftobiprole, which had a binding score of -6.6 kcal/mol...Additionally, the compounds demonstrated strong affinity, as indicated by negative binding free energy values. Taken together, findings of this study strongly suggest that beta-amyrin and episwertenol have the potential to act as inhibitors against the UspA1 protein of M. catarrhalis, offering promising prospects for the treatment and management of COPD."

Journal • Chronic Obstructive Pulmonary Disease • Immunology • Pulmonary Disease • Respiratory Diseases

"Seesaw effect" between daptomycin and ceftobiprole in daptomycin-resistant methicillin-resistant staphylococcus aureus isolates. (PubMed, Int J Antimicrob Agents) - "The "seesaw effect" between DAP and BPR was prevalent among DAP-R MRSA isolates. This phenomenon was associated with the mprF mutations of MRSA."

Journal • Infectious Disease

Basilea reports strong 2024 full-year results with significant increase in revenue, profit and operating cash flow (GlobeNewswire) - "For the full year (FY) 2024, Basilea recognized total revenue of CHF 208.5m (FY 2023: CHF 157.6m). This included royalty income of CHF 96.7m (FY 2023: CHF 78.9m) from Cresemba, which increased by 22.6% year-on-year, and product revenue of CHF 57.8m (FY 2023: CHF 37.9m), which increased by 52.5% year-on-year...Other revenue amounted to CHF 13.7m (FY 2023: CHF 7.4m). This included CHF 10.2m BARDA reimbursements (FY 2023: CHF 4.2m) for remaining activities related to the phase 3 program for ceftobiprole and under the Other Transaction Agreement (OTA) executed in September 2024. In 2024, Basilea invested CHF 77.1m (FY 2023: CHF 77.9m) in research and development, mainly for the phase 3 program with fosmanogepix, the preclinical profiling of BAL2062 and tonabacase, the acquisition and preclinical activities for the LptA inhibitor program, the remainder of the phase 3 ceftobiprole program and for research work on compounds in the Company’s early-stage portfolio."

Commercial • Infectious Disease • Pneumonia

Checkerboard synergistic data analysis using a Hill function-based approach. (PubMed, bioRxiv) - "This analysis also provides "n" (steepness) values from column and row fits, which are themselves dependent on the other antibiotic concentration and can be exceptionally, as in the case of ceftobiprole alone (n>10). This synergistic checkerboard analysis approach is implemented in MATLAB, which performs the fits and provides statistics variable values and alternative models significance."

Journal

Current role of ceftobiprole in the treatment of hospital-acquired and community-acquired pneumonia: Expert opinion based on literature and real-life experiences. (PubMed, Expert Rev Anti Infect Ther) - "Caution is advised in patients at high risk of ESBL-producing organisms or MDR Pseudomonas aeruginosa infections, where combination therapy is recommended. Moreover, therapeutic drug monitoring is recommended to improve outcomes, particularly in complex clinical conditions."

Journal • Review • Infectious Disease • Pneumonia • Respiratory Diseases

A Study to Assess the Effect of Ceftobiprole on the PK of Pitavastatin and on Plasma Levels of Coproporphyrin (clinicaltrials.gov) - P1 | N=12 | Recruiting | Sponsor: Basilea Pharmaceutica

Biomarker • New P1 trial

Evaluation of ampicillin plus ceftobiprole combination therapy in treating Enterococcus faecalis infective endocarditis and bloodstream infection. (PubMed, Sci Rep) - "In cases where a bactericidal effect of ceftobiprole alone was not evident, synergism with ampicillin and bactericidal activity were demonstrated instead. The prolonged infusion of ceftobiprole, either alone or with ampicillin, emerges as a valuable option for the treatment of severe invasive E. faecalis infections."

Journal • Retrospective data • Cardiovascular • Infectious Disease

The Drug Update: Recent drug approvals, winter 2025 edition. (PubMed, Nurse Pract) - "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)."

Journal