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

Development of a Cyclodextrin-Based Drug Delivery System to Improve the Physicochemical Properties of Ceftobiprole as a Model Antibiotic. (PubMed, Int J Mol Sci) - "The most promising formulation was a ternary system of ceftobiprole, maleic acid, and SBE-β-CD (1:25:4 molar ratio), showing ~300-fold solubility improvement, low levels of degradation products, and stability after eight months at -20 °C. After pH adjustment to a parenterally acceptable level, the formulation demonstrated solubility and a pH comparable to the marketed drug product."

Journal

Stability of Ceftobiprole Medocaril in Portable Elastomeric Infusion Devices. (PubMed, Infect Dis Ther) - "Ceftobiprole medocaril is suitable for administration in OPAT at 6.25 mg/mL in sodium chloride 0.9% over 24 h at 25 °C using Accufuser® portable elastomeric infusion devices. These findings support the development of practical administration protocols for ceftobiprole medocaril in home-based antimicrobial therapy. Ceftobiprole medocaril is a new antibiotic used to treat serious infections. Because it was recently introduced, there is limited information about its stability when used for outpatient parenteral antimicrobial therapy (OPAT), a treatment that allows patients to receive intravenous antibiotics at home using portable elastomeric infusion devices. This study examined how stable ceftobiprole medocaril remains when stored and administered in portable elastomeric infusion devices. The antibiotic was diluted in two commonly used fluids (saline and dextrose) and kept at different temperatures: refrigerated (2-8 °C), room temperature..."

Journal • Infectious Disease

Use of Daptomycin to Manage Severe MRSA Infections in Humans. (PubMed, Antibiotics (Basel)) - "The data suggest that treatment with high-dose (8-10 mg kg⁻1) DAP shortened the time to blood-culture sterilisation by a median of 2 days compared with standard-dose vancomycin without increasing toxicity when model-informed area-under-the-curve monitoring was employed. Particular attention is given to the synergistic effects of DAP combined with fosfomycin or β-lactams, especially ceftaroline and ceftobiprole, in overcoming persistent and refractory MRSA infections; this approach results in a reduction in microbiological failure relative to monotherapy...Despite promising preclinical and clinical evidence supporting combination strategies, further randomized controlled trials are necessary to establish their definitive role in clinical practice, as are head-to-head cost-effectiveness evaluations. DAP remains a critical option in the evolving landscape of MRSA management, provided its use is integrated with precision dosing, resistance surveillance, and..."

Journal • Review • Infectious Disease

Ceftobiprole versus ceftriaxone ± linezolid in Community-Acquired Bacterial Pneumonia (CABP): Re-analysis of a randomized, phase 3 study using 2020 FDA guidance. (PubMed, PLoS One) - "Ceftobiprole was non-inferior to ceftriaxone ± linezolid for clinical success at Day 3 according to the current 2020 FDA CABP Guidance."

Clinical • Journal • P3 data • Cough • Infectious Disease • Pain • Pneumonia • Respiratory Diseases

In Vitro Activity of Novel Antibiotics Against Corynebacterium spp. Clinical Isolates Responsible for Difficult-to-Treat Infections. (PubMed, Microb Drug Resist) - "The activity of ceftaroline (MIC90 >2 mg/L), ceftobiprole (MIC90 >8 mg/L), and delafloxacin (MIC90 >1 mg/L) was limited. By contrast, other molecules tested showed higher activity with low MIC90 values: linezolid (MIC90 ≤0.5 mg/L), tedizolid (MIC90 = 0.12 mg/L), dalbavancin (MIC90 = 0.12 mg/L), tigecycline (MIC90 = 0.12 mg/L), eravacycline (MIC90 = 0.06 mg/L), and omadacycline (MIC90 = 0.5 mg/L). One C. striatum strain exhibited a high level of daptomycin resistance after antibiotic exposure (MIC >16 mg/L). The in vitro activity of most of these novel antibiotics is excellent against Corynebacterium clinical isolates. They could represent a real alternative for treating DTT infections due to Corynebacterium spp."

Journal • Preclinical • Infectious Disease

Antimicrobial Susceptibility Testing of 26,908 Gram-Positive Pathogens Isolated from Patients in Canadian Hospitals: 18 Years of the CANWARD Study 2007-2024 (ASM Microbe 2025) - "MRSA susceptibility rates were: ceftobiprole (BPR) 100%; linezolid (LZD), vancomycin (VAN), and daptomycin (DAP) 99.9%; dalbavancin (DAL) 99.8%, tigecycline (TGC) 98.2%; and trimethoprim/sulfamethoxazole 94.7%. VRE susceptibility rates were: TGC 97.3%; DAP 95.7%; LZD 86.1%; nitrofurantoin (NIT) 17.3%; and ciprofloxacin 0%. SPN susceptibility rates were: VAN 100%; LZD 99.9%; ceftriaxone 99.4%; moxifloxacin 99.1%; amoxicillin/clavulanate 97.7%; doxycycline 86.3%; PEN 82.6%; and clarithromycin 78.3%... MSSA, MRSA, SPN, other Streptococcus spp., and E. faecalis are the most common GP pathogens in Canadian hospitals. MRSA rates in 2007 (26.1%) and 2024 (26.7%) were similar as were VRE rates (2007, 3.8%; 2024, 4.2%); however, year-to-year fluctuations were observed. For SPN, PEN-I rates decreased from 2007 to 2024 while the PEN-R rate was unchanged."

Clinical • Gram positive • Infectious Disease • Pneumococcal Infections • Pneumonia

In Vitro Activity of Ceftobiprole Against Pathogens Isolated from Patients in Canadian Hospitals: CANWARD Study 2015-2023 (ASM Microbe 2025) - "Ceftobiprole inhibited 100% of MSSA and MRSA isolates at ≤4 μg/ml and 100% of penicillin-resistant Streptococcus pneumoniae at ≤0.5 μg/ml (Health Canada MIC susceptible breakpoints). Breakpoints have not been published for E. faecalis, however, it's in vitro activity based on the MICs generated was comparable to S. aureus. Ceftobiprole's in vitro activity was comparable to cefepime and ceftriaxone against E. coli and K. pneumoniae."

Preclinical • Infectious Disease • Pneumococcal Infections • Pneumonia • Respiratory Diseases

Antimicrobial Susceptibility of 35,459 Gram-Negative Pathogens Isolated from Patients in Canadian Hospitals: 18 Years of the CANWARD Study 2007-2024 (ASM Microbe 2025) - "Susceptibility rates for E. coli were: meropenem/vaborbactam (MV) 100%; meropenem (MER) and tigecycline (TGC) 99.9%; ertapenem (ERT) 99.6%; ceftolozane/tazobactam (C/T) 99.1%; piperacillin/tazobactam (PTZ) 95.5%; ceftobiprole (BPR) 91.2%; gentamicin (GEN) 89.9%; ceftriaxone (CTR) 89.4%; amoxicillin/clavulanate 79.8%; ciprofloxacin (CIP) 73.9%; and trimethoprim-sulfamethoxazole (SXT) 72.7%. Susceptibility rates for P. aeruginosa were: C/T 96.7%; colistin (COL, MIC ≤2 μg/mL) 96.3%; M/V 92.1% (MIC ≤8 μg/mL); PTZ 80.0%; ceftazidime (CAZ) 78.1%; MER 78.0%; BPR (MIC ≤8 μg/mL) 77.2%; and CIP 68.6%... E. coli, K. pneumoniae, other Enterobacterales species, P. aeruginosa, and H. influenzae were the most common GN pathogens in Canadian hospitals. ESBL-producing E. coli (3.4%-12.6%) and K. pneumoniae (1.5%-13.7%) increased from 2007 to 2024 while CRE remained <1%. MDR P. aeruginosa increased (10.3-12.8%) over time."

Clinical • Gram negative • Infectious Disease • Influenza • Pneumonia • Respiratory Diseases

Adjunctive β-lactams for Staphylococcus aureus bacteremia: a narrative review. (PubMed, Ther Adv Infect Dis) - "Approaches such as the Desirability of Outcome Ranking (DOOR) and Response Adjusted for Duration of Antibiotic Risk (RADAR) enable holistic evaluations of treatment efficacy and safety, accounting for the overall patient experience. Future research should prioritize individualized treatment strategies, leveraging biomarkers and refined risk stratification to identify patients most likely to benefit from adjunct β-lactam therapy while minimizing adverse events."

Journal • Review • Acute Kidney Injury • Infectious Disease • Nephrology • Renal Disease

Ceftobiprole in cystic fibrosis: a case series. (PubMed, JAC Antimicrob Resist) - "Its broad-spectrum coverage may help to reduce polypharmacy. However, further clinical studies are needed."

Journal • Cystic Fibrosis • Genetic Disorders • Immunology • Infectious Disease • Inflammation • Pulmonary Disease • Respiratory Diseases

Pharmacophore modeling, 2D-QSAR, molecular docking and ADME studies for the discovery of inhibitors of PBP2a in MRSA. (PubMed, J Biomol Struct Dyn) - "The study led to the development of a satisfactory, predictive and significant 2D-QSAR model for predicting anti-MRSA activity of compounds and also led to the identification of two molecules: C21H25N7O4S2 (ChEMBL30602) and C20H17NO6S (ChEMBL304837) with favorable pharmacophore features and ADME properties with potential to bind strongly to PBP2a receptor of MRSA. MD simulation analysis showed that the interactions of C20H17NO6S (ChEMBL304837) with PBP2a over 100 ns was more stable and similar to the interaction of ceftobiprole with PBP2a and may become potential drug candidate against MRSA which has developed a lot of resistance to current antibiotics."

Journal • Infectious Disease

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