Cedax (ceftibuten dihydrate) / Currax - LARVOL DELTA

Association between Targeted Therapy and Survival in Patients with MDS (ASH 2024) - "Targeted therapy was recorded if patients had claims for ivosidenib (IDH1), enasidenib (IDH2), luspatercept (SF3B1), or cedaxuridine (TP53) in the Symphony administrative claims data. In addition, our study confirms that a significant number of biomarker-positive MDS patients do not receive targeted therapies, highlighting challenges such as disparities in access to care and provider awareness. Addressing these issues is essential to ensure all eligible patients benefit from advancements in targeted therapies, ultimately improving survival and quality of life."

Clinical • Hematological Malignancies • Myelodysplastic Syndrome • Oncology • IDH1 • IDH2 • SF3B1 • TP53

P1, DDI & MAD PK and Safety Study of Xeruborbactam Oral Prodrug in Combo With Ceftibuten in Healthy Participants (clinicaltrials.gov) - P1 | N=71 | Recruiting | Sponsor: Qpex Biopharma, Inc. | Trial primary completion date: Aug 2025 ➔ Dec 2025

Trial primary completion date • Infectious Disease

Dilution susceptibility testing method evaluation for the combination of ceftibuten and avibactam against Enterobacterales. (PubMed, J Clin Microbiol) - "During anti-infective development, it is important to delineate the variables for susceptibility testing so that clinicians can confidently evaluate whether an infecting organism is resistant or susceptible to a potential therapy. This study evaluated dilution susceptibility testing methods for ceftibuten in combination with avibactam against targeted organisms (Enterobacterales) and found that broth and agar dilution testing methods agree, and this combination is recalcitrant to most variations, aside from low pH and inoculum size, in standard test parameters."

Journal • Infectious Disease • Nephrology

ETIOLOGY OF URINARY TRACT INFECTIONS IN NEONATES AND BACTERIAL RESISTANCE IN CROATIA. (PubMed, Acta Clin Croat) - "Most commonly prescribed empirical antibiotics included ceftriaxone (31.1%) and the ampicillin-gentamicin combination (10.7%)...In this study, Escherichia coli frequently exhibited antibiotic resistance to ampicillin, amoxicillin, trimethoprim-sulfamethoxazole, and gentamicin. For UTIs attributed to Klebsiella pneumoniae, the prevailing bacterial resistance was observed against gentamicin, ceftibuten, ampicillin, cefazolin, and piperacillin. The predominance of Escherichia coli as the most common pathogen causing UTI was consistent with global trends. Founded on continuous differences in bacterial resistance, this study can serve as a basis for comprehending local resistance patterns of pathogens causing neonatal UTI, highlighting the need of additional prospective research."

Journal • Retrospective data • Cardiovascular • Hypertension • Infectious Disease • Nephrology • Pneumonia • Septic Shock

VNRX-7145-106: Safety and PK of Ceftibuten-ledaborbactam Etzadroxil Fixed-dose Combination (clinicaltrials.gov) - P1 | N=46 | Active, not recruiting | Sponsor: Venatorx Pharmaceuticals, Inc. | Trial completion date: Sep 2025 ➔ Jun 2026 | Trial primary completion date: Aug 2025 ➔ Jun 2026

Trial completion date • Trial primary completion date

Human Antimicrobial Use in Bangladesh: Five-Year Trend Analysis Including COVID-19 Pandemic Era. (PubMed, Antibiotics (Basel)) - " To achieve the global target of 70% use of Access category antibiotics by 2030, the use of Watch-group antibiotics, like cefixime, azithromycin, ciprofloxacin, levofloxacin, and ceftibuten, needs to be reduced through investing in and strengthening stewardship programs and eliminating self-medication in Bangladesh. The findings of this study provide useful information to policymakers to tackle AMR in Bangladesh."

Journal • Infectious Disease • Novel Coronavirus Disease

Beta-lactams and beta-lactamase inhibitors-current developments (PubMed, Inn Med (Heidelb)) - "These included MRSA-active cephalosporins (ceftaroline and ceftobiprole), new, broadly effective combinations of beta-lactams with beta-lactamase inhibitors, and cefiderocol, a new siderophore cephalosporin that uses the bacteria's own iron uptake systems of gram-negative bacteria to better reach the site of action through the outer membrane.In addition to cefiderocol, the most important active ingredients or fixed combinations already available on the German market include ceftazidime-avibactam, ceftolozane-tazobactam, and aztreonam-avibactam. Imipenem-relebactam and meropenem-vaborbactam are also available; Cefepim-enmetazobactam was recently added...However, interesting new combinations, such as ceftibutene-avibactam for oral use, are in development. Such combinations could also enable the oral treatment of infections by some carbapenemase producers in the future."

Journal • Review • Infectious Disease

Safety and pharmacokinetics of single and multiple doses of ledaborbactam etzadroxil with or without ceftibuten in healthy volunteers. (PubMed, Antimicrob Agents Chemother) - P1 | "No clinically relevant CTB and LED PK interactions occurred with the CTB + LED-E combination. These results support further development of the CTB + LED-E combination for the treatment of complicated urinary tract infections caused by drug-resistant Enterobacterales.CLINICAL TRIALSThese studies are registered with ClinicalTrials.gov as NCT04243863 and NCT04877379."

Journal • PK/PD data • Gastroenterology • Gastrointestinal Disorder • Infectious Disease • Nephrology

Pharmacokinetics and safety of single and repeat doses of ceftibuten in healthy participants: a phase 1 dose escalation study. (PubMed, Antimicrob Agents Chemother) - P1 | "Low levels of cis-ceftibuten accumulation were observed at steady state, with accumulation ratios of 1.06, 1.09, and 1.24 for the 400 mg once daily, q12h, and q8h cohorts, respectively. Cis-ceftibuten and trans-ceftibuten recovery in urine was 47% and 6%, respectively, following a single dose of 1,200 mg.CLINICAL TRIALSThis study is registered with ClinicalTrials.gov as NCT04314206."

Journal • P1 data • PK/PD data • Fatigue • Infectious Disease • Pain

In vivo activity of ceftibuten-ledaborbactam oral combination against serine-β-lactamase-producing Enterobacterales: an assessment in the pyelonephritis and cystitis murine model. (PubMed, J Antimicrob Chemother) - "HSR exposures of ceftibuten-ledaborbactam administered q8 h and q12 h resulted in similar and marked bacterial reduction in an upper (kidney) and lower (bladder) UTI model caused by a variety of multi-drug resistant Enterobacterales."

Journal • Preclinical • Infectious Disease • Nephrology

Development of a commercial - batch and continuous flow process for Avibactam Tomilopolil (ACS-Fall 2025) - "Avibactam tomilopolil is currently in development in combination with ceftibuten as an oral antibiotic to treat certain bacterial infections...This results in multiple chemical process safety concerns like low temperature degradation onsets, high energy intermediates and chemical stability issues. This talk will focus on how both batch and flow development teams undertook different approaches to mitigate these problems, culminating in development of a commercial process and demonstration on multiple kilogram scales."

Infectious Disease

Unexploited Oral Therapeutics to Combat Resistant Klebsiella pneumoniae: It's Not the Size of the Drugs in the Fight, It's the Size of the Fight in the Drugs (ASM Microbe 2025) - "New unexploited oral BL/BLI combinations, ceftibuten/avibactam and ceftibuten/avibactam/mecillinam hold significant promise against ESBL-producing Kp. This opens up the opportunity to explore additional concentrations, alternative drug combinations, and assess the mechanistic potential in other MDR bacteria, such as Escherichia coli or Pseudomonas aeruginosa."

Infectious Disease • Pneumonia

The Fair, the Foul, and the Filamentous: Aztreonam/Avibactam Overcomes Strain-Specific Phenotypic Variability in Klebsiella pneumoniae When Targeting PBP-2 and PBP-3 (ASM Microbe 2025) - "Here, we assessed the pharmacodynamics and phenotypic responsiveness to mono and combination therapies involving aztreonam (ATM), ceftibuten (CBT), and avibactam (AVI) in several resistant isolates. ATM-induced filamentation is not consistent across resistant Kp isolates. Independent of strain-specific responses to monotherapy, ATM+AVI proved to be the superior combination as it produces a universal bulging elongated rod/filament intermediary phenotype that gives way to a "pop and kill mechanism"."

Infectious Disease • Pneumonia

In Vivo Efficacy of Ceftibuten/Ledaborbactam Human-Simulated Oral Exposures Against ESBL- and Carbapenemase Producing Enterobacterales in the Murine Complicated Urinary Tract Infection Model (CUTI) (ASM Microbe 2025) - "HSR exposures of CTB/LED administered q8h and q12h resulted in marked bacterial reduction in kidneys and bladders against a variety of CTB-resistant Enterobacterales harboring a range of β-lactamase-mediated resistance mechanisms. No significant difference in efficacy was noted between the two CTB/LED HSR despite varying the administration frequency."

Preclinical • Infectious Disease • Nephrology

PK & Safety Study of Xeruborbactam Oral Prodrug Combined With Ceftibuten in Participants With Renal Impairment (clinicaltrials.gov) - P1 | N=32 | Completed | Sponsor: Qpex Biopharma, Inc. | Recruiting ➔ Completed

Trial completion • Infectious Disease • Renal Disease

Activity of novel ceftibuten-avibactam, ceftazidime-avibactam, and comparators against a challenge set of Enterobacterales from outpatient centers and nursing homes across the United States (2022-2024). (PubMed, Antimicrob Agents Chemother) - "Susceptibility rates were as follows: cefpodoxime (2.6%), ceftriaxone (1%), ceftazidime-avibactam (99.6%), tebipenem (89%), ertapenem (94.4%), levofloxacin (26.6%), trimethoprim-sulfamethoxazole (40.2%), and fosfomycin (96.8%). Ceftibuten-avibactam demonstrates potent in vitro activity against cephalosporin non-susceptible isolates."

Journal

VNRX-7145-106: Safety and PK of Ceftibuten-ledaborbactam Etzadroxil Fixed-dose Combination (clinicaltrials.gov) - P1 | N=46 | Active, not recruiting | Sponsor: Venatorx Pharmaceuticals, Inc. | Trial completion date: May 2025 ➔ Sep 2025 | Trial primary completion date: Mar 2025 ➔ Aug 2025

Trial completion date • Trial primary completion date

Ceftibuten/ledaborbactam etzadroxil in participants with varying degrees of renal function (ESCMID Global 2025) - No abstract available

Immunology

In vitro potency of ceftibuten with xeruborbactam against β-lactamase-producing isolates of Enterobacterales (ENT) from the SENTRY global surveillance programme (ESCMID Global 2025) - No abstract available

Preclinical

Plasma and Intrapulmonary Pharmacokinetics of Ceftibuten and Ledaborbactam in Healthy Male and Female Participants 18 to ≤55 Years of Age (clinicaltrials.gov) - P1 | N=34 | Completed | Sponsor: Venatorx Pharmaceuticals, Inc. | Recruiting ➔ Completed

Trial completion

PK & Safety Study of Xeruborbactam Oral Prodrug Combined With Ceftibuten in Participants With Renal Impairment (clinicaltrials.gov) - P1 | N=32 | Recruiting | Sponsor: Qpex Biopharma, Inc. | Not yet recruiting ➔ Recruiting

Enrollment open • Infectious Disease • Renal Disease

P1, DDI & MAD PK and Safety Study of Xeruborbactam Oral Prodrug in Combo With Ceftibuten in Healthy Participants (clinicaltrials.gov) - P1 | N=71 | Recruiting | Sponsor: Qpex Biopharma, Inc. | Trial completion date: Dec 2024 ➔ Oct 2025 | Trial primary completion date: Sep 2024 ➔ Aug 2025

Trial completion date • Trial primary completion date • Infectious Disease

Cefepime-taniborbactam and ceftibuten-ledaborbactam maintain activity against KPC variants that lead to ceftazidime-avibactam resistance. (PubMed, Antimicrob Agents Chemother) - "K2/K was less affected for D179Y-containing KPC-3 variants, and robust inhibition was observed by TAN, LED, and AVI. Together, the findings illustrate a biochemical basis for FEP-TAN and CTB-LED efficacy in KPC variant-mediated CAZ-AVI resistance backgrounds, whereby the boronate inhibitors have sufficient inhibitory activity, while FEP and CTB are poor substrates and bind to the variant enzymes with reduced affinity."

Journal • Infectious Disease • Pneumonia

Evaluation of Larrea tridentata Extracts and Their Antimicrobial Effects on Strains of Clinical Interest. (PubMed, Int J Mol Sci) - "The inhibitory activities of the ethanolic extract and the Cedax® control were similar for Enterococcus faecalis. A principal component analysis was performed with X2 and ANOVA tests to identify the relationships and the effects of the extracts on bacterial inhibition, obtaining p > 0.05 with a confidence level of 95%. This research highlights the potential of L. tridentata extracts as an alternative treatment and to mitigate the growing problem of resistance to traditional antibiotics."

Journal • Hematological Disorders

VNRX-7145-106: Safety and PK of Ceftibuten-ledaborbactam Etzadroxil Fixed-dose Combination (clinicaltrials.gov) - P1 | N=46 | Active, not recruiting | Sponsor: Venatorx Pharmaceuticals, Inc. | Recruiting ➔ Active, not recruiting

Enrollment closed