Plasma and Intrapulmonary Pharmacokinetics of Ceftibuten and Ledaborbactam in Healthy Male and Female Participants 18 to ≤55 Years of Age

A Phase 1, Open-label Study to Evaluate the Safety and Plasma and Intrapulmonary Pharmacokinetics of Ceftibuten and Ledaborbactam in Healthy Adult Participants

This is a Phase 1, open-label, single-center PK study in healthy adult male and female participants between 18 and 55 years of age (both inclusive). Thirty-one participants will each undergo one standard bronchoscopy with bronchoalveolar lavage (BAL) following the fifth dose of ceftibuten-ledaborbactam etzadroxil or ceftibuten alone. BAL fluid samples and plasma samples will be collected at designated timepoints to determine the concentrations of ceftibuten, ledaborbactam, and urea.

Study Overview

• Status: Completed
• Conditions: Healthy Volunteers; Pharmacokinetics
• Intervention / Treatment: Drug: ledaborbactam etzadroxil; Drug: ceftibuten

• Study Type: Interventional
• Enrollment (Actual): 34
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • Arizona
    • Phoenix, Arizona, United States, 85032
      • Pulmonary Associates

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: Adult
• Accepts Healthy Volunteers: Yes

Description

Inclusion Criteria:

• Healthy adults 18-55 years
• Males or non-pregnant, non-lactating females
• Body Mass Index: ≥18 and ≤32 kg/m2
• Forced expiratory volume in 1 second of at least 80% of predicted value
• Laboratory values meeting defined entry criteria

Exclusion Criteria:

• History of drug allergy or hypersensitivity to penicillin, cephalosporin, or β-lactam antibacterial drug or to medications used during a bronchoscopy
• Conditions that potentially alter absorption and/or excretion of orally administered drugs
• History or presence of significant diseases, including any clinically relevant acute illness or surgery within the past 3 months
• Positive alcohol, drug, or tobacco use/test

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Non-Randomized
• Interventional Model: Parallel Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Group 1; Participants in Group 1 will undergo one standardized bronchoscopy with bronchoalveolar lavage after the fifth dose of ceftibuten-ledaborbactam etzadroxil.	Drug: ledaborbactam etzadroxil; Five doses of ledaborbactam etzadroxil will be administered orally every 12 hours; Drug: ceftibuten; Five doses of ceftibuten will be administered orally every 12 hours
Experimental: Group 2; Participants in Group 2 will undergo one standardized bronchoscopy with bronchoalveolar lavage after the fifth of dose of ceftibuten alone.	Drug: ceftibuten; Five doses of ceftibuten will be administered orally every 12 hours

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Intrapulmonary PK - AUC0-12 (ceftibuten)	Area under the curve from time zero to 12 hours	0-12 hours after 5th dose
Intrapulmonary PK - AUC0-12 (ledaborbactam)	Area under the curve from time zero to 12 hours	0-12 hours after 5th dose
Plasma PK - Cmax (ceftibuten)	Maximum concentration	0-12 hours after 5th dose
Plasma PK - Cmax (ledaborbactam)	Maximum concentration	0-12 hours after 5th dose
Plasma PK - AUC0-12 (ceftibuten)	Area under the curve from time zero to 12 hours	Time Frame: 0-12 hours after 5th dose
Plasma PK - AUC0-12 (ledaborbactam)	Area under the curve from time zero to 12 hours	0-12 hours after 5th dose
Ratios of drug exposure in ELF to plasma using the AUC values for each matrix		0-12 hours after 5th dose

Secondary Outcome Measures

Outcome Measure	Time Frame
Proportion of participants experiencing treatment-emergent adverse events (TEAEs) and serious adverse events (SAEs)	Day 1 - Day 8
Proportion of participants discontinuing study drug due to TEAEs and SAEs	Day 1 - Day 8

Collaborators and Investigators

• Sponsor: Basilea Pharmaceutica
• Collaborators: National Institute of Allergy and Infectious Diseases (NIAID)
• Investigators: Study Director: Kamal Hamed, MD, Basilea Pharmaceutica International Ltd, Allschwil

Study record dates

Study Major Dates

• Study Start (Actual): November 4, 2024
• Primary Completion (Actual): March 13, 2025
• Study Completion (Actual): March 17, 2025

Study Registration Dates

• First Submitted: October 29, 2024
• First Submitted That Met QC Criteria: October 29, 2024
• First Posted (Actual): October 30, 2024

Study Record Updates

• Last Update Posted (Actual): January 23, 2026
• Last Update Submitted That Met QC Criteria: January 22, 2026
• Last Verified: January 1, 2026

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Sulfur Compounds; Organic Chemicals; Heterocyclic Compounds; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring; Amides; beta-Lactams; Lactams; Cephalosporins; Thiazines; Ceftibuten
• Other Study ID Numbers: VNRX-7145-105

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No
• product manufactured in and exported from the U.S.: No