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Completed

NCT Number: NCT06665555

Plasma and Intrapulmonary Pharmacokinetics of Ceftibuten and Ledaborbactam in Healthy Adults (18-55 Years)

This was a Phase 1, open-label, single-center Pharmacokinetic (PK) study to evaluate plasma and intrapulmonary pharmacokinetics (PK) of ceftibuten and ledaborbactam in healthy adult participants.

Approximately 31 participants were planned to be enrolled in two groups, with approximately 25 in Group 1 and approximately six in Group 2.

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Key information

Conditions

Pharmacokinetics Healthy Volunteers

Age range

18 year–55 year

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 1

Primary location

Pulmonary Associates

Phoenix, Arizona, 85032, United States

About this study

In Group 1, participants were to receive a total of five oral doses of ceftibuten ledaborbactam etzadroxil (600 mg ceftibuten/600 mg ledaborbactam etzadroxil) every 12 hours. Following the fifth dose, each participant was to undergo one standardized bronchoscopy with bronchoalveolar lavage (BAL) at one of five designated timepoints (2, 4, 6, 8, and 12 hours), with five participants assigned to each timepoint.

In Group 2, participants were to receive a total of five doses of 600 mg oral ceftibuten alone every 12 hours. After the last dose, each participant was to undergo one standardized bronchoscopy with BAL at one of two designated timepoints (4 and 12 hours), with three participants assigned to each timepoint.

Blood samples to determine plasma concentrations of ceftibuten, ledaborbactam etzadroxil (Group 1 only), and urea were to be collected at the designated timepoints.

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

Participants must have met the following key criteria to be eligible for enrollment into the study:

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

Treatment and study plan

Ledaborbactam etzadroxil

Drug

Five doses of ledaborbactam etzadroxil administered orally every 12 hours

Ceftibuten

Drug

Five doses of ceftibuten administered orally every 12 hours

Primary outcomes

  1. Intrapulmonary PK - AUC0-12 at Steady State in Group 1: Ceftibuten and Ledaborbactam Etzadroxil

    Time frame: Samples were taken at 0, 2, 4, 6, 8, and 12 hours post 5th dose

    The PK parameter AUC0-12 for ceftibuten and ledaborbactam etzadroxil was assessed by standardized bronchoscopy with bronchoalveolar lavage (BAL). BAL samples were collected from each participant at one of five designated time points (2, 4, 6, 8, and 12 hours). The first aspirate was collected separately (BAL 1), while the second through the fourth aspirates were pooled (BAL 2).

    Mean concentration values at each BAL sampling time point were determined, and data from all sampling times were combined into a single dataset to calculate the AUC0-12 value for each matrix.

    AUC 0-12 was estimated using Phoenix WinNonlin Non-compartmental analysis. Each participant only contributed one ELF concentration at one time point, so the pharmacokinetic parameters for ELF were calculated using the arithmetic mean concentration at each BAL sampling time point, resulting in a single parameter estimate of ELF across all participants.

  2. Plasma Maximum Concentration (Cmax) of Ceftibuten

    Time frame: Samples were taken at 0, 2, 4, 6, 8, and 12 hours post 5th dose

    The pharmacokinetic parameter (PK) Cmax of ceftibuten assessed at at steady-state.

  3. Plasma Area Under the Curve From Time Zero to 12 Hours (AUC0-12) for Ceftibuten

    Time frame: Samples were taken at 0, 2, 4, 6, 8, and 12 hours post 5th dose

    The PK parameter AUC0-12 for ceftibuten assessed at at steady-state.

  4. Plasma Maximum Concentration (Cmax) of Ledaborbactam Etzadroxil

    Time frame: Samples were taken at 0, 2, 4, 6, 8, and 12 hours post 5th dose

    The pharmacokinetic parameter (PK) Cmax of ledaborbactam etzadroxil assessed at at steady-state.

  5. Plasma AUC0-12h for Ledaborbactam Etzadroxil

    Time frame: Samples were taken at 0, 2, 4, 6, 8, and 12 hours post 5th dose

    The pharmacokinetic parameter (PK) AUC0-12h of ledaborbactam etzadroxil assessed at at steady-state.

  6. Ratios of Drug Exposure for Ledaborbactam Etzadroxil and Ceftibuten

    Time frame: Samples were taken at 0, 2, 4, 6, 8, and 12 hours post 5th dose

    Drug penetration ratio of epithelial lining fluid (ELF) to unbound plasma were assessed using the AUC values for each matrix for BAL 1 and BAL 2. BAL samples were collected from each participant at one of five designated time points (2, 4, 6, 8, and 12 hours). The first aspirate was collected separately (BAL 1), while the second through the fourth aspirates were pooled (BAL 2).

    All pharmacokinetic parameters (PK) were estimated using Phoenix WinNonlin Non-compartmental analysis. Each participant only contributed one ELF concentration at one time point, so the PK parameters for ELF were calculated using the arithmetic mean concentration at each BAL sampling time point, resulting in a single parameter estimate of ELF across all participants.

  7. Ratios of Drug Exposure for Ceftibuten

    Time frame: Samples were taken at 0, 2, 4, 6, 8, and 12 hours post 5th dose

    Drug penetration ratio of epithelial lining fluid (ELF) to unbound plasma were assessed using the AUC values for each matrix for BAL 1 and BAL 2. BAL samples were collected from each participant at one of five designated time points (2, 4, 6, 8, and 12 hours). The first aspirate was collected separately (BAL 1), while the second through the fourth aspirates were pooled (BAL 2).

    All pharmacokinetic parameters (PK) were estimated using Phoenix WinNonlin Non-compartmental analysis. Each participant only contributed one ELF concentration at one time point, so the PK parameters for ELF were calculated using the arithmetic mean concentration at each BAL sampling time point, resulting in a single parameter estimate of ELF across all participants.

Secondary outcomes

  1. Number of Participants Reporting Treatment-emergent Adverse Events (TEAEs) After Administration of Ceftibuten and Ledaborbactam Etzadroxil

    Time frame: Up to Day 8

    A TEAE was defined as any event not present prior to the first administration of the study drug, or any event already present that worsens in either severity or frequency following exposure to the study drug.

Sponsors and collaborators

Lead sponsor

Basilea Pharmaceutica

Industry

Collaborators

  • Biomedical Advanced Research and Development Authority

Registry information

Official study title

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

Important dates

Study start
2024
Primary completion
2025
Study completion
2025
First posted
Oct 30, 2024
Registry last updated
Aug 24, 2026

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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