PharmacokineticsPhase 1NCT06665555
Plasma and Intrapulmonary Pharmacokinetics of Ceftibuten and Ledaborbactam in Healthy Adults (18-55 Years)
A Phase 1 study testing ledaborbactam etzadroxil and ceftibuten in people with Pharmacokinetics and Healthy Volunteers, run by Basilea Pharmaceutica at 1 site in United States.
Trial summary
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. Read more about this study
- Who is it for?
- Ages 18 to 55 yearsHealthy volunteers can take part
- Conditions the study is for
- Pharmacokinetics, Healthy Volunteers
- What is being tested?
- ledaborbactam etzadroxil and ceftibuten
- Type of treatment
- Pill or oral medicine
- Could I receive a placebo?
- No, everyone receives an active treatment
- How many people
- 34 participants
- Where
- 1 siteUnited States
- Study dates
- 4 Nov 2024to 17 Mar 2025
- Phase
- Phase 1
- Are there results?
- Yes, posted in the registrySummary in the doctors' view
Key requirements
Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.
- Ages 18 to 55 years
- All sexes
- Healthy volunteers accepted
- Adult
Who may be able to join
- 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
Who cannot join
- 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
Trial locations and contacts
1 site in 1 country.
About this study
Official title: A Phase 1, Open-label Study to Evaluate the Safety and Plasma and Intrapulmonary Pharmacokinetics of Ceftibuten and Ledaborbactam in Healthy Adult Participants
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.
Read the detailed description
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.
- Conditions
- Pharmacokinetics, Healthy Volunteers
- Being tested
- ledaborbactam etzadroxil, ceftibuten
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
ledaborbactam etzadroxilDrug
Five doses of ledaborbactam etzadroxil administered orally every 12 hours
ceftibutenDrug
Five doses of ceftibuten administered orally every 12 hours
| Study group | Role | What they receive |
|---|---|---|
| Group 1 | Experimental | Participants in Group 1 underwent one standardized bronchoscopy with bronchoalveolar lavage after the fifth dose of ceftibuten-ledaborbactam etzadroxil. Receives: Drug: ledaborbactam etzadroxil; Drug: ceftibuten |
| Group 2 | Experimental | Participants in Group 2 underwent one standardized bronchoscopy with bronchoalveolar lavage after the fifth of dose of ceftibuten alone. Receives: Drug: ceftibuten |
What is being measured
The primary outcome is the main question the study is designed to answer.
Intrapulmonary PK - AUC0-12 at Steady State in Group 1: Ceftibuten and Ledaborbactam Etzadroxil
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.
Measured: Samples were taken at 0, 2, 4, 6, 8, and 12 hours post 5th dose
Plasma Maximum Concentration (Cmax) of Ceftibuten
The pharmacokinetic parameter (PK) Cmax of ceftibuten assessed at at steady-state.
Measured: Samples were taken at 0, 2, 4, 6, 8, and 12 hours post 5th dose
Plasma Area Under the Curve From Time Zero to 12 Hours (AUC0-12) for Ceftibuten
The PK parameter AUC0-12 for ceftibuten assessed at at steady-state.
Measured: Samples were taken at 0, 2, 4, 6, 8, and 12 hours post 5th dose
Plasma Maximum Concentration (Cmax) of Ledaborbactam Etzadroxil
The pharmacokinetic parameter (PK) Cmax of ledaborbactam etzadroxil assessed at at steady-state.
Measured: Samples were taken at 0, 2, 4, 6, 8, and 12 hours post 5th dose
Plasma AUC0-12h for Ledaborbactam Etzadroxil
The pharmacokinetic parameter (PK) AUC0-12h of ledaborbactam etzadroxil assessed at at steady-state.
Measured: Samples were taken at 0, 2, 4, 6, 8, and 12 hours post 5th dose
Ratios of Drug Exposure for Ledaborbactam Etzadroxil and Ceftibuten
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.
Measured: Samples were taken at 0, 2, 4, 6, 8, and 12 hours post 5th dose
Ratios of Drug Exposure for Ceftibuten
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.
Measured: Samples were taken at 0, 2, 4, 6, 8, and 12 hours post 5th dose
Secondary outcomes (1)
Number of Participants Reporting Treatment-emergent Adverse Events (TEAEs) After Administration of Ceftibuten and Ledaborbactam Etzadroxil
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.
Measured: Up to Day 8
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted30 Oct 2024
- Study start4 Nov 2024
- Primary completion13 Mar 2025
- Study completion17 Mar 2025
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Posted resultsParticipant flow, outcome measures and adverse events reported by the sponsor.
- Publications (1)Papers the sponsor has linked to this study.
- Other trials for PharmacokineticsStudies of the same condition, open and under way.
- What the trial phases meanHow a treatment moves from first tests in people to approval.
More details
For doctors and researchers: how the study is designed, who runs it, and its registry IDs.
Study design
- Study type
- Interventional
- Phase
- Phase 1
- Primary purpose
- Treatment
- Allocation
- Non-randomised
- Intervention model
- Parallel groups
- Masking
- None (open label)
- Enrolment
- 34 participants (actual)
Sponsor and investigators
- Lead sponsor
- Basilea Pharmaceutica
- Sponsor type
- Industry (pharma, biotech, devices)
- Collaborators
- Biomedical Advanced Research and Development Authority
- Responsible party
- Sponsor
- Investigators
- Kamal Hamed, MD, MPH, Study director, Basilea Pharmaceutica International Ltd, Allschwil
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT06665555
- Sponsor's protocol ID
- VNRX-7145-105
- Other IDs
- HHSN272201600029C
- Status last verified
- Jul 2026
- First submitted
- 29 Oct 2024
- Last updated
- 24 Aug 2026
- Results posted
- Yes, on ClinicalTrials.gov
- Data monitoring committee
- No
- FDA-regulated drug
- Yes
- FDA-regulated device
- No
Publications
Rodvold KA, Gotfried MH, de Oliveira CF, Lowe K, Hamed KA, Litherland K, Engelhardt M, McGovern PC. Plasma and intrapulmonary pharmacokinetics of ceftibuten and ledaborbactam in healthy male and female adults. Antimicrob Agents Chemother. 2026 Jun 3;70(6):e0195025. doi: 10.1128/aac.01950-25. Epub 2026 Apr 20.
PubMed 42008649
Study at a glance
From the registry record, last updated by the sponsor on 24 Aug 2026. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official title
- A Phase 1, Open-label Study to Evaluate the Safety and Plasma and Intrapulmonary Pharmacokinetics of Ceftibuten and Ledaborbactam in Healthy Adult Participants
- ClinicalTrials.gov ID
- NCT06665555
- Acronym / sponsor ID
- VNRX-7145-105
- Conditions
- Pharmacokinetics, Healthy Volunteers
- Phase
- Phase 1
- Study type
- Interventional
- Recruitment status
- Completed
- Enrolment
- 34 participants (actual)
- Lead sponsor
- Basilea PharmaceuticaIndustry (pharma, biotech, devices)
- Collaborators
- Biomedical Advanced Research and Development Authority
- Study start
- 4 Nov 2024 (actual)
- Primary completion
- 13 Mar 2025 (actual)
- Study completion
- 17 Mar 2025 (actual)
- First posted
- 30 Oct 2024 (actual)
- Results
- Posted 24 Aug 2026
Clinical summary
The research question as the sponsor registered it. This describes what the study plans to test, not what it found.
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.
Detailed description
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.
Study design
- Primary purpose
- Treatment
- Allocation
- Non-randomised
- Intervention model
- Parallel groups
- Masking
- None (open label)
- Number of arms
- 2
| Arm | Type | Receives |
|---|---|---|
| Group 1 | Experimental | Drug: ledaborbactam etzadroxil, Drug: ceftibutenParticipants in Group 1 underwent one standardized bronchoscopy with bronchoalveolar lavage after the fifth dose of ceftibuten-ledaborbactam etzadroxil. |
| Group 2 | Experimental | Drug: ceftibutenParticipants in Group 2 underwent one standardized bronchoscopy with bronchoalveolar lavage after the fifth of dose of ceftibuten alone. |
Who may qualify
- Ages
- 18 to 55 years
- Sex
- All
- Healthy volunteers
- Accepted
- Age groups
- Adult
Key inclusion criteria (5 listed)
- 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
Key exclusion criteria (4 listed)
- 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
Eligibility is decided by the study team after screening; this overview does not establish that a patient qualifies. Full inclusion and exclusion criteria.
Interventions
| Intervention | Type | Arms |
|---|---|---|
| ledaborbactam etzadroxilFive doses of ledaborbactam etzadroxil administered orally every 12 hours | Drug | Group 1 |
| ceftibutenFive doses of ceftibuten administered orally every 12 hours | Drug | Group 1, Group 2 |
Primary outcome
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.
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.
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.
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.
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.
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.
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.
1 secondary outcome
Number of Participants Reporting Treatment-emergent Adverse Events (TEAEs) After Administration of Ceftibuten and Ledaborbactam Etzadroxil
Time frame: Up to Day 8
Results and safety
Loading the posted results from ClinicalTrials.gov…
Research links
- Official record on ClinicalTrials.govLast updated by the sponsor 24 Aug 2026.
- Posted resultsParticipant flow, baseline, all outcome measures and adverse events.
- Results publication: PubMed 42008649Rodvold KA, Gotfried MH, de Oliveira CF, Lowe K, Hamed KA, Litherland K, Engelhardt M, McGovern PC. Plasma and intrapulmonary pharmacokinetics of ceftibuten and ledaborbactam in healthy male and female adults. Antimicrob Agents Chemother. 2026 Jun 3;70(6):e0195025. doi: 10.1128/aac.01950-25. Epub 2026 Apr 20.
Related trials for Pharmacokinetics
RecruitingPhase 1
Safety and PK of Ceftibuten-ledaborbactam Etzadroxil Fixed-dose Combination
Healthy Volunteer, Pharmacokinetics
RecruitingPhase 1
Effects of Trigonelline Monohydrate on NAD+ Metabolism, Pharmacokinetics, Safety, and Tolerability in Healthy Adults
NAD+ Metabolism, Pharmacokinetics
Not yet recruitingObservational study
Pharmacokinetics and Optimal Dosing of Levetiracetam in Critically Ill Patients Undergoing Continuous Renal Replacement Therapy
Continuous Renal Replacement Therapy (CRRT), Pharmacokinetics
RecruitingPhase 1
A Randomized, Double-Blind, Positive-Controlled, Parallel Pharmacokinetic Phase I Clinical Study of Cetuximab Injection Versus Erbitux in Healthy Male Subjects
Cetuximab, Bioequivalence
RecruitingPhase 1
Safety, Tolerability, and Pharmacokinetics of RCS-21 in Healthy Volunteers.
Healthy Volunteers, Safety
Referral and contact
AzTrials does not enrol participants or take referrals. Contact the study team or a site listed below; they decide who can take part. This study is not recruiting at the moment.
Kamal Hamed, MD, MPH study director
Basilea Pharmaceutica International Ltd, Allschwil
1 site in 1 country: see every site and its status.
Questions about this trial
What is this clinical trial studying?
A Phase 1 study testing ledaborbactam etzadroxil and ceftibuten in people with Pharmacokinetics and Healthy Volunteers, run by Basilea Pharmaceutica at 1 site in United States.
The full registered description is in the About this study section and the official record.
Who may be eligible to take part?
The sponsor lists 5 inclusion and 4 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.
Is this clinical trial currently recruiting?
The record says: finished, as of the sponsor's last update on 24 Aug 2026. Status can change between updates, so confirm with the study contact before making plans.
Where is the study taking place?
The record lists 1 site in United States. Whether a site is taking part right now should be confirmed with that site. See every site.
What are the possible benefits and risks?
They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.
What does this phase mean?
Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.
Not every study follows the same path, and some studies (observational studies, device studies) have no phase.
Are results available for this study?
Yes. Results are posted in the registry (first posted 24 Aug 2026). A summary is in the For doctors view, and the full results are on ClinicalTrials.gov.
How can a doctor refer a patient or contact the research team?
The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.
What does the primary outcome measure?
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 study lists 7 primary outcomes in all. It is what the study was designed to measure, not a finding.
Where can I read the original study information?
On the ClinicalTrials.gov record for NCT06665555, which also lists 1 linked publication.
Does a listing mean the treatment is approved or proven to work?
No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.
How often is this information updated?
AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 24 Aug 2026; AzTrials last refreshed its copy on 8 Nov 2026.