Trial Outcomes & Findings for Plasma and Intrapulmonary Pharmacokinetics of Ceftibuten and Ledaborbactam in Healthy Adults (18-55 Years) (NCT NCT06665555)
NCT ID: NCT06665555
Last Updated: 2026-08-24
Results Overview
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.
COMPLETED
PHASE1
34 participants
Samples were taken at 0, 2, 4, 6, 8, and 12 hours post 5th dose
2026-08-24
Participant Flow
Participants were screened and randomized at one site in the USA
Participant milestones
| Measure |
Group 1: Ceftibuten and Ledaborbactam Etzadroxil
Participants received a total of five oral doses of ceftibuten ledaborbactam etzadroxil (600 mg ceftibuten/600 mg ledaborbactam etzadroxil) every 12 hours.
|
Group 2: Ceftibuten
Participants received a total of five doses of 600 mg oral ceftibuten alone every 12 hours.
|
|---|---|---|
|
Overall Study
STARTED
|
28
|
6
|
|
Overall Study
COMPLETED
|
27
|
6
|
|
Overall Study
NOT COMPLETED
|
1
|
0
|
Reasons for withdrawal
| Measure |
Group 1: Ceftibuten and Ledaborbactam Etzadroxil
Participants received a total of five oral doses of ceftibuten ledaborbactam etzadroxil (600 mg ceftibuten/600 mg ledaborbactam etzadroxil) every 12 hours.
|
Group 2: Ceftibuten
Participants received a total of five doses of 600 mg oral ceftibuten alone every 12 hours.
|
|---|---|---|
|
Overall Study
Adverse Event
|
1
|
0
|
Baseline Characteristics
Plasma and Intrapulmonary Pharmacokinetics of Ceftibuten and Ledaborbactam in Healthy Adults (18-55 Years)
Baseline characteristics by cohort
| Measure |
Group 1: Ceftibuten and Ledaborbactam Etzadroxil
n=28 Participants
Participants received a total of five oral doses of ceftibuten ledaborbactam etzadroxil (600 mg ceftibuten/600 mg ledaborbactam etzadroxil) every 12 hours.
|
Group 2: Ceftibuten
n=6 Participants
Participants received a total of five doses of 600 mg oral ceftibuten alone every 12 hours.
|
Total
n=34 Participants
Total of all reporting groups
|
|---|---|---|---|
|
Age, Continuous
|
38.4 years
STANDARD_DEVIATION 10.64 • n=1541 Participants
|
40.7 years
STANDARD_DEVIATION 6.74 • n=1121 Participants
|
38.8 years
STANDARD_DEVIATION 10.02 • n=2662 Participants
|
|
Sex: Female, Male
Female
|
21 Participants
n=1541 Participants
|
4 Participants
n=1121 Participants
|
25 Participants
n=2662 Participants
|
|
Sex: Female, Male
Male
|
7 Participants
n=1541 Participants
|
2 Participants
n=1121 Participants
|
9 Participants
n=2662 Participants
|
|
Race/Ethnicity, Customized
White
|
15 Participants
n=1541 Participants
|
5 Participants
n=1121 Participants
|
20 Participants
n=2662 Participants
|
|
Race/Ethnicity, Customized
Black or African American
|
7 Participants
n=1541 Participants
|
1 Participants
n=1121 Participants
|
8 Participants
n=2662 Participants
|
|
Race/Ethnicity, Customized
Asian
|
2 Participants
n=1541 Participants
|
0 Participants
n=1121 Participants
|
2 Participants
n=2662 Participants
|
|
Race/Ethnicity, Customized
Other
|
4 Participants
n=1541 Participants
|
0 Participants
n=1121 Participants
|
4 Participants
n=2662 Participants
|
|
Race/Ethnicity, Customized
Hispanic Or Latino
|
6 Participants
n=1541 Participants
|
3 Participants
n=1121 Participants
|
9 Participants
n=2662 Participants
|
|
Race/Ethnicity, Customized
Not Hispanic Or Latino
|
22 Participants
n=1541 Participants
|
3 Participants
n=1121 Participants
|
25 Participants
n=2662 Participants
|
|
Region of Enrollment
United States
|
28 Participants
n=1541 Participants
|
6 Participants
n=1121 Participants
|
34 Participants
n=2662 Participants
|
|
Weight
|
79.07 kg
STANDARD_DEVIATION 12.84 • n=1541 Participants
|
78.53 kg
STANDARD_DEVIATION 11.98 • n=1121 Participants
|
78.97 kg
STANDARD_DEVIATION 12.52 • n=2662 Participants
|
|
Height
|
173.2 cm
STANDARD_DEVIATION 9.01 • n=1541 Participants
|
169.7 cm
STANDARD_DEVIATION 7.20 • n=1121 Participants
|
172.6 cm
STANDARD_DEVIATION 8.73 • n=2662 Participants
|
|
BMI
|
26.30 kg/m^2
STANDARD_DEVIATION 3.45 • n=1541 Participants
|
27.27 kg/m^2
STANDARD_DEVIATION 3.75 • n=1121 Participants
|
26.47 kg/m^2
STANDARD_DEVIATION 3.46 • n=2662 Participants
|
PRIMARY outcome
Timeframe: Samples were taken at 0, 2, 4, 6, 8, and 12 hours post 5th dosePopulation: PK Evaluable Set: all participants who received at least one dose of study drug and had at least one evaluable plasma or BAL concentration. Participants may have been excluded from this set for relevant protocol deviations. Only five participants were evaluable for this outcome measure.
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.
Outcome measures
| Measure |
Group 1: Ceftibuten and Ledaborbactam Etzadroxil
n=5 Participants
Participants received a total of five oral doses of ceftibuten ledaborbactam etzadroxil (600 mg ceftibuten/600 mg ledaborbactam etzadroxil) every 12 hours.
|
Group 2: Ceftibuten
Participants received a total of five doses of 600 mg oral ceftibuten alone every 12 hours.
|
|---|---|---|
|
Intrapulmonary PK - AUC0-12 at Steady State in Group 1: Ceftibuten and Ledaborbactam Etzadroxil
Value for ceftibuten for BAL 1
|
14867 h*ng/mL
Standard Deviation NA
It was pre-specified in the study protocol to only calculate an arithmetic mean with no measure of dispersion using Phoenix WinNonlin Non-compartmental analysis.
|
—
|
|
Intrapulmonary PK - AUC0-12 at Steady State in Group 1: Ceftibuten and Ledaborbactam Etzadroxil
Value for ceftibuten for BAL 2
|
10486 h*ng/mL
Standard Deviation NA
It was pre-specified in the study protocol to only calculate an arithmetic mean with no measure of dispersion using Phoenix WinNonlin Non-compartmental analysis.
|
—
|
|
Intrapulmonary PK - AUC0-12 at Steady State in Group 1: Ceftibuten and Ledaborbactam Etzadroxil
Value for ledaborbactam etzadroxil for BAL 1
|
14529 h*ng/mL
Standard Deviation NA
It was pre-specified in the study protocol to only calculate an arithmetic mean with no measure of dispersion using Phoenix WinNonlin Non-compartmental analysis.
|
—
|
|
Intrapulmonary PK - AUC0-12 at Steady State in Group 1: Ceftibuten and Ledaborbactam Etzadroxil
Value for ledaborbactam etzadroxil for BAL 2
|
9809 h*ng/mL
Standard Deviation NA
It was pre-specified in the study protocol to only calculate an arithmetic mean with no measure of dispersion using Phoenix WinNonlin Non-compartmental analysis.
|
—
|
PRIMARY outcome
Timeframe: Samples were taken at 0, 2, 4, 6, 8, and 12 hours post 5th dosePopulation: PK Evaluable Set: all participants who received at least one dose of study drug and had at least one evaluable plasma or BAL concentration. Participants may have been excluded from this set for relevant protocol deviations.
The pharmacokinetic parameter (PK) Cmax of ceftibuten assessed at at steady-state.
Outcome measures
| Measure |
Group 1: Ceftibuten and Ledaborbactam Etzadroxil
n=25 Participants
Participants received a total of five oral doses of ceftibuten ledaborbactam etzadroxil (600 mg ceftibuten/600 mg ledaborbactam etzadroxil) every 12 hours.
|
Group 2: Ceftibuten
n=6 Participants
Participants received a total of five doses of 600 mg oral ceftibuten alone every 12 hours.
|
|---|---|---|
|
Plasma Maximum Concentration (Cmax) of Ceftibuten
|
22708 ng/mL
Standard Deviation 5317
|
21017 ng/mL
Standard Deviation 9828
|
PRIMARY outcome
Timeframe: Samples were taken at 0, 2, 4, 6, 8, and 12 hours post 5th dosePopulation: PK Evaluable Set: all participants who received at least one dose of study drug and had at least one evaluable plasma or BAL concentration. Participants may have been excluded from this set for relevant protocol deviations.
The PK parameter AUC0-12 for ceftibuten assessed at at steady-state.
Outcome measures
| Measure |
Group 1: Ceftibuten and Ledaborbactam Etzadroxil
n=25 Participants
Participants received a total of five oral doses of ceftibuten ledaborbactam etzadroxil (600 mg ceftibuten/600 mg ledaborbactam etzadroxil) every 12 hours.
|
Group 2: Ceftibuten
n=6 Participants
Participants received a total of five doses of 600 mg oral ceftibuten alone every 12 hours.
|
|---|---|---|
|
Plasma Area Under the Curve From Time Zero to 12 Hours (AUC0-12) for Ceftibuten
|
121799 h*ng/mL
Standard Deviation 27105
|
110962 h*ng/mL
Standard Deviation 46516
|
PRIMARY outcome
Timeframe: Samples were taken at 0, 2, 4, 6, 8, and 12 hours post 5th dosePopulation: PK Evaluable Set: all participants who received at least one dose of study drug and had at least one evaluable plasma or BAL concentration. Participants may have been excluded from this set for relevant protocol deviations.
The pharmacokinetic parameter (PK) Cmax of ledaborbactam etzadroxil assessed at at steady-state.
Outcome measures
| Measure |
Group 1: Ceftibuten and Ledaborbactam Etzadroxil
n=25 Participants
Participants received a total of five oral doses of ceftibuten ledaborbactam etzadroxil (600 mg ceftibuten/600 mg ledaborbactam etzadroxil) every 12 hours.
|
Group 2: Ceftibuten
Participants received a total of five doses of 600 mg oral ceftibuten alone every 12 hours.
|
|---|---|---|
|
Plasma Maximum Concentration (Cmax) of Ledaborbactam Etzadroxil
|
15796 ng/mL
Standard Deviation 2754
|
—
|
PRIMARY outcome
Timeframe: Samples were taken at 0, 2, 4, 6, 8, and 12 hours post 5th dosePopulation: PK Evaluable Set: all participants who received at least one dose of study drug and had at least one evaluable plasma or BAL concentration. Participants may have been excluded from this set for relevant protocol deviations.
The pharmacokinetic parameter (PK) AUC0-12h of ledaborbactam etzadroxil assessed at at steady-state.
Outcome measures
| Measure |
Group 1: Ceftibuten and Ledaborbactam Etzadroxil
n=25 Participants
Participants received a total of five oral doses of ceftibuten ledaborbactam etzadroxil (600 mg ceftibuten/600 mg ledaborbactam etzadroxil) every 12 hours.
|
Group 2: Ceftibuten
Participants received a total of five doses of 600 mg oral ceftibuten alone every 12 hours.
|
|---|---|---|
|
Plasma AUC0-12h for Ledaborbactam Etzadroxil
|
70406 ng x h/mL
Standard Deviation 12964
|
—
|
PRIMARY outcome
Timeframe: Samples were taken at 0, 2, 4, 6, 8, and 12 hours post 5th dosePopulation: PK Evaluable Set: all participants who received at least one dose of study drug and had at least one evaluable plasma or BAL concentration. Participants may have been excluded from this set for relevant protocol deviations. Only five participants were evaluable for this outcome measure.
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.
Outcome measures
| Measure |
Group 1: Ceftibuten and Ledaborbactam Etzadroxil
n=5 Participants
Participants received a total of five oral doses of ceftibuten ledaborbactam etzadroxil (600 mg ceftibuten/600 mg ledaborbactam etzadroxil) every 12 hours.
|
Group 2: Ceftibuten
Participants received a total of five doses of 600 mg oral ceftibuten alone every 12 hours.
|
|---|---|---|
|
Ratios of Drug Exposure for Ledaborbactam Etzadroxil and Ceftibuten
Ratio for BAL 1 for ceftibuten
|
0.341 Ratio
Standard Deviation NA
It was pre-specified in the study protocol to only calculate an arithmetic mean with no measure of dispersion using Phoenix WinNonlin Non-compartmental analysis.
|
—
|
|
Ratios of Drug Exposure for Ledaborbactam Etzadroxil and Ceftibuten
Ratio for BAL 2 for ceftibuten
|
0.239 Ratio
Standard Deviation NA
It was pre-specified in the study protocol to only calculate an arithmetic mean with no measure of dispersion using Phoenix WinNonlin Non-compartmental analysis.
|
—
|
|
Ratios of Drug Exposure for Ledaborbactam Etzadroxil and Ceftibuten
Ratio for BAL 1 for ledaborbactam etzadroxil
|
1.560 Ratio
Standard Deviation NA
It was pre-specified in the study protocol to only calculate an arithmetic mean with no measure of dispersion using Phoenix WinNonlin Non-compartmental analysis.
|
—
|
|
Ratios of Drug Exposure for Ledaborbactam Etzadroxil and Ceftibuten
Ratio for BAL 2 for ledaborbactam etzadroxil
|
1.032 Ratio
Standard Deviation NA
It was pre-specified in the study protocol to only calculate an arithmetic mean with no measure of dispersion using Phoenix WinNonlin Non-compartmental analysis.
|
—
|
PRIMARY outcome
Timeframe: Samples were taken at 0, 2, 4, 6, 8, and 12 hours post 5th dosePopulation: PK Evaluable Set: all participants who received at least one dose of study drug and had at least one evaluable plasma or BAL concentration. Participants may have been excluded from this set for relevant protocol deviations. Only five participants were evaluable for this outcome measure.
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.
Outcome measures
| Measure |
Group 1: Ceftibuten and Ledaborbactam Etzadroxil
n=5 Participants
Participants received a total of five oral doses of ceftibuten ledaborbactam etzadroxil (600 mg ceftibuten/600 mg ledaborbactam etzadroxil) every 12 hours.
|
Group 2: Ceftibuten
Participants received a total of five doses of 600 mg oral ceftibuten alone every 12 hours.
|
|---|---|---|
|
Ratios of Drug Exposure for Ceftibuten
Ratio for BAL 1 for ceftibuten
|
0.272 Ratio
Standard Deviation NA
It was pre-specified in the study protocol to only calculate an arithmetic mean with no measure of dispersion using Phoenix WinNonlin Non-compartmental analysis.
|
—
|
|
Ratios of Drug Exposure for Ceftibuten
Ratio for BAL 2 for ceftibuten
|
0.222 Ratio
Standard Deviation NA
It was pre-specified in the study protocol to only calculate an arithmetic mean with no measure of dispersion using Phoenix WinNonlin Non-compartmental analysis.
|
—
|
SECONDARY outcome
Timeframe: Up to Day 8Population: Safety Set: participants who received at least one dose of study drug.
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.
Outcome measures
| Measure |
Group 1: Ceftibuten and Ledaborbactam Etzadroxil
n=28 Participants
Participants received a total of five oral doses of ceftibuten ledaborbactam etzadroxil (600 mg ceftibuten/600 mg ledaborbactam etzadroxil) every 12 hours.
|
Group 2: Ceftibuten
n=6 Participants
Participants received a total of five doses of 600 mg oral ceftibuten alone every 12 hours.
|
|---|---|---|
|
Number of Participants Reporting Treatment-emergent Adverse Events (TEAEs) After Administration of Ceftibuten and Ledaborbactam Etzadroxil
Any serious TEAE
|
0 Participants
|
0 Participants
|
|
Number of Participants Reporting Treatment-emergent Adverse Events (TEAEs) After Administration of Ceftibuten and Ledaborbactam Etzadroxil
Any non-serious TEAE leading to early termination
|
1 Participants
|
0 Participants
|
|
Number of Participants Reporting Treatment-emergent Adverse Events (TEAEs) After Administration of Ceftibuten and Ledaborbactam Etzadroxil
Any non-serious TEAE
|
2 Participants
|
0 Participants
|
|
Number of Participants Reporting Treatment-emergent Adverse Events (TEAEs) After Administration of Ceftibuten and Ledaborbactam Etzadroxil
Not any TEAE
|
25 Participants
|
6 Participants
|
Adverse Events
Group 1: Ceftibuten and Ledaborbactam Etzadroxil
Group 2: Ceftibuten
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
Group 1: Ceftibuten and Ledaborbactam Etzadroxil
n=28 participants at risk
Participants received a total of five oral doses of ceftibuten ledaborbactam etzadroxil (600 mg ceftibuten/600 mg ledaborbactam etzadroxil) every 12 hours.
|
Group 2: Ceftibuten
n=6 participants at risk
Participants received a total of five doses of 600 mg oral ceftibuten alone every 12 hours.
|
|---|---|---|
|
Gastrointestinal disorders
Dyspepsia
|
3.6%
1/28 • 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.
|
0.00%
0/6 • 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.
|
|
Nervous system disorders
Headache
|
3.6%
1/28 • 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.
|
0.00%
0/6 • 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.
|
|
Psychiatric disorders
Anxiety
|
3.6%
1/28 • 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.
|
0.00%
0/6 • 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.
|
Additional Information
Kamal Hamed, MD
Basilea Pharmaceutica International Ltd, Allschwil
Results disclosure agreements
- Principal investigator is a sponsor employee
- Publication restrictions are in place
Restriction type: GT60