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

NCT06665555 | Completed Phase 1 FDA Drug

• 1 other identifier: VNRX-7145-105
• Study Type: interventional
• Target: 34
• Locations: 1 country
• Sites: 1

Brief Summary

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.

Conditions

Pharmacokinetics; Healthy Volunteers

Outcome Measures

Primary Outcomes (7)

• 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 Outcomes (2)

• 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

Study Arms (2)

Group 1

EXPERIMENTAL

Participants in Group 1 will undergo one standardized bronchoscopy with bronchoalveolar lavage after the fifth dose of ceftibuten-ledaborbactam etzadroxil.

Drug: ledaborbactam etzadroxil; Drug: ceftibuten

Group 2

EXPERIMENTAL

Participants in Group 2 will undergo one standardized bronchoscopy with bronchoalveolar lavage after the fifth of dose of ceftibuten alone.

Drug: ceftibuten

Interventions

ledaborbactam etzadroxil DRUG

Five doses of ledaborbactam etzadroxil will be administered orally every 12 hours

Group 1

ceftibuten DRUG

Five doses of ceftibuten will be administered orally every 12 hours

Group 1; Group 2

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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

You may not qualify if:

• 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

Sponsors & Collaborators

• Basilea Pharmaceutica: lead
• National Institute of Allergy and Infectious Diseases (NIAID): collaborator

Study Sites (1)

Pulmonary Associates

Phoenix, Arizona, 85032, United States

Location

MeSH Terms

Interventions

Ceftibuten

Intervention Hierarchy (Ancestors)

Cephalosporins; beta-Lactams; Lactams; Amides; Organic Chemicals; Thiazines; Sulfur Compounds; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring; Heterocyclic Compounds

Study Officials

• Kamal Hamed, MD

  Basilea Pharmaceutica International Ltd, Allschwil

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: October 29, 2024
• First Posted: October 30, 2024
• Study Start: November 4, 2024
• Primary Completion: March 13, 2025
• Study Completion: March 17, 2025
• Last Updated: January 23, 2026

Record last verified: 2026-01

Locations

US (1)