Safety and PK of Ceftibuten-ledaborbactam Etzadroxil Fixed-dose Combination

NCT06733675 | Recruiting Phase 1 FDA Drug

• 1 other identifier: VNRX-7145-106
• Study Type: interventional
• Target: 96
• Locations: 1 country
• Sites: 1

Brief Summary

This is a Phase 1, open-label, three-part, study in approximately 96 healthy adult participants between 18 and 55 years of age (both inclusive) (16 participants in Part 1, 20 participants in Part 2 and , and approximately 60 participants in Part 3). The study will be conducted at one clinical site in the United States. Participants in Part 1 and Part 2 may be conducted in parallel. The duration of an individual participation will be approximately 46 days for Part 1 , 43 days for Part 2 and 83 days for Part 3. All participants in Parts I und 2 will be screened within 28 days prior to dosing. All participants in Part 3 will be screened within 33 days prior to dosing. They will be admitted to the clinical research unit (CRU) the day prior to dosing and will remain in the CRU until the end of the PK sample collection period. All participants will return to the clinic for follow-up assessments 7 days ± 1 day after the last dose of study intervention. Participants in Part 3 will also return to the clinic for follow-up assessments 28 days ± 2 days and 42 days ± 2 days after the last dose of study intervention.

Conditions

Healthy Volunteer; Safety; Pharmacokinetics; FDC; Drug-Drug Interaction (DDI)

Keywords

Healthy Volunteers; Ceftibuten; Ledaborbactam etzadroxil

Outcome Measures

Primary Outcomes (4)

• Part 1 Plasma PK AUC0-∞ (ceftibuten, ledaborbactam, and ledaborbactam etzadroxil)

  Area under the concentration time curve from time zero to infinity (AUC0-∞)

  0 - 48 hours on days 1, 4 and 11

• Part 1 Plasma PK Cmax (ceftibuten, ledaborbactam, and ledaborbactam etzadroxil)

  Maximum observed concentration (Cmax)

  0 - 48 hours on days 1, 4 and 11

• Proportion of participants of Part 2 experiencing Treatment-emergent adverse events (TEAEs), Serious TEAEs, or TEAEs leading to discontinuation.

  Participants experiencing Treatment-emergent adverse events (TEAEs), Serious TEAEs, or TEAEs leading to discontinuation.

  Day 1 thru Day 18 (+/-1)

• Proportion of participants of Part 3 experiencing Treatment-emergent adverse events (TEAEs), Serious TEAEs, or TEAEs leading to discontinuation.

  Participants experiencing Treatment-emergent adverse events (TEAEs), Serious TEAEs, or TEAEs leading to discontinuation.

  Day 1 thru Day 49 (± 2 days)

Secondary Outcomes (5)

• Proportion of participants of Part 1 experiencing Treatment-emergent adverse events (TEAEs), Serious TEAEs, or TEAEs leading to discontinuation.

  Day 1 thru Day 18 (+/-1)

• Part 2 Plasma PK AUC0-12h (ceftibuten, ledaborbactam, and ledaborbactam etzadroxil)

  Day 1 and Day 7

• Part 2 Plasma PK Cmax (ceftibuten, ledaborbactam, and ledaborbactam etzadroxil)

  Day 1 and Day 7

• Part 3 Plasma PK AUC0-Tau (ceftibuten and/or ledaborbactam)

  At Day 1 and Day 7

• Part 3 Plasma PK Cmax (ceftibuten and/or ledaborbactam)

  At Day 1 and Day 7

Study Arms (5)

Part 1

EXPERIMENTAL

Part 1 will enroll at least 16 participants who will receive a single oral dose of ceftibuten and ledaborbactam etzadroxil following a 10-hour fast on 3 occasions in a fixed sequence: (a) Ceftibuten and ledaborbactam etzadroxil as separate capsules; (b) Ceftibuten-ledaborbactam etzadroxil as fixed-dose combination (FDC) capsules; (c) Ceftibuten-ledaborbactam etzadroxil as FDC capsules after 5 days of esomeprazole orally once daily

Drug: Ledaborbactam etzadroxil; Drug: Ceftibuten; Drug: Ceftibuten-ledaborbactam etzadroxil; Drug: Esomeprazole

Part 2 Group 1

EXPERIMENTAL

Part 2 Group 1 will enroll 10 participants. Each will receive oral doses of Ceftibuten-ledaborbactam etzadroxil FDC capsules for 7 days (Fasted Group)

Drug: Ceftibuten-ledaborbactam etzadroxil

Part 2 Group 2

EXPERIMENTAL

Part 2 Group 2 will enroll 10 participants. Each will receive oral doses of Ceftibuten-ledaborbactam etzadroxil FDC capsules for 7 days (Fed Group)

Drug: Ceftibuten-ledaborbactam etzadroxil

Part 3 (Groups 1, 2, 4, 5, 6)

EXPERIMENTAL

Part 3 will enroll up to 50 participants. Each will receive oral doses of ceftibuten and/or ledaborbactam etzadroxil capsules (combined as FDC when administered together) in fed conditions

Drug: Ledaborbactam etzadroxil; Drug: Ceftibuten

Part 3 Group 3

ACTIVE COMPARATOR

Part 3 Group 3 will enroll up to 10 participants. Each will receive oral doses of amoxicillin-clavulanate

Drug: amoxicillin-clavulanate

Interventions

Ceftibuten DRUG

capsules

Part 1; Part 3 (Groups 1, 2, 4, 5, 6)

Ceftibuten-ledaborbactam etzadroxil DRUG

Fixed Dose Combination (FDC)

Part 1; Part 2 Group 1; Part 2 Group 2

Ledaborbactam etzadroxil DRUG

capsules

Part 1; Part 3 (Groups 1, 2, 4, 5, 6)

Esomeprazole DRUG

40 mg capsule

Part 1

amoxicillin-clavulanate DRUG

500 mg-125 mg oral doses

Part 3 Group 3

Eligibility Criteria

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

You may qualify if:

• Healthy adult male or female, between 18 and 55 years of age
• Body mass index ≥ 18 and ≤ 32 kg/m2
• Laboratory values meeting defined laboratory ranges
• Males or non-pregnant, non-lactating females

You may not qualify if:

• History of any hypersensitivity reaction following administration of a cephalosporin, penicillin, or other β-lactam antibacterial drug
• Any acute illness or surgery within the past 3 months determined by the investigator to be clinically relevant
• Positive alcohol, drug or tobacco use/test

Sponsors & Collaborators

• Basilea Pharmaceutica: lead
• Biomedical Advanced Research and Development Authority: collaborator

Study Sites (1)

ICON, Clinical Research Phase I Unit

Lenexa, Kansas, 66219, United States

RECRUITING

MeSH Terms

Interventions

Ceftibuten; Esomeprazole; Amoxicillin-Potassium Clavulanate Combination

Intervention Hierarchy (Ancestors)

Cephalosporins; beta-Lactams; Lactams; Amides; Organic Chemicals; Thiazines; Sulfur Compounds; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring; Heterocyclic Compounds; Omeprazole; 2-Pyridinylmethylsulfinylbenzimidazoles; Sulfoxides; Pyridines; Heterocyclic Compounds, 1-Ring; Benzimidazoles; Clavulanic Acid; Clavulanic Acids; Amoxicillin; Ampicillin; Penicillin G; Penicillins; Drug Combinations; Pharmaceutical Preparations

Study Officials

• Kamal Hamed, MD

  Basilea Pharmaceutica International Ltd, Allschwil

  STUDY DIRECTOR

Central Study Contacts

Karine Litherland, PhD

CONTACT

+41616061111; Karine.Litherland@basilea.com

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: December 10, 2024
• First Posted: December 13, 2024
• Study Start: January 7, 2025
• Primary Completion (Estimated): December 30, 2026
• Study Completion (Estimated): December 30, 2026
• Last Updated: July 9, 2026

Record last verified: 2026-07

Locations

US (1)