P1, DDI & MAD PK and Safety Study of Xeruborbactam Oral Prodrug in Combo With Ceftibuten in Healthy Participants

NCT06079775 | Completed Phase 1 DMC FDA Drug

• 1 other identifier: Qpex-102
• Study Type: interventional
• Target: 53
• Locations: 1 country
• Sites: 1

Brief Summary

A Phase 1, Open-Label, Drug-drug Interaction, and Randomized, Double-blind, Controlled, Multiple-dose Pharmacokinetics and Safety Study of Xeruborbactam Oral Prodrug (QPX7831) in Combination with Ceftibuten in Healthy Adult Participants

Conditions

Bacterial Infections

Keywords

beta-lactamase inhibitor

Outcome Measures

Primary Outcomes (7)

• Incidence of Treatment -Emergent Adverse events by subject and by cohort (single dose, multiple doses)

  Number of patients with Treatment-Emergent Adverse Events by subject, by cohort, severity and relationship to treatment

  16 days

• Number of patients with changes from baseline in safety parameters

  Number of patients with changes in safety parameters before and after dosing by subject and cohort

  16 days

• Peak plasma Concentration measurements by subject and by cohort (Cmax)

  Comparison will be performed between the cohorts for concentration measurements (Cmax). Mean graphical presentation of the data will be reported. Statistical analysis of exposure parameters will be performed.

  16 days

• Time concentration data measurements by subject and by cohort (Tmax)

  Comparison will be performed between the cohorts for time concentration data measurements (Tmax)

  16 days

• Area under the plasma concentration versus time curve (AUC) between cohorts

  Comparison will be performed between the cohorts for area under the plasma concentration versus time curve (AUC). Mean graphical presentation of the data will be reported. Statistical analysis of exposure parameters will be performed.

  16 days

• Urine Pharmacokinetic (PK) amount excreted by subject and by cohort

  Urine Pharmacokinetic (PK) parameters such as amount excreted will be calculated from urinary excretion data

  16 days

• Urine Pharmacokinetic (PK) % dose excreted by subject and by cohort

  Urine Pharmacokinetic (PK) parameters such as amount of % dose excreted will be calculated from urinary excretion data

  16 days

Study Arms (2)

Single Dose Drug-Drug-Interaction Crossover & Multiple Dose Cohorts

EXPERIMENTAL

DDI crossover part of the study, subjects will be enrolled into 3 cohorts of 8 subjects each, Cohorts 1, 2, \& 3 respectively. All subjects in Cohorts 1, 2, and 3 will receive a single dose of xeruborbactam oral prodrug (XOP) on Day 1. On Day 6, they will receive a single dose of ceftibuten. On Day 9 they will receive a single combined dose of XOP and ceftibuten. During the MAD part of the study, subjects will be enrolled into 2 cohorts, Cohorts 4 \& 5 respectively. Subjects in Cohorts 4 (16 subjects) will receive either a combined dose of XOP and ceftibuten, active ceftibuten, or active XOP. Cohort 4 will be dosed BID on Days 1-9, with last dose on the morning of Day 10. Subjects in Cohort 5 (15 subjects) will receive active XOP in comb with active ceftibuten which will be admin orally either twice on Day 1 and QD on Days 2-10 (Group 1), BID on Days 1-9 and QD on Day 10 (Group 2), or TID on Days 1-9 and once on Day 10 (Group 3), based on group assignment.

Drug: Xeruborbactam Oral Prodrug; Drug: Ceftibuten

Placebo Comparator to maintain the blind

PLACEBO COMPARATOR

During Cohort 4, Xeruborbactam Oral Prodrug Placebo and Ceftibuten placebo will be used to maintain the blind. In Cohort 4, ten (10) subjects in each cohort will receive a combined dose of xeruborbactam oral prodrug and ceftibuten. Three (3) subjects in each cohort will receive active ceftibuten capsules with xeruborbactam oral prodrug placebo capsules. Three (3) subjects in each cohort will receive active xeruborbactam oral prodrug capsules with ceftibuten placebo capsules.

Drug: Xeruborbactam Oral Prodrug Placebo; Drug: Ceftibuten Placebo

Interventions

Xeruborbactam Oral Prodrug DRUG

Experimental

Also known as: QPX7831

Single Dose Drug-Drug-Interaction Crossover & Multiple Dose Cohorts

Ceftibuten DRUG

Experimental

Single Dose Drug-Drug-Interaction Crossover & Multiple Dose Cohorts

Xeruborbactam Oral Prodrug Placebo DRUG

Placebo Comparator

Also known as: QPX7831 Placebo

Placebo Comparator to maintain the blind

Ceftibuten Placebo DRUG

Placebo Comparator

Placebo Comparator to maintain the blind

Eligibility Criteria

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

You may qualify if:

• Participants will be eligible to be included in the study only if all of the following criteria apply:
• Age
• Participant must be a healthy adult male or female, 18 to 55 years of age (inclusive) at the time of screening.
• Type of Participant and Disease Characteristics
• Participants who are overtly medically healthy with clinically insignificant screening results (eg, laboratory profiles, medical histories, ECGs, physical examination) as assessed by the investigator, sub-investigator, or medical officer.
• Weight
• Body mass index (BMI) ≥ 18.5 and ≤ 29.9 (kg/m2) and weight between 55.0 and 100.0 kg (inclusive). Note: BMI = kg/m2 where kg is a weight in kilograms and m2 is a height in meters squared.
• Sex and Contraceptive/Barrier Requirements
• Contraceptive use by men and women should be consistent with local regulations regarding the methods of contraception for those participating in clinical studies.
• Male participants:
• Female participants:
• Females of childbearing potential must either be sexually abstinent for 14 days prior to Day 1 and agree to remain so through 30 days following the last administration of the study drug, OR have been using (or agree to use) 2 of the following acceptable methods of birth control for the times specified:
• Intra-uterine device (IUD) in place for at least 3 months prior to Day 1 through 30 days following the final dosing of the study drug
• Barrier method (condom or diaphragm) for at least 14 days prior to Day 1 through 30 days following the final dosing of the study drug
• Stable hormonal contraceptive for at least 3 months prior to Day 1 and barrier method (condom or diaphragm) for at least 14 days prior to Day 1 through 30 days following final dosing of the study drug

You may not qualify if:

• Participants will be excluded from the study if any of the following criteria apply:
• Medical Conditions
• History or presence of significant cardiovascular, pulmonary, hepatic, renal, hematological, gastrointestinal, endocrine, immunologic, dermatologic, neurological, or psychiatric disease.
• Documented hypersensitivity reaction or anaphylaxis to any medication, including ceftibuten or other beta-lactam antibiotics (e.g. cephalosporins, penicillins, carbapenems or monobactams) or any excipients used in this formulation.
• Positive testing for human immunodeficiency virus (HIV), hepatitis B surface antigen (HBsAg), or hepatitis C virus (HCV).
• Females who are pregnant or lactating.
• Surgery within the past 3 months prior to Day 1 determined by the investigator, sub-investigator, or medical officer to be clinically relevant.
• Any acute illness within 30 days prior to Day 1.
• Any other condition or prior therapy, which, in the opinion of the investigator, sub-investigator, or medical officer would make the participant unsuitable for this study.
• Prior/Concomitant Therapy
• Use of any prescription medication (with the exception of hormonal contraceptives or hormone replacement therapy for females) within 14 days prior to Day 1.
• Use of any over-the-counter medication, including herbal products, probiotics and vitamins, within the 7 days prior to Day 1. Up to 2 grams per day of paracetamol is allowed for acute events at the discretion of the investigator, sub-investigator, or medical officer.
• Use of antacids, H2 receptor blockers or proton pump inhibitors 7 days prior to Day 1. This includes calcium carbonate.
• Prior/Concurrent Clinical Study Experience
• Participation in another investigational clinical trial within 30 days prior to Day 1 or within 5 half-lives of the previous investigational drug, whichever is longer.

Sponsors & Collaborators

• Qpex Biopharma, Inc.: lead
• Shionogi Inc.: collaborator
• Biomedical Advanced Research and Development Authority: collaborator

Study Sites (1)

CMAX

Adelaide, South Australia, 5000, Australia

Location

MeSH Terms

Conditions

Bacterial Infections

Interventions

Ceftibuten

Condition Hierarchy (Ancestors)

Bacterial Infections and Mycoses; Infections

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

• Jeff Loutit, MBChB

  Qpex Biopharma, Inc.

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: QUADRUPLE
• Who Masked: PARTICIPANT, CARE PROVIDER, INVESTIGATOR, OUTCOMES ASSESSOR
• Masking Details: matched oral placebo capsules
• Purpose: TREATMENT
• Intervention Model: SEQUENTIAL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Model Details: Randomized, Double-Blind, Controlled, Crossover, ascending single-and multipledose design

Study Record Dates

• First Submitted: October 6, 2023
• First Posted: October 12, 2023
• Study Start: January 30, 2024
• Primary Completion: January 5, 2025
• Study Completion: January 5, 2025
• Last Updated: December 12, 2025

Record last verified: 2025-06

Data Sharing

• IPD Sharing: Will not share

Locations

AU (1)