Evaluation of Penetration of Ceftobiprole Into Soft Tissue Determined by Microdialysis in Healthy Volunteers

An Exploratory Study to Evaluate the Penetration of Ceftobiprole Into Soft Tissue Determined by In Vivo Microdialysis in Healthy Volunteers

The primary objective of this study is to measure the penetration of ceftobiprole into subcutaneous (s.c.) adipose tissue and skeletal muscle and to determine the concentration over time of ceftobiprole in these tissues and in plasma after administration of a single intravenous (i.v.) infusion (directly into the vein) of ceftobiprole 500 mg administered over 2 hours. The secondary objective was to further assess the safety and tolerability of ceftobiprole after a single i.v. infusion.

Study Overview

• Status: Completed
• Conditions: Streptococcal Infections; Staphylococcal Skin Infections
• Intervention / Treatment: Drug: Ceftobiprole

Detailed Description

This is a single-center, open-label (all patients involved know the identity of the drug), single-arm, nonrandomized study of ceftobiprole in healthy men and women. The study is conducted in 2 parts: a pilot study and a main study. Each study (i.e. the pilot study and the main study) consists of 3 phases: a pretreatment phase that includes up to a 21-day screening period, an open-label treatment phase (1 day in the pilot study and 2 days in the main study), and a posttreatment phase that included the end of study evaluations and follow-up study visit or telephone contact planned for 1 to 2 weeks after discharge from the study unit. Serial blood and dialysis samples will be collected at specified time points from predose through 24 hours after the start of the infusion for estimation of ceftobiprole and ceftobiprole medocaril concentrations. Additional samples will be collected for measurement of protein binding. The study will include the following evaluations of safety and tolerability: adverse events, clinical laboratory tests (including hematology, serum chemistry, and urinalysis), electrocardiogram (ECG), vital signs, physical examination, serology, pregnancy tests, urine drug screen, and alcohol breath test. In the pilot study, Ceftobiprole will be locally administered via a microdialysis probe at a concentration of approximately 30 µg/mL for 60 minutes. In the main Study, each volunteer will receive ceftobiprole locally via the microdialysis probe. After the washout period determined by the pilot study, each volunteer will receive a single 2-hour i.v. infusion of ceftobiprole.

• Study Type: Interventional
• Enrollment (Actual): 15
• Phase: Phase 1

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 55 years (ADULT)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Body mass index (BMI between 18 to 29 kg/m2
• Nonsmoker
• Normal renal function

Exclusion Criteria:

• History of gastric or duodenal ulcer
• History of allergies or hypersensitivity (including penicillin, cephalosporins, or other ß-lactams or quinolones)
• Hypersensitivity or intolerance to heparin
• History of drug or alcohol abuse

Study Plan

How is the study designed?

Design Details

• Primary Purpose: BASIC_SCIENCE
• Allocation: NA
• Interventional Model: SINGLE_GROUP
• Masking: NONE

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
EXPERIMENTAL: 001; Ceftobiprole 500 mg, single infusion over 2 hours	Drug: Ceftobiprole; single intravenous (i.v.) infusion, 500 mg ceftobiprole administered over 2 hours.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
To measure the penetration of ceftobiprole into subcutaneous (s.c.) adipose tissue and skeletal muscle and to determine the concentration-versus-time profiles of ceftobiprole in these tissues and in plasma.	Day 1 pre- and post-dose during the pilot study and on Days 1 and 2 during the main study

Secondary Outcome Measures

Outcome Measure	Time Frame
To assess the safety and tolerability of ceftobiprole after a single intravenous (iv) infusion.	Approximately 5 weeks during the pilot study including screening, treatment, and posttreatment follow up and for approximately 5 weeks during the main study including screening, treatment, and posttreatment follow up

Collaborators and Investigators

• Sponsor: Basilea Pharmaceutica

Publications and helpful links

Helpful Links

• An Exploratory Study to Evaluate the Penetration of Ceftobiprole Into Soft Tissue Determined by In Vivo Microdialysis in Healthy Volunteers
• An Exploratory Study to Evaluate the Penetration of Ceftobiprole Into Soft Tissue Determined by In Vivo Microdialysis in Healthy Volunteers

Study record dates

Study Major Dates

• Study Start: June 1, 2007
• Primary Completion (ACTUAL): September 1, 2007
• Study Completion (ACTUAL): September 1, 2007

Study Registration Dates

• First Submitted: December 3, 2009
• First Submitted That Met QC Criteria: December 3, 2009
• First Posted (ESTIMATE): December 4, 2009

Study Record Updates

• Last Update Posted (ESTIMATE): July 30, 2012
• Last Update Submitted That Met QC Criteria: July 27, 2012
• Last Verified: July 1, 2012

More Information

Terms related to this study

• Keywords: Staphylococcal Skin Infections; Streptococcal Infections
• Additional Relevant MeSH Terms: Pathologic Processes; Skin Diseases; Inflammation; Disease Attributes; Connective Tissue Diseases; Bacterial Infections; Bacterial Infections and Mycoses; Gram-Positive Bacterial Infections; Staphylococcal Infections; Suppuration; Skin Diseases, Bacterial; Infections; Communicable Diseases; Cellulitis; Skin Diseases, Infectious; Staphylococcal Skin Infections; Streptococcal Infections; Anti-Infective Agents; Anti-Bacterial Agents; Ceftobiprole; Ceftobiprole medocaril
• Other Study ID Numbers: CR011416; CSI-1002 (OTHER: Basilea)