Pharmacokinetics and Safety of Moxifloxacin (MFX468)
Primary Purpose
Tuberculosis
Status
Terminated
Phase
Phase 4
Locations
Netherlands
Study Type
Interventional
Intervention
Moxifloxacin
Sponsored by
About this trial
This is an interventional treatment trial for Tuberculosis focused on measuring Tuberculosis, Moxifloxacin, Pharmacokinetics, Safety
Eligibility Criteria
Inclusion Criteria:
- Patients with TB, with Mycobacterium tuberculosis (or M. africanum) by culture
- Starting treatment with MFX in a dose of 400 mg as part of their TB treatment
Exclusion Criteria:
- Contra-indication for MFX
- Baseline QTc-interval > 450 msec
- History of resuscitation
- History of ventricular tachycardia (including Torsades de Pointes)
- Family history of sudden cardiac death or Torsades de Pointes
- Additional risk factors for Torsades de Pointes (including known heart failure, Left ventricular hypertrophy)
- Use of concomitant treatment with QT/QTc prolonging drugs (including anti-dysrhythmics class IA and III, antipsychotics, tricyclic antidepressants or the antihistaminic drug terfenadine)
- Abnormal electrolytes (K, Mg, Na, Ca)
- Abnormal cardiac repolarisation on screening/baseline ECG
- History of adverse events to fluoroquinolones
- HIV co-infection
- RIF treatment during last 3 weeks before start of the study. After a washout period of 3 weeks the patient can be included.
Sites / Locations
- University Medical Center Groningen
Arms of the Study
Arm 1
Arm Type
Experimental
Arm Label
Moxifloxacin
Arm Description
Moxifloxacinin escalating dose
Outcomes
Primary Outcome Measures
Bound area under the plasma concentration-time curve (AUC0-24h) relative to the minimal inhibitory concentration (MIC)
% of patients who will reach an AUC0-24h/MIC ratio of at least 100 after administration of 400 mg (i.e. 7 days post dosage) moxifloxacin
Unbound AUC0-24h/MIC ratio as predictive parameter for efficacy of unbound MFX dose escalated treatment of tuberculosis
% of patients who will reach an unbound AUC0-24h/MIC ratio of at least 60 after administration of 400 mg (i.e. 7 day post dosage) moxifloxacin.
Bound AUC0-24h/Mutant Prevention Concentration (MPC) ratio
% of patients who will reach an adequate AUC0-24h/MPC ratio of at least 93 after administration of 400 mg (i.e. 7 days post dosage) moxifloxacin
Unbound AUC0-24h/MPC ratio as predictive parameter for efficacy of unbound MFX dose escalated treatment of tuberculosis and suppression of MFX resistance
% of patients who will reach an unbound AUC0-24h/MPC ratio of at least 53 after administration of 400 mg (i.e. 7 days post dosage) moxifloxacin
% of patients having adverse effects, including QT interval prolongation, hypersensitive reactions, diarrhoea, vomiting and hepatic or renal injury
QT interval in msec
Percentage of patients developing hepatic toxicity grade ≥ 2 or 3 Common Toxicity Criteria (CTC)
Percentage of patients developing renal toxicity grade ≥ 2 CTC
Bound area under the plasma concentration-time curve (AUC0-24h) relative to the minimal inhibitory concentration (MIC)
% of patients who will reach an AUC0-24h/MIC ratio of at least 100 after administration of 600 mg (i.e. 14 days post dosage) moxifloxacin
Bound area under the plasma concentration-time curve (AUC0-24h) relative to the minimal inhibitory concentration (MIC)
% of patients who will reach an AUC0-24h/MIC ratio of at least 100 after administration of 800 mg (i.e. 21 days post dosage) moxifloxacin
Unbound AUC0-24h/MIC ratio as predictive parameter for efficacy of unbound MFX dose escalated treatment of tuberculosis
% of patients who will reach an unbound AUC0-24h/MIC ratio of at least 60 after administration of 600 mg (i.e. 14 days post dosage) moxifloxacin.
Unbound AUC0-24h/MIC ratio as predictive parameter for efficacy of unbound MFX dose escalated treatment of tuberculosis
% of patients who will reach an unbound AUC0-24h/MIC ratio of at least 60 after administration of 800 mg (21 days post dosage) moxifloxacin.
Bound AUC0-24h/Mutant Prevention Concentration (MPC) ratio
% of patients who will reach an adequate AUC0-24h/MPC ratio of at least 93 after administration of 600 mg (i.e. 14 days post dosage) moxifloxacin
Bound AUC0-24h/Mutant Prevention Concentration (MPC) ratio
% of patients who will reach an adequate AUC0-24h/MPC ratio of at least 93 after administration of 800 mg (i.e. 21 days post dosage) moxifloxacin
Unbound AUC0-24h/MPC ratio as predictive parameter for efficacy of unbound MFX dose escalated treatment of tuberculosis and suppression of MFX resistance
% of patients who will reach an unbound AUC0-24h/MPC ratio of at least 53 after administration of 600 mg (i.e. 14 days post dosage) and moxifloxacin
Unbound AUC0-24h/MPC ratio as predictive parameter for efficacy of unbound MFX dose escalated treatment of tuberculosis and suppression of MFX resistance
% of patients who will reach an unbound AUC0-24h/MPC ratio of at least 53 after administration of 800 mg (i.e. 21 days post dosage) moxifloxacin
Secondary Outcome Measures
Evaluation of the predictive performance of the limited sampling strategies based on a pharmacokinetic population model to calculate AUC0-24h. Several limited sampling points will be evaluated.
Several limited sampling strategies to predict moxifloxacin AUC0-24h, based on limited sampling points, will be evaluated after administration of 400 mg (i.e. 7 days post dosage)moxifloxacin
Correlation between MFX concentration (mg/L) and QT interval (msec)
Correlation between MFX concentration (mg/L) and QT interval (msec) after administration of 400 mg (i.e. 7 days post dosage) moxifloxacin
Correlation of drug exposure (AUC) and adverse effects
vomiting and diarrhoea
QT interval (msec)
Correlation between the genetic risk score and MFX induced QT prolongation
Evaluation of the predictive performance of the limited sampling strategies based on a pharmacokinetic population model to calculate AUC0-24h. Several limited sampling points will be evaluated.
Several limited sampling strategies to predict moxifloxacin AUC0-24h, based on limited sampling points, will be evaluated after administration of 600 mg (i.e. 14 days post dosage) moxifloxacin
Evaluation of the predictive performance of the limited sampling strategies based on a pharmacokinetic population model to calculate AUC0-24h. Several limited sampling points will be evaluated.
Several limited sampling strategies to predict moxifloxacin AUC0-24h, based on limited sampling points, will be evaluated after administration of 800 mg (i.e. 21 days post dosage) moxifloxacin
Correlation between MFX concentration (mg/L) and QT interval (msec)
Correlation between MFX concentration (mg/L) and QT interval (msec) after administration of 600 mg (i.e. 14 days post dosage) moxifloxacin
Correlation between MFX concentration (mg/L) and QT interval (msec)
Correlation between MFX concentration (mg/L) and QT interval (msec) after administration of 800 mg (i.e. 21 days post dosage) moxifloxacin
Full Information
NCT ID
NCT01329250
First Posted
March 8, 2011
Last Updated
November 17, 2016
Sponsor
University Medical Center Groningen
1. Study Identification
Unique Protocol Identification Number
NCT01329250
Brief Title
Pharmacokinetics and Safety of Moxifloxacin
Acronym
MFX468
Official Title
Pharmacokinetics and Safety of Moxifloxacin; a Dose Escalation in Patients With Tuberculosis
Study Type
Interventional
2. Study Status
Record Verification Date
November 2016
Overall Recruitment Status
Terminated
Why Stopped
slow enrolment of patients and new insights
Study Start Date
May 2011 (undefined)
Primary Completion Date
June 2015 (Actual)
Study Completion Date
August 2016 (Actual)
3. Sponsor/Collaborators
Responsible Party, by Official Title
Principal Investigator
Name of the Sponsor
University Medical Center Groningen
4. Oversight
Data Monitoring Committee
Yes
5. Study Description
Brief Summary
The main objective of this prospective clinical trial is to compare pharmacokinetics and safety and tolerability of a standard dose (400 mg) with an escalated dose (600 mg; 800 mg) of moxifloxacin (MFX). This clinical trial will provide important safety information on MFX in a higher dosage in TB patients.
Detailed Description
Moxifloxacin (MFX) is a fluoroquinolone with a high in vitro and in vivo bactericidal activity against Mycobacterium tuberculosis. A daily dose of 600-800 mg MFX should be considered for optimal killing of the involved mycobacteria and suppression of drug resistance, which is higher than the currently used dose of 400 mg once daily. In general, safety data to support switching to the suggested higher dose are limited.
For this purpose, twenty tuberculosis patients will start on a standard dose of MFX 400 mg once daily. After 8 days the dose will be increased to 600 mg once daily and on the 15th day of treatment, the dose of MFX will be escalated to 800 mg. In patients who have been treated with rifampicin (RIF) in the past three weeks prior to start of MFX treatment an additional washout period of 3 weeks to reduce the rifampicin induced enzymatic activity will precede the dose escalation.
6. Conditions and Keywords
Primary Disease or Condition Being Studied in the Trial, or the Focus of the Study
Tuberculosis
Keywords
Tuberculosis, Moxifloxacin, Pharmacokinetics, Safety
7. Study Design
Primary Purpose
Treatment
Study Phase
Phase 4
Interventional Study Model
Single Group Assignment
Masking
None (Open Label)
Allocation
Non-Randomized
Enrollment
9 (Actual)
8. Arms, Groups, and Interventions
Arm Title
Moxifloxacin
Arm Type
Experimental
Arm Description
Moxifloxacinin escalating dose
Intervention Type
Drug
Intervention Name(s)
Moxifloxacin
Other Intervention Name(s)
MFX
Intervention Description
Patients will start on a standard dose of MFX 400 mg once daily. After 8 days the dose will be increased to 600 mg once daily and on the 15th day of treatment, the dose of MFX will be escalated to 800 mg. In patients who have been treated with rifampicin (RIF) in the past three weeks prior to start of MFX treatment an additional washout period of 3 weeks to reduce the rifampicin induced enzymatic activity will precede the dose escalation.
Primary Outcome Measure Information:
Title
Bound area under the plasma concentration-time curve (AUC0-24h) relative to the minimal inhibitory concentration (MIC)
Description
% of patients who will reach an AUC0-24h/MIC ratio of at least 100 after administration of 400 mg (i.e. 7 days post dosage) moxifloxacin
Time Frame
7 days post dosage
Title
Unbound AUC0-24h/MIC ratio as predictive parameter for efficacy of unbound MFX dose escalated treatment of tuberculosis
Description
% of patients who will reach an unbound AUC0-24h/MIC ratio of at least 60 after administration of 400 mg (i.e. 7 day post dosage) moxifloxacin.
Time Frame
7 days post dosage
Title
Bound AUC0-24h/Mutant Prevention Concentration (MPC) ratio
Description
% of patients who will reach an adequate AUC0-24h/MPC ratio of at least 93 after administration of 400 mg (i.e. 7 days post dosage) moxifloxacin
Time Frame
7 days post dosage
Title
Unbound AUC0-24h/MPC ratio as predictive parameter for efficacy of unbound MFX dose escalated treatment of tuberculosis and suppression of MFX resistance
Description
% of patients who will reach an unbound AUC0-24h/MPC ratio of at least 53 after administration of 400 mg (i.e. 7 days post dosage) moxifloxacin
Time Frame
7 days post dosage
Title
% of patients having adverse effects, including QT interval prolongation, hypersensitive reactions, diarrhoea, vomiting and hepatic or renal injury
Description
QT interval in msec
Percentage of patients developing hepatic toxicity grade ≥ 2 or 3 Common Toxicity Criteria (CTC)
Percentage of patients developing renal toxicity grade ≥ 2 CTC
Time Frame
up to 21 days
Title
Bound area under the plasma concentration-time curve (AUC0-24h) relative to the minimal inhibitory concentration (MIC)
Description
% of patients who will reach an AUC0-24h/MIC ratio of at least 100 after administration of 600 mg (i.e. 14 days post dosage) moxifloxacin
Time Frame
14 days post dosage
Title
Bound area under the plasma concentration-time curve (AUC0-24h) relative to the minimal inhibitory concentration (MIC)
Description
% of patients who will reach an AUC0-24h/MIC ratio of at least 100 after administration of 800 mg (i.e. 21 days post dosage) moxifloxacin
Time Frame
21 days post dosage
Title
Unbound AUC0-24h/MIC ratio as predictive parameter for efficacy of unbound MFX dose escalated treatment of tuberculosis
Description
% of patients who will reach an unbound AUC0-24h/MIC ratio of at least 60 after administration of 600 mg (i.e. 14 days post dosage) moxifloxacin.
Time Frame
14 days post dosage
Title
Unbound AUC0-24h/MIC ratio as predictive parameter for efficacy of unbound MFX dose escalated treatment of tuberculosis
Description
% of patients who will reach an unbound AUC0-24h/MIC ratio of at least 60 after administration of 800 mg (21 days post dosage) moxifloxacin.
Time Frame
21 days post dosage
Title
Bound AUC0-24h/Mutant Prevention Concentration (MPC) ratio
Description
% of patients who will reach an adequate AUC0-24h/MPC ratio of at least 93 after administration of 600 mg (i.e. 14 days post dosage) moxifloxacin
Time Frame
14 post dosage
Title
Bound AUC0-24h/Mutant Prevention Concentration (MPC) ratio
Description
% of patients who will reach an adequate AUC0-24h/MPC ratio of at least 93 after administration of 800 mg (i.e. 21 days post dosage) moxifloxacin
Time Frame
21 post dosage
Title
Unbound AUC0-24h/MPC ratio as predictive parameter for efficacy of unbound MFX dose escalated treatment of tuberculosis and suppression of MFX resistance
Description
% of patients who will reach an unbound AUC0-24h/MPC ratio of at least 53 after administration of 600 mg (i.e. 14 days post dosage) and moxifloxacin
Time Frame
14 days post dosage
Title
Unbound AUC0-24h/MPC ratio as predictive parameter for efficacy of unbound MFX dose escalated treatment of tuberculosis and suppression of MFX resistance
Description
% of patients who will reach an unbound AUC0-24h/MPC ratio of at least 53 after administration of 800 mg (i.e. 21 days post dosage) moxifloxacin
Time Frame
21 days post dosage
Secondary Outcome Measure Information:
Title
Evaluation of the predictive performance of the limited sampling strategies based on a pharmacokinetic population model to calculate AUC0-24h. Several limited sampling points will be evaluated.
Description
Several limited sampling strategies to predict moxifloxacin AUC0-24h, based on limited sampling points, will be evaluated after administration of 400 mg (i.e. 7 days post dosage)moxifloxacin
Time Frame
7 days post dosage
Title
Correlation between MFX concentration (mg/L) and QT interval (msec)
Description
Correlation between MFX concentration (mg/L) and QT interval (msec) after administration of 400 mg (i.e. 7 days post dosage) moxifloxacin
Time Frame
7 days post dosage
Title
Correlation of drug exposure (AUC) and adverse effects
Description
vomiting and diarrhoea
QT interval (msec)
Time Frame
up to 21 days
Title
Correlation between the genetic risk score and MFX induced QT prolongation
Time Frame
up to 21 days
Title
Evaluation of the predictive performance of the limited sampling strategies based on a pharmacokinetic population model to calculate AUC0-24h. Several limited sampling points will be evaluated.
Description
Several limited sampling strategies to predict moxifloxacin AUC0-24h, based on limited sampling points, will be evaluated after administration of 600 mg (i.e. 14 days post dosage) moxifloxacin
Time Frame
14 days post dosage
Title
Evaluation of the predictive performance of the limited sampling strategies based on a pharmacokinetic population model to calculate AUC0-24h. Several limited sampling points will be evaluated.
Description
Several limited sampling strategies to predict moxifloxacin AUC0-24h, based on limited sampling points, will be evaluated after administration of 800 mg (i.e. 21 days post dosage) moxifloxacin
Time Frame
21 days post dosage
Title
Correlation between MFX concentration (mg/L) and QT interval (msec)
Description
Correlation between MFX concentration (mg/L) and QT interval (msec) after administration of 600 mg (i.e. 14 days post dosage) moxifloxacin
Time Frame
14 days post dosage
Title
Correlation between MFX concentration (mg/L) and QT interval (msec)
Description
Correlation between MFX concentration (mg/L) and QT interval (msec) after administration of 800 mg (i.e. 21 days post dosage) moxifloxacin
Time Frame
21 days post dosage
10. Eligibility
Sex
All
Minimum Age & Unit of Time
18 Years
Accepts Healthy Volunteers
No
Eligibility Criteria
Inclusion Criteria:
Patients with TB, with Mycobacterium tuberculosis (or M. africanum) by culture
Starting treatment with MFX in a dose of 400 mg as part of their TB treatment
Exclusion Criteria:
Contra-indication for MFX
Baseline QTc-interval > 450 msec
History of resuscitation
History of ventricular tachycardia (including Torsades de Pointes)
Family history of sudden cardiac death or Torsades de Pointes
Additional risk factors for Torsades de Pointes (including known heart failure, Left ventricular hypertrophy)
Use of concomitant treatment with QT/QTc prolonging drugs (including anti-dysrhythmics class IA and III, antipsychotics, tricyclic antidepressants or the antihistaminic drug terfenadine)
Abnormal electrolytes (K, Mg, Na, Ca)
Abnormal cardiac repolarisation on screening/baseline ECG
History of adverse events to fluoroquinolones
HIV co-infection
RIF treatment during last 3 weeks before start of the study. After a washout period of 3 weeks the patient can be included.
Overall Study Officials:
First Name & Middle Initial & Last Name & Degree
Jos GW Kosterink, PharmD, PhD
Organizational Affiliation
Univeristy Medical Center Groningen
Official's Role
Study Chair
First Name & Middle Initial & Last Name & Degree
Jan-Willem C Alffenaar, PharmD, PhD
Organizational Affiliation
University Medical Center Groningen
Official's Role
Principal Investigator
Facility Information:
Facility Name
University Medical Center Groningen
City
Groningen
Country
Netherlands
12. IPD Sharing Statement
Learn more about this trial
Pharmacokinetics and Safety of Moxifloxacin
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