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A Study To Assess The Effect Of Linezolid On QTc Interval

Phase 1
Completed
Conditions
Bacterial Infections
Interventions
Registration Number
NCT00795145
Lead Sponsor
Pfizer
Brief Summary

The FDA has asked Pfizer to assess the risk of linezolid on QT interval (obtained from ECG readings) which could predispose patients to ventricular arrhythmias. This study is conducted to satisfy this requirement.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
49
Inclusion Criteria
  • Healthy male and female subjects between the ages of 21 and 55 years.
  • Body mass Index (BMI) of 18 to 30 kg/m2; and a total body weight > 45 kg (99 lbs).
  • An informed consent document signed and dated.
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Exclusion Criteria
  • Evidence or history of clinically significant abnormality.
  • 12-lead ECG demonstrating QTc >450 msec at Screening.
  • Receiving selective serotonin reuptake inhibitors (SSRIs) and/or sympathomimetic agents.
  • Abnormal liver function tests.
  • A positive urine drug screen, history of excessive alcohol and tobacco use.
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Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
Cohort 1: PlaceboPlacebo-
Cohort 1: 900 mg linezolidLinezolid 900 mg-
Cohort 1: 1200 mg linezolidLinezolid 1200 mg-
Cohort 2: PlaceboPlacebo-
Cohort 2: 600 mg linezolidLinezolid 600 mg-
Cohort 2: 1200 mg linezolidLinezolid 1200 mg-
Cohort 2: 400 mg MoxifloxacinMoxifloxacin 400 mg-
Primary Outcome Measures
NameTimeMethod
Cohort 1: Number of Subjects With Adverse Events (AEs) and Serious Adverse Events (SAEs)From the time the subject had taken at least one dose of study treatment up to 5 weeks

All observed or volunteered AEs and SAEs regardless of treatment group or suspected causal relationship to the investigational product(s) were reported.

Cohort 2: Mean Time-Matched Difference in Time Corresponding to Beginning of Depolarization to Repolarization of the Ventricles, Corrected for Heart Rate Using Fridericia's Formula (QTcF Interval) Between Linezolid 600 mg and 1200 mg Compared to Placebo0.5, 1, 2, 4, 8, 12, 24 hours post-dose

The time corresponding to the beginning of depolarization to repolarization of the ventricles (QT interval) was adjusted for ventricular rate (VR) using the QT and VR from each electrocardiogram by Fridericia's formula (QTcF = QT divided by cube root of VR in seconds). A measure of dispersion is not available.

Secondary Outcome Measures
NameTimeMethod
Cohort 1: Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUC Inf) and Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUC Last)predose, 30 minutes, and at 1 (end of infusion), 1.5, 2, 3, 4, 6, 8, 12, 24, and 46 hours after start of infusion

AUC inf = Area under the plasma concentration versus time curve from time zero (pre-dose) to extrapolated infinite time.

AUC last = Area under the plasma concentration versus time curve from time zero (pre-dose) to time of last quantifiable concentration (0-t).

Cohort 1: Maximum Observed Plasma Concentration (Cmax)predose, 30 minutes, and at 1 (end of infusion), 1.5, 2, 3, 4, 6, 8, 12, 24, and 46 hours after start of infusion
Cohort 1: Time to Reach Maximum Observed Plasma Concentration (Tmax) and Plasma Decay Half-Life (t1/2)predose, 30 minutes, and at 1 (end of infusion), 1.5, 2, 3, 4, 6, 8, 12, 24, and 46 hours after start of infusion

Plasma decay half-life is the time measured for the plasma concentration to decrease by one half.

Cohort 1: Clearance of Linezolid (CL)predose, 30 minutes, and at 1 (end of infusion), 1.5, 2, 3, 4, 6, 8, 12, 24, and 46 hours after start of infusion

Drug clearance = Dose / AUC inf

Cohort 1: Steady-State Volume of Distribution (Vss)predose, 30 minutes, and at 1 (end of infusion), 1.5, 2, 3, 4, 6, 8, 12, 24, and 46 hours after start of infusion

Vss = (mean residence time \[The average total time molecules of a given dose spend in the body\] extrapolated to infinity) multiplied by CL

Cohort 2: Mean Time-Matched Difference in QTcF Intervals Between Moxifloxacin and Placebo0.5, 1, 2, 4, 8, 12, 24 hours post-dose

A measure of dispersion is not available.

Cohort 2: Mean Time-Matched Difference in Uncorrected QT Intervals Between Linezolid 600 mg and 1200 mg Compared to Placebo0.5, 1, 2, 4, 8, 12, 24 hours post-dose

A measure of dispersion is not available.

Cohort 2: AUC Inf and AUC LastPredose, 30 minutes, 1, 2, 4, 8, 12 hours post-dose

AUC inf = Area under the plasma concentration versus time curve from time zero (pre-dose) to extrapolated infinite time.

AUC last = Area under the plasma concentration versus time curve from time zero (pre-dose) to time of last quantifiable concentration (0-t).

Cohort 2: CmaxPredose, 30 minutes, 1, 2, 4, 8, 12 hours post-dose
Cohort 2: Tmax and t1/2Predose, 30 minutes, 1, 2, 4, 8, 12 hours post-dose

Plasma decay half-life is the time measured for the plasma concentration to decrease by one half. Tmax is the time to reach Cmax.

Cohort 2: CLPredose, 30 minutes, 1, 2, 4, 8, 12 hours post-dose

Drug clearance = Dose / AUC inf

Cohort 2: VssPredose, 30 minutes, 1, 2, 4, 8, 12 hours post-dose

Vss = (mean residence time \[The average total time molecules of a given dose spend in the body\] extrapolated to infinity) multiplied by CL

Cohort 2: Number of Subjects With AEs and SAEsFrom the time the subject had taken at least one dose of study treatment up to 5 weeks

All observed or volunteered AEs and SAEs regardless of treatment group or suspected causal relationship to the investigational product(s) were reported.

Trial Locations

Locations (1)

Pfizer Investigational Site

🇸🇬

Singapore, Singapore

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