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A Study to Evaluate the Effect of Mipomersen on Cardiac Repolarization Conducted in Healthy Subjects

Phase 1
Completed
Conditions
Healthy
Interventions
Registration Number
NCT01090661
Lead Sponsor
Kastle Therapeutics, LLC
Brief Summary

To assess the electrocardiogram (ECG) effects of mipomersen administered as a 200-mg subcutaneous (SC) therapeutic and a 200-mg intravenous (IV; \[2-hour infusion\]) supra-therapeutic dose relative to placebo in healthy adult male and female subjects; and to evaluate the safety and pharmacokinetics (PK) of mipomersen when administered as a single therapeutic (200 mg) SC and a single, supra-therapeutic (200 mg) IV dose.

Detailed Description

This will be a randomized, double-blind, single-site, crossover study in healthy male and female subjects to determine if mipomersen administered as a single therapeutic (200 mg) SC and a single supra-therapeutic (200 mg) IV dose delays cardiac repolarization as determined by the measurement of QT/corrected QT (QTc) interval. A total of 60 healthy male and female subjects will be enrolled in this 4-way crossover study, randomly assigned to 1 of 8 treatment sequences, and cross over into 4 treatment periods where each subject will receive both a single SC injection and a single IV infusion during each period.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
60
Inclusion Criteria
  • Written informed consent provided before any study-related procedures are performed.
  • Body mass index (BMI) of 19 to 32 kg/m2 inclusive.
  • Subjects can not have consumed nicotine or nicotine-containing products for at least 6 months before Screening.
  • Subjects are nonpregnant and nonlactating, surgically sterile, postmenopausal, abstinent, or subject or partner is willing to use a reliable method of contraception during the study and 5 months after the last dose of investigational product.
Exclusion Criteria
  • History of risk factors for Torsades de Pointes, known Long QT Syndrome, heart failure, myocardial infarction, angina, or clinically significant abnormal laboratory assessments or family history of Long QT or Brugada Syndrome.
  • Abnormal screening ECG that is interpreted by the Investigator to be clinically significant.
  • Use of concomitant medications (prescribed or over-the-counter), without the approval of the Investigator and Sponsor, within 7 days before the first dose of investigational product.
  • Clinically significant abnormal findings on the physical examination, ECG, blood pressure, heart rate, medical history, or clinical laboratory results at Screening or before dosing.
  • History of clinically significant allergies or hematological, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, or neurological disease.
  • Positive test for HIV antibody, hepatitis C antibody, or hepatitis B surface antigen.
  • Positive test for drugs of abuse, alcohol, or cotinine at Screening or before dosing or history of drug or alcohol abuse or dependence within 1 year before Screening.
  • History of cancer, with the exception of basal cell carcinoma.

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
placeboplaceboPlacebo IV / placebo SC
moxifloxacin IVplacebo400 mg of moxifloxacin IV / placebo SC
mipomersen IV (supra-therapeutic dose)placebo200 mg of mipomersen IV / placebo SC
mipomersen SC (therapeutic dose)mipomersen sodium200 mg of mipomersen SC / placebo IV
mipomersen SC (therapeutic dose)placebo200 mg of mipomersen SC / placebo IV
mipomersen IV (supra-therapeutic dose)mipomersen sodium200 mg of mipomersen IV / placebo SC
moxifloxacin IVmoxifloxacin hydrochloride (Avelox®)400 mg of moxifloxacin IV / placebo SC
Primary Outcome Measures
NameTimeMethod
change from baseline in QTcF (corrected Frederica's CT interval)ECG monitoring up to 24 hours post dose
Secondary Outcome Measures
NameTimeMethod
change in ECG morphological patternsECG monitoring up to 24 hours post dose
ECG intervals (QTcB (corrected Bazett's QT interval), HR (heart rate, PR, QRS, and QT)ECG monitoring up to 24 hours post dose
Correlation between delta delta QTc interval and plasma mipomersen concentrationsECG monitoring up to 24 hours post dose
Incidence of treatment-emergent Adverse EventsAssessed at each visit
mipomersen plasma pharmacokinetic (PK) parameters: Area Under the Curve (AUC 0-22.5h), Maximum Concentration (Cmax), Time to Maximum Concentration (Tmax)Serial PK sampling up to 24 hours post dose

Trial Locations

Locations (1)

PPD Development, LP

🇺🇸

Austin, Texas, United States

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