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Study to Assess the Tolerability and Efficacy of Anacetrapib (MK-0859) Co-Administered With Statin in Participants With Heterozygous Familial Hypercholesterolemia (MK-0859-020)

Phase 3
Completed
Conditions
Hyperlipoproteinemia Type II
Hypercholesterolemia, Familial
Interventions
Drug: Placebo
Registration Number
NCT01524289
Lead Sponsor
Merck Sharp & Dohme LLC
Brief Summary

The objective of this study is to evaluate the efficacy and tolerability of adding anacetrapib to ongoing statin therapy in participants with heterozygous familial hypercholesterolemia (HeFH).

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
306
Inclusion Criteria
  • If of reproductive potential, must agree to remain abstinent or use (or have their partner use) 2 acceptable methods of birth control for the duration of the study
  • Diagnosed with Heterozygous Familial Hypercholesterolemia (HeFH)
  • Have been treated with an optimal dose of statin for at least 6 weeks
Exclusion Criteria
  • Received treatment with low-density lipoprotein (LDL) apheresis within 4 weeks of screening or expect to undergo treatment with LDL apheresis during the course of the study
  • Homozygous familial hypercholesterolemia
  • Severe chronic heart failure
  • Uncontrolled hypertension
  • Uncontrolled cardiac arrhythmias, myocardial infarction (MI), percutaneous coronary intervention (PCI), coronary artery bypass graft (CABG), unstable angina, or stroke within 3 months
  • Uncontrolled endocrine or metabolic disease known to influence serum lipids or lipoproteins
  • Active or chronic hepatobiliary, hepatic, or gall bladder disease
  • Pregnant or breast-feeding, or plans to become pregnant during the study or within 2 years after stopping study medication
  • History of ileal bypass, gastric bypass, or other significant condition associated with malabsorption
  • Human immunodeficiency virus (HIV) positive
  • History of malignancy ≤5 years
  • Donated blood products or has had phlebotomy of >300 mL within 8 weeks or intends to donate 250 mL of blood products or receive blood products within the projected duration of the study
  • Currently taking medications that are potent inhibitors or inducers of cytochrome P450 3A4 (CYP3A) (including but not limited to cyclosporine, systemic itraconazole or ketoconazole, erythromycin, clarithromycin, or telithromycin, nefazodone, protease inhibitors, carbamazepine, phenobarbital, phenytoin, rifabutin, rifampin, St John's wort) or has discontinued treatment <3 weeks prior
  • Consumes more than 2 alcoholic drinks per day
  • Currently participating or has participated in a study with an investigational compound or device within 3 months
  • Receiving treatment with systemic corticosteroids or taking systemic anabolic agents

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
PlaceboPlaceboParticipants were administered one matching placebo tablet orally once daily with a meal for 52 weeks during the treatment period.
AnacetrapibAnacetrapibParticipants were administered one tablet of 100 mg anacetrapib orally once daily with a meal for 52 weeks during the treatment period.
Primary Outcome Measures
NameTimeMethod
Percentage of Participants With Any Serious Adverse Event - Treatment PhaseUp to 52 weeks

A serious adverse experience (SAE) was any adverse event that occurred at any dose that resulted in death or was life threatening, resulted in a persistent or significant disability/incapacity, resulted in or prolonged an existing inpatient hospitalization, or was a congenital anomaly/birth defect. The percentage of participants with any serious adverse event during the treatment phase is presented.

Percentage of Participants With Potassium Levels < Lower Limit of Normal (LLN)Up to 52 weeks

Participants had potassium levels assessed throughout the 52-week treatment period. The percentage of participants who had any potassium level that was \< the LLN of 3.5 mEq/L during the treatment phase is presented.

Percentage of Participants With CK Level >=10 x ULN With Muscle SpasmsUp to 52 weeks

Participants had CK levels assessed throughout the 52-week treatment period. The percentage of participants who had any CK level that was \>=10 x ULN and had associated muscle spasms during the treatment phase is presented.

Percent Change From Baseline in Low-Density Lipoprotein Cholesterol (LDL-C) - Treatment PhaseBaseline and Week 52

LDL-C levels were measured at baseline and week 52 (or at discontinuation) using a beta quantification method. The Treatment Phase was the period from the date of the participant's first dose of study treatment (randomization visit, Visit 3) to the participant's last visit on treatment (discontinuation visit or Visit 8 \[Week 52\]).

Percentage of Participants With Changes in Diastolic Blood Pressure (DBP) >= 10 mm HgUp to 52 weeks

Participants had DBP assessed at baseline and throughout the 52-week treatment period. The percentage of participants who had a DBP reading that was \>= 10 mm Hg higher than their baseline DBP for any assessment performed during the treatment phase is presented.

Percentage of Participants With Chloride Levels > ULNUp to 52 weeks

Participants had chloride levels assessed throughout the 52-week treatment period. The percentage of participants who had any chloride level that was \> the ULN of 110 mEq/L during the treatment phase is presented.

Percentage of Participants Adjudicated Cardiovascular (CV) SAEUp to 52 weeks

An AE or suspected adverse reaction was considered an SAE if it resulted in any of the following outcomes: death, a life-threatening adverse event, inpatient hospitalization or prolongation of existing hospitalization, a persistent or significant incapacity or substantial disruption of the ability to conduct normal life functions, or a congenital anomaly/birth defect. All events were adjudicated by an expert committee independent of the Sponsor. The percentage of participants that experienced adjudicated SAEs of CV death, non-fatal stroke, non-fatal myocardial infarction, or unstable angina during the treatment phase is presented.

Percentage of Participants Who Died From Any Cause - Treatment PhaseUp to 52 weeks

The percentage of participants who died from any cause during the treatment phase is presented. All deaths were adjudicated by an expert committee independent of the Sponsor.

Percentage of Participants With Changes in Systolic Blood Pressure (SBP) >= 10 mm HgUp to 52 weeks

Participants had SBP assessed at baseline and throughout the 52-week treatment period. Percentage of participants who had a SBP reading that was \>= 10 mm Hg higher than their baseline SBP for any assessment performed during the treatment phase is presented.

Percentage of Participants With Bicarbonate Levels > ULNUp to 52 weeks

Participants had bicarbonate levels assessed throughout the 52-week treatment period. The percentage of participants who had any bicarbonate level that was \> the ULN of 33 mEq/L during the treatment phase is presented.

Percentage of Participants With Creatine Kinase (CK) Level >=10 x ULNUp to 52 weeks

Participants had CK levels assessed throughout the 52-week treatment period. The percentage of participants who had any CK level that was \>=10 x ULN during the treatment phase is presented.

Percentage of Participants With Any Adverse Event - Treatment PhaseUp to 52 weeks

An adverse event (AE) or experience was any unfavorable and unintended change in the structure (signs), function (symptoms), or chemistry (laboratory data) of the body temporally associated with any use of a study treatment, whether or not considered related to the use of the study treatment. Any worsening of a preexisting condition which was temporally associated with the use of the study treatment is also an AE. The percentage of participants with any adverse event during the treatment phase is presented.

Percentage of Participants With Any Treatment-Related Adverse Event - Treatment PhaseUp to 52 weeks

An AE was defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the study treatment, whether or not considered related to the use of the treatment. Any worsening of a preexisting condition which was temporally associated with the use of the study treatment was also an AE. AEs reported by the investigator as definitely, probably or possibly related to study treatment were considered treatment-related. The percentage of participants with any treatment-related adverse event during the treatment phase is presented.

Percentage of Participants Discontinuing Study Treatment Due to an Adverse Event - Treatment PhaseUp to 52 weeks

An adverse event (AE) was defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the study treatment, whether or not considered related to the use of the drug. Any worsening of a preexisting condition which was temporally associated with the use of the study drug was also an AE. The percentage of participants who discontinued study treatment due to an AE during the treatment phase is presented.

Percentage of Participants With Sodium Levels > Upper Limit of Normal (ULN)Up to 52 weeks

Participants had sodium levels assessed throughout the 52-week treatment period. The percentage of participants who had any sodium level that was greater than the ULN of 145 mEq/L during the treatment phase is presented.

Percentage of Participants With Changes in SBP >= 15 mm HgUp to 52 weeks

Participants had SBP assessed at baseline and throughout the 52-week treatment period. The percentage of participants who had a SBP reading that was \>= 15 mm Hg higher than their baseline SBP for any assessment performed during the treatment phase is presented.

Percentage of Participants With Consecutive Changes in Alanine Aminotransferase (ALT) and/or Aspartate Aminotransferase (AST) of >=3 x ULNUp to 52 weeks

Participants had AST and ALT levels assessed throughout the 52-week treatment period. The percentage of participants who had 2 consecutive assessments of either AST or ALT that were 3 x ULN or greater during the treatment phase is presented.

Secondary Outcome Measures
NameTimeMethod
Percent Change From Baseline in High-Density Lipoprotein Cholesterol LevelsBaseline and Week 52

The efficacy of adding anacetrapib 100 mg relative to placebo on plasma concentrations of high-density lipoprotein cholesterol (HDL-C) was evaluated at Week 0 (start of treatment phase) and Week 52 (end of treatment phase) or at discontinuation.

Percent Change From Baseline in Non-High-Density Lipoprotein Cholesterol LevelsBaseline and Week 52

The efficacy of adding anacetrapib 100 mg was evaluated relative to placebo on plasma concentrations of non-high-density lipoprotein cholesterol (HDL-C) for the FAS population at Week 0 (start of treatment phase) and Week 52 (end of treatment phase) or at discontinuation.

Percent Change From Baseline in Apolipoprotein (Apo) B LevelsBaseline and Week 52

The efficacy of adding anacetrapib 100 mg was evaluated relative to placebo on plasma concentrations of apolipoprotein (Apo) B for the FAS population at Week 0 (start of treatment phase) and Week 52 (end of treatment phase) or at discontinuation.

Percent Change From Baseline in Lipoprotein(a) (Lp[a]) LevelsBaseline and Week 52

The efficacy of adding anacetrapib 100 mg was evaluated relative to placebo on plasma concentrations of lipoprotein(a) (Lp\[a\]) for the FAS population at Week 0 (start of treatment phase) and Week 52 (end of treatment phase) or at discontinuation.

Percent Change From Baseline in Apolipoprotein (Apo) A-1 LevelsBaseline and Week 52

The efficacy of adding anacetrapib 100 mg was evaluated relative to placebo on plasma concentrations of Apo A-1 for the FAS population at Week 0 (start of treatment phase) and Week 52 (end of treatment phase) or at discontinuation.

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