MedPath

A Study of the Efficacy and Safety of MK-0653H in Japanese Participants With Hypercholesterolemia (MK-0653H-832)

Registration Number
NCT02741245
Lead Sponsor
Organon and Co
Brief Summary

This study will evaluate the efficacy and safety and tolerability of 2 dose levels of MK-0653H in Japanese participants. The primary hypotheses are that the administration of MK-0653H is safe and tolerable and that MK-0653H is superior to single entity of Ezetimibe and Rosuvastatin in percent reduction from baseline in low-density lipoprotein-cholesterol (LDL-C) after 12 weeks of treatment.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
321
Inclusion Criteria
  • Japanese
  • Outpatient with hypercholesterolemia
  • Female participant who is of reproductive potential has to agree to remain abstinent or use (or partner use) two acceptable methods of birth control from date of signed informed consent to the 14 days after the last dose of study drug
  • Will maintain a stable diet that is consistent with the Japan Atherosclerosis Society Guideline 2012 (JAS 2012) for prevention of atherosclerotic cardiovascular diseases for the duration of the study
Exclusion Criteria
  • Uncontrolled hypertension (treated or untreated)
  • Uncontrolled type 1 or type 2 diabetes mellitus
  • History of coronary artery disease (CAD), CAD-equivalent disease
  • Familial hypercholesterolemia or has undergone LDL apheresis
  • Uncontrolled endocrine or metabolic disease known to influence serum lipids or lipoproteins
  • Has had a gastrointestinal tract bypass, or other significant intestinal malabsorption
  • History of cancer within the past 5 years (except for successfully treated dermatological basal cell or squamous cell carcinoma or in situ cervical cancer)
  • Human Immunodeficiency Virus (HIV) positive
  • History of drug/ alcohol abuse within the past 5 years or psychiatric illness not adequately controlled and stable on pharmacotherapy
  • Consumes more than 25 g of alcohol per day
  • Currently following an excessive weight reduction diet
  • Currently engages in a vigorous exercise regimen (e.g.; marathon training, body building training etc.) or intends to start training during the study
  • Hypersensitivity or intolerance to Ezetimibe or Rosuvastatin
  • Myopathy or rhabdomyolysis with Ezetimibe or any statin
  • Pregnant or lactating
  • Taking any other investigational drugs and/or has taken any investigational drugs within 30 days

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Ezetimibe 10 mgEzetimibe 10 mg1 Ezetimibe 10 mg tablet and 2 Rosuvastatin placebo capsules once daily for 12 weeks
Rosuvastatin 2.5 mgRosuvastatin 2.5 mg1 Rosuvastatin 2.5 mg capsule, 1 Rosuvastatin placebo capsule and 1 Ezetimibe placebo tablet once daily for 12 weeks.
Rosuvastatin 5.0 mgPlacebo for Ezetimibe2 Rosuvastatin 2.5 mg capsules and Ezetimibe placebo tablet once daily for 12 weeks.
Rosuvastatin 2.5 mgPlacebo for Rosuvastatin1 Rosuvastatin 2.5 mg capsule, 1 Rosuvastatin placebo capsule and 1 Ezetimibe placebo tablet once daily for 12 weeks.
Ezetimibe 10 mg+ Rosuvastatin 2.5 mgRosuvastatin 2.5 mg1 Ezetimbie 10 mg tablet, 1 Rosuvastatin 2.5 mg capsule and 1 Rosuvastatin placebo capsule once daily for 12 weeks.
Ezetimibe 10 mg+ Rosuvastatin 2.5 mgPlacebo for Rosuvastatin1 Ezetimbie 10 mg tablet, 1 Rosuvastatin 2.5 mg capsule and 1 Rosuvastatin placebo capsule once daily for 12 weeks.
Ezetimibe 10 mgPlacebo for Rosuvastatin1 Ezetimibe 10 mg tablet and 2 Rosuvastatin placebo capsules once daily for 12 weeks
Rosuvastatin 2.5 mgPlacebo for Ezetimibe1 Rosuvastatin 2.5 mg capsule, 1 Rosuvastatin placebo capsule and 1 Ezetimibe placebo tablet once daily for 12 weeks.
Rosuvastatin 5.0 mgRosuvastatin 2.5 mg2 Rosuvastatin 2.5 mg capsules and Ezetimibe placebo tablet once daily for 12 weeks.
Ezetimibe 10 mg+ Rosuvastatin 2.5 mgEzetimibe 10 mg1 Ezetimbie 10 mg tablet, 1 Rosuvastatin 2.5 mg capsule and 1 Rosuvastatin placebo capsule once daily for 12 weeks.
Ezetimibe 10 mg+ Rosuvastatin 5.0 mgEzetimibe 10 mg1 Ezetimbie 10 mg tablet and 2 Rosuvastatin 2.5 mg capsules once daily for 12 weeks.
Ezetimibe 10 mg+ Rosuvastatin 5.0 mgRosuvastatin 2.5 mg1 Ezetimbie 10 mg tablet and 2 Rosuvastatin 2.5 mg capsules once daily for 12 weeks.
Primary Outcome Measures
NameTimeMethod
Percentage Change From Baseline in Low-density Lipoprotein-cholesterol (LDL-C)Baseline and Week 12

Participants had LDL-C levels assessed at baseline and after 12 weeks of study drug administration. The change from baseline was calculated. Results were reported as a M-estimate.

Percentage of Participants Who Experience 1 or More Gallbladder-related AEsup to 14 weeks

Gallbladder-related AEs included Bile Duct Obstruction, Bile Duct Stone, Bile Duct Stenosis, Biliary Colic, Cholangitis, Cholecystectomy, Cholecystitis, Cholelithiasis, Gallbladder Disorder, Gallbladder Perforation, Hepatic Pain, and Hydrocholecystis.

Percentage of Participants Who Had Study Drug Discontinued Due to Adverse Eventup to 12 weeks

An AE was defined as any untoward medical occurrence in a subject which does not necessarily have a causal relationship with the treatment. An AE was any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with use of a medicinal product, whether or not considered related to the medicinal product. The percentage of participants that had study drug discontinued due to an AE was summarized.

Percentage of Participants Who Experience Elevations in Creatine Kinase (CK) ≥10 Times ULN With Muscle Symptomsup to 12 weeks

Participants had CK levels assessed throughout the 52 week treatment period. Participants who had any CK level that was ≥10 x ULN and had associated muscle symptoms present within +/- 7 days were recorded. The CK ULNs for males and females were 287 IU/L and 163 IU/L, respectively.

Percentage of Participants Who Experience 1 or More Gastrointestinal-related AEsup to 14 weeks

Gastrointestinal-related AEs included all preferred terms within system organ class of Gastrointestinal Disorders except Chapped Lips and Toothache.

Percentage of Participants Who Experience 1 or More Hepatitis-related AEsup to 14 weeks

Hepatitis-related AEs included Cholestasis, Cytolytic Hepatitis, Hepatic Cyst, Hepatic Failure, Hepatic Lesion, Hepatic Necrosis, Hepatitis, Hepatitis Cholestatic, Hepatitis Fulminant, Hepatitis Infectious, Hepatocellular Injury, Hepatomegaly, Jaundice, Jaundice Cholestatic.

Percentage of Participants Who Experience Elevation in Alanine Aminotransferase (ALT) ≥5 Times Upper Normal Limit (ULN)up to 12 weeks

Participants had ALT levels assessed throughout the 12 week treatment period. Participants who had an assessments of ALT that was 5x ULN or greater were recorded. The ALT ULN was 40 U/L.

Percentage of Participants Who Experience Elevation in Aspartate Aminotransferase (AST) ≥10 Times Upper Normal Limit (ULN)up to 12 weeks

Participants had AST levels assessed throughout the 12 week treatment period. Participants who had an assessments of AST that was 10x ULN or greater were recorded. The AST ULN was 40 U/L.

Percentage of Participants Who Experience Elevations in Creatine Kinase (CK) ≥10 Times ULNup to 12 weeks

Participants had creatine phosphokinase (CK) levels assessed throughout the 12 week treatment period. Participants who had any CK level that was ≥10 x ULN were recorded. The CK ULNs for males and females were 287 IU/L and 163 IU/L, respectively.

Percentage of Participants Who Experience Consecutive Elevations in Alanine Aminotransferase (ALT) and/or Aspartate Aminotransferase (AST) ≥3 Times Upper Normal Limit (ULN)up to 12 weeks

Participants had ALT and AST levels assessed throughout the 12 week treatment period. Participants who had 2 consecutive assessments of ALT and/or AST that were 3 x ULN or greater were recorded. The ALT and AST ULNs were 40 U/L.

Percentage of Participants Who Experience at Least 1 Adverse Event (AE)up to 14 weeks

An AE was defined as any untoward medical occurrence in a subject which does not necessarily have a causal relationship with the treatment. An AE was any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with use of a medicinal product, whether or not considered related to the medicinal product. The percentage of participants that reported at least 1 AE was summarized

Percentage of Participants Who Experience 1 or More Allergic Reaction or Rash AEsup to 14 weeks

Allergic Reaction or Rash AEs included Allergy to Arthropod Sting, Anaphylactoid Reaction, Anaphylactic Reaction, Anaphylatic Shock, Anaphylactoid Shock, Angioedema, Conjunctivitis Allergic, Contrast Media Reaction, Dermatitis, Dermatitis Allergic, Dermatitis Atopic, Dermatitis Bullous, Dermatitis Contact, Dermatitis Psoriasiform, Drug Hypersensitivity, Eczema, Eosinophila, Erythema, Eye Allergy, Face Oedema, Hypersensitivity, Mechanical Urticaria, Palmar Erythema, Periorbital Oedema, Photodermatosis, Photosensitivity Allergic reaction, Photosensitivity Reaction, Pigmentation Disorder, Pruritus, Pruritus Generalised, Rash, Rash Erythematous, Rash Follicular, Rash Generalised, Rash Maculo-Papular, Rash Papulosquamous, Rash Pruritic, Rash Pustular, Rash Vesicular, Rhinitis, Rhinitis Allergic, Rosacea, Skin Exfoliation, Skin Disorder, Skin Hyperpigmentation, Skin Lesion, Skin Mass, Skin Ulcer, Subcutaneous Nodule, Swelling Face, Systemic Lupus Erythematosus Rash, Urticaria.

Percentage of Participants Who Experience Elevation in Aspartate Aminotransferase (AST) ≥5 Times Upper Normal Limit (ULN)up to 12 weeks

Participants had AST levels assessed throughout the 12 week treatment period. Participants who had an assessments of AST that was 5x ULN or greater were recorded. The AST ULN was 40 U/L.

Percentage of Participants Who Experience Consecutive Elevations in Alanine Aminotransferase (ALT) and/or Aspartate Aminotransferase (AST) ≥10 Times Upper Normal Limit (ULN)up to 12 weeks

Participants had ALT and AST levels assessed throughout the 12 week treatment period. Participants who had 2 consecutive assessments of ALT and/or AST that were 10x ULN or greater were recorded. The ALT and AST ULNs were 40 U/L.

Percentage of Participants Who Experience Consecutive Elevations in Alanine Aminotransferase (ALT) ≥3 Times Upper Normal Limit (ULN)up to 12 weeks

Participants had ALT levels assessed throughout the 12 week treatment period. Participants who had 2 consecutive assessments of ALT that were 3 x ULN or greater were recorded. The ALT ULN was 40 U/L.

Percentage of Participants Who Experience Consecutive Elevations in Aspartate Aminotransferase (AST) ≥3 Times Upper Normal Limit (ULN)up to 12 weeks

Participants had AST levels assessed throughout the 12 week treatment period. Participants who had 2 consecutive assessments of AST that were 3 x ULN or greater were recorded. The AST ULN was 40 U/L..

Percentage of Participants Who Experience Elevation in Alanine Aminotransferase (ALT) ≥10 Times Upper Normal Limit (ULN)up to 12 weeks

Participants had ALT levels assessed throughout the 12 week treatment period. Participants who had an assessments of ALT that was 10x ULN or greater were recorded. The ALT ULN was 40 U/L.

Percentage of Participants With Potential Hy's Law Conditionup to 12 weeks

Percentage of Participants with Potential Hy's Law Condition (defined as serum ALT or serum AST elevations \>3xULN, with serum alkalinephosphatase \<2xULN and total bilirubin (TBL) ≥2xULN) was summarized. The ALT and AST ULNs were 40 U/L. The ULN for alkaline phosphatase was 359 IU/L and the ULN for total bilirubin was 1.2 mg/dL.

Percentage of Participants Who Experience Elevations in Creatine Kinase (CK) ≥10 Times ULN and Drug-Related Muscle Symptomsup to 12 weeks

Participants had CK levels assessed throughout the 52 week treatment period. Participants who had any CK level that was ≥10 x ULN and had associated muscle symptoms present within +/- 7 days that were reported as at least possibly-related to study drug were recorded. The CK ULNs for males and females were 287 IU/L and 163 IU/L, respectively.

Secondary Outcome Measures
NameTimeMethod
© Copyright 2025. All Rights Reserved by MedPath