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A Double-Blind, Randomized Study to Evaluate the Efficacy and Safety of Lapaquistat Acetate 50 mg versus Placebo in Subjects with Hypercholesterolemia, With an Optional Open-Label Extensio

Phase 3
Conditions
elevated cholesterol
hypercholesterolemia
10013317
Registration Number
NL-OMON31031
Lead Sponsor
Takeda
Brief Summary

Not available

Detailed Description

Not available

Recruitment & Eligibility

Status
Pending
Sex
Not specified
Target Recruitment
71
Inclusion Criteria

1. The subject is a male or female and at least 18 years of age.
2. A female subject of childbearing potential who is sexually active agrees to use adequate contraception from screening throughout the duration of the study and for 30 days following the last dose. Women NOT of child bearing potential are defined as those who have been surgically sterilized (hysterectomy, oophorectomy, tubal ligation) or who are postmenopausal (defined as at least 2 years since last regular menses). Acceptable methods of contraception are defined in Section 9.1.10 Contraception and Pregnancy Avoidance Procedure.
3. The subject is capable of understanding and complying with protocol requirements.
4. The subject or the subject*s legally acceptable representative signs a written informed consent form prior to the initiation of any study procedures.
5. Prior to Randomization, the subject has a mean LDL-C *130 mg/dL (3.36 mmol/L) and *190 mg/dL (4.92 mmol/L) for 2 consecutive samples (at least 1 week apart). The difference between the 2 individual LDL-C values must not exceed 15% of the higher value.
6. Prior to Randomization, the subject has mean TG <400 mg/dL (4.52 mmol/L) for 2 consecutive samples (at least 1 week apart). The upper value for either sample must be *450 mg/dL (5.08 mmol/L).
7. The subject is willing and able to comply with a standardized diet (TLC or equivalent).

Exclusion Criteria

1. The subject has an ALT or AST level >2 times the upper limit of normal (ULN), identified during screening (eg, from the V1 blood sample). If a repeat test is *2 times ULN then contact the Medical Monitor for consideration of inclusion - See Section 9.3.1
2. The subject has a serum creatinine >133 mmol/L (>1.5mg/dL), identified during screening (eg, from the V1 blood sample).
3. The subject has a CK >3 times the upper limit of normal (ULN), identified during screening (eg, from the V1 blood sample). If a repeat test is *3 times the ULN then contact the Medical Monitor for consideration of inclusion - See Section 9.3.1
4. The subject has active liver disease or jaundice.
5. The subject has taken any fibrates within 42 days of Visit 1 or any lipid-lowering therapy for at least 30 days prior to Screening (Visit 1). (See Excluded Medications 7.3)
1. The subject has an ALT or AST level >2 times the upper limit of normal (ULN), identified during screening (eg, from the V1 blood sample). If a repeat test is *2 times ULN then contact the Medical Monitor for consideration of inclusion - See Section 9.3.1
2. The subject has a serum creatinine >133 mmol/L (>1.5mg/dL), identified during screening (eg, from the V1 blood sample).
3. The subject has a CK >3 times the upper limit of normal (ULN), identified during screening (eg, from the V1 blood sample). If a repeat test is *3 times the ULN then contact the Medical Monitor for consideration of inclusion - See Section 9.3.1
4. The subject has active liver disease or jaundice.
5. The subject has taken any fibrates within 42 days of Visit 1 or any lipid-lowering therapy for at least 30 days prior to Screening (Visit 1). (See Excluded Medications 7.3)
6. The subject has a previous history of cancer that has been in remission for less than 5 years prior to the first dose of study medication. This criterion does not include those subjects with basal cell or stage 1 squamous cell carcinoma of the skin.
7. The subject has an endocrine disorder, such as Cushing*s syndrome, hyperthyroidism, or inappropriately treated hypothyroidism affecting lipid metabolism. Subjects with hypothyroidism on appropriate replacement therapy (defined as stable thyroid hormone replacement at least 3 months prior to Screening and TSH levels *1.5 times ULN) will be eligible for enrollment.
8. The subject has a history of myocardial infarction, angina pectoris, unstable angina, transient ischemic attacks, cerebrovascular accident, peripheral vascular disease, abdominal aortic aneurysm, coronary angioplasty, coronary or peripheral arterial surgery (bypass graft surgery), or multiple risk factors that confer a 10-year risk for cardiovascular heart disease (CHD) >20% based on Framingham risk scoring.
9. The subject has a positive hepatitis B surface antigen or hepatitis C virus antibody test, as determined by medical history and/or subject*s verbal report.
10. The subject has a positive human immunodeficiency virus (HIV) status or is taking antiretroviral medications, as determined by medical history and/or subject*s verbal report.
11. The subject is unable or unwilling to discontinue excluded medications or to continue stable doses of *stable dose* medications. (See Excluded Medications and Concomitant Medications.)
12. The subject has received any investigational medication 30 days prior to screening, (for drugs with a long half-life, within a period of less than 5 ti

Study & Design

Study Type
Interventional
Study Design
Not specified
Primary Outcome Measures
NameTimeMethod
<p>The primary efficacy variable for this study is fasting plasma LDL-C</p><br>
Secondary Outcome Measures
NameTimeMethod
<p>The secondary efficacy variables are other lipid parameters including:<br /><br>TC.<br /><br>Apolipoprotein B.<br /><br>TG.<br /><br>HDL-C.<br /><br>Apolipoprotein A1.<br /><br>VLDL-C.<br /><br>Non-HDL-C (TC-HDL-C).<br /><br>LDL-C/HDL-C, TC/HDLC, Apo B/Apo A1 ratios.<br /><br><br /><br>Other:<br /><br>hs-CRP.<br /><br><br /><br>The percentage of subjects reaching LDL-C levels of <160 mg/dL (4.1 mmol/L),<br /><br><130 mg/dL (3.37 mmol/L) and <100 mg/dL (2.59 mmol/L) at Week 12 (or ET) during<br /><br>the double-blind will be evaluated.<br /><br><br /><br>Safety Variables<br /><br>The safety assessments include the following variables:<br /><br>AEs.<br /><br>Safety laboratory tests.<br /><br>Physical examination.<br /><br>Vital signs.<br /><br>12-Lead ECG.</p><br>
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