Safety and Efficacy of Lapaquistat Acetate Taken Alone and With Atorvastatin in Subjects With Primary Dyslipidemia

NCT ID: NCT00487994

Last Updated: 2012-05-24

Study Results

Results pending

The study team has not published outcome measurements, participant flow, or safety data for this trial yet. Check back later for updates.

Basic Information

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Recruitment Status

COMPLETED

Clinical Phase

PHASE3

Total Enrollment

2130 participants

Study Classification

INTERVENTIONAL

Study Start Date

2004-11-30

Study Completion Date

2007-05-31

Brief Summary

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The purpose of this study is to evaluate the overall safety of Lapaquistat Acetate, once daily (QD), by itself or in combination with atorvastatin in subjects with primary dyslipidemia.

Detailed Description

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According to the World Health Organization, CHD is now the leading cause of death worldwide. In 2001, CHD caused 7.2 million deaths and estimates for 2020 indicate that annual CHD deaths will increase to 11.1 million. These statistics suggest that improved options are needed to treat hypercholesterolemia and dyslipidemia.

The balance among cholesterol synthesis, dietary intake, and degradation is normally adequate to maintain healthy cholesterol plasma levels. However, in patients with hypercholesterolemia, elevated low-density lipoprotein cholesterol leads to atherosclerotic deposition of cholesterol in the arterial walls. Consequently, in this population it has been established that lowering low-density lipoprotein cholesterol plasma concentrations effectively reduces cardiovascular morbidity and mortality. The National Cholesterol Education Program Adult Treatment Panel III has therefore identified control of low-density lipoprotein cholesterol as essential in the prevention and management of CHD. Additional lipid risk factors designated by National Cholesterol Education Program Adult Treatment Panel III include elevated triglycerides, elevated non-high-density lipoprotein cholesterol (atherogenic lipoproteins), and low levels of high-density lipoprotein cholesterol. Lipoproteins rich in triglycerides, such as very-low-density lipoprotein cholesterol, appear to contribute to atherosclerosis, whereas the apparent protective effect of high-density lipoprotein cholesterol, which is likely related to high-density lipoprotein cholesterol-facilitated transport of cholesterol away from atherosclerotic deposits, may be limited at low high-density lipoprotein cholesterol concentrations.

Initial dietary and lifestyle measures taken to control dyslipidemia are often inadequate, and most patients require pharmacologic intervention. Currently, 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors (statins) are the first-line monotherapies most often prescribed to reduce low-density lipoprotein cholesterol, after diet and therapeutic lifestyle change. However, with statin monotherapy, many patients fail to reach National Cholesterol Education Program Adult Treatment Panel III recommended levels of low-density lipoprotein cholesterol reduction. As a result, the statin dosage must be increased or an additional treatment added to achieve treatment goals. Increasing the statin dosage may result in decreased tolerability and potential safety concerns, contributing to the high discontinuation rates of statins and their prescription at low and often ineffective doses. Further, although the effectiveness of increasing the dose varies among the statins, in general, doubling of the dose above the minimum effective dose has been found to decrease serum low-density lipoprotein cholesterol by only an additional 6 percent.

TGRD is developing an orally active squalene synthase inhibitor, TAK-475 (lapaquistat acetate) for the treatment of dyslipidemia. Lapaquistat acetate inhibits the biosynthesis of cholesterol by inhibiting the enzyme squalene synthase, which catalyzes the conversion of farnesyl diphosphate to squalene-a precursor in the final steps of cholesterol production.

Study Participation is anticipated to be up to two years.

Conditions

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Dyslipidemia

Study Design

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Allocation Method

RANDOMIZED

Intervention Model

PARALLEL

Primary Study Purpose

TREATMENT

Blinding Strategy

QUADRUPLE

Participants Caregivers Investigators Outcome Assessors

Study Groups

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Lapaquistat Acetate 100 mg QD

Group Type EXPERIMENTAL

Lapaquistat acetate

Intervention Type DRUG

Lapaquistat acetate 100 mg, tablets, orally, once daily and Atorvastatin placebo-matching capsules, orally, once daily for up to 96 weeks.

Lapaquistat Acetate 100 mg QD + Atorvastatin 10 mg QD

Group Type EXPERIMENTAL

Lapaquistat acetate and atorvastatin

Intervention Type DRUG

Lapaquistat acetate 100 mg, tablets, orally, once daily and Atorvastatin 10 mg, capsules, orally, once daily for up to 96 weeks.

Atorvastatin 10 mg QD

Group Type ACTIVE_COMPARATOR

Atorvastatin

Intervention Type DRUG

Lapaquistat acetate placebo-matching tablets, orally, once daily and Atorvastatin 10 mg, capsules, orally, once daily for up to 96 weeks.

Interventions

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Lapaquistat acetate

Lapaquistat acetate 100 mg, tablets, orally, once daily and Atorvastatin placebo-matching capsules, orally, once daily for up to 96 weeks.

Intervention Type DRUG

Lapaquistat acetate and atorvastatin

Lapaquistat acetate 100 mg, tablets, orally, once daily and Atorvastatin 10 mg, capsules, orally, once daily for up to 96 weeks.

Intervention Type DRUG

Atorvastatin

Lapaquistat acetate placebo-matching tablets, orally, once daily and Atorvastatin 10 mg, capsules, orally, once daily for up to 96 weeks.

Intervention Type DRUG

Other Intervention Names

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TAK-475 TAK-475 Lipitor Lipitor

Eligibility Criteria

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Inclusion Criteria

* Has a confirmatory central laboratory result with low density lipoprotein cholesterol greater than or equal to 3.37 mmol/L and less than 5.69 mmol/L, and triglyceride less than 4.52 mmol/L.
* Females of child-bearing age must have undergone surgical sterilization, hysterectomy, tubal ligation, or bilateral oophorectomy; other female subjects must have been postmenopausal.
* Must be in good physical and mental health as determined by a physician on the basis of medical history, physical examination, and laboratory results.
* Has a fasting low density lipoprotein cholesterol level greater than or equal to 3.37 mmol/L and less than 4.92 mmol/L, and a triglyceride value less than 4.52 mmol/L.

Exclusion Criteria

* Coronary Heart Disease or Coronary Heart Disease-risk factors comprised of:

* Diabetes mellitus type 1 or 2.
* History or presence of myocardial infarction, angina pectoris, unstable angina, coronary angioplasty, coronary or peripheral arterial surgery (bypass graft), aortic aneurysm, transient ischemic attacks, or cerebrovascular accident.
* A body mass index less than 15 or greater than 35.
* A history or presence of:

* Drug abuse or a history of alcohol abuse within the 2 years previous to screening.
* Uncontrolled hypertension despite medical treatment
* Thyroid disease, particularly hyperthyroidism or subjects whose thyroid replacement therapy was initiated within the previous 3 months.
* Human immunodeficiency virus-positive status, or hepatitis B or C infection.
* Malignancy, except subjects whose malignancy had been diagnosed as stage I basal or squamous cell carcinoma.
* Heterozygous or homozygous familial hypercholesterolemia or known type III hyperlipoproteinemia.
* Fibromyalgia, myopathy, rhabdomyolysis, or unexplained muscle pain and/or discontinuation of statins due to myalgia.
* Trauma to the eye or eye irradiation; glaucoma; iritis; uveitis; prior intraocular surgery, laser surgery to the iris, retinal photocoagulation, or laser trabeculoplasty; corneal opacification or other medial opacities; or had undergone LASIK refractive surgery within 6 months prior to screening.
* A clinically significant food allergy that would prevent adherence to the specialized diet.
* Any other serious disease or condition that might have affected life expectancy or made it difficult to successfully manage and monitor the subject according to the protocol.
* Has a known hypersensitivity or history of adverse reaction to atorvastatin or to lapaquistat acetate.
* Is taking part in another investigational study or had been participating in an investigational study within the 30 days prior to Screening Visit 1.
* Has an alanine aminotransferase or aspartate aminotransferase level greater than 2 times the upper limit of normal, active liver disease, jaundice, serum creatinine greater than 135 μmol/L (1.5 mg/dL), or creatine kinase greater than 3 times the upper limit of normal.
Minimum Eligible Age

18 Years

Eligible Sex

ALL

Accepts Healthy Volunteers

No

Sponsors

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Takeda

INDUSTRY

Sponsor Role lead

Responsible Party

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Responsibility Role SPONSOR

Principal Investigators

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Medical Director

Role: STUDY_DIRECTOR

Takeda

Locations

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Birmingham, Alabama, United States

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Mobile, Alabama, United States

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Northport, Alabama, United States

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Chandler, Arizona, United States

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Phoenix, Arizona, United States

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Sierra Vista, Arizona, United States

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Jonesboro, Arkansas, United States

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Little Rock, Arkansas, United States

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Anaheim, California, United States

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Rancho Cucamonga, California, United States

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Santa Rosa, California, United States

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Golden, Colorado, United States

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Coral Gables, Florida, United States

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Fort Myers, Florida, United States

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Jacksonville, Florida, United States

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Sarasota, Florida, United States

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West Palm Beach, Florida, United States

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Dunwoody, Georgia, United States

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Boise, Idaho, United States

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Idaho Falls, Idaho, United States

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Arlington Heights, Illinois, United States

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Chicago, Illinois, United States

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Elk Grove Village, Illinois, United States

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Evansville, Indiana, United States

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Indianapolis, Indiana, United States

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Waterloo, Iowa, United States

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Kansas City, Kansas, United States

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Overland Park, Kansas, United States

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Louisville, Kentucky, United States

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New Orleans, Louisiana, United States

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Flint, Michigan, United States

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Edina, Minnesota, United States

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St Louis, Missouri, United States

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Omaha, Nebraska, United States

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Ship Bottom, New Jersey, United States

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Rochester, New York, United States

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Syracuse, New York, United States

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Charlotte, North Carolina, United States

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Statesville, North Carolina, United States

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Wilmington, North Carolina, United States

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Winston-Salem, North Carolina, United States

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Cincinnati, Ohio, United States

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Tulsa, Oklahoma, United States

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Philadelphia, Pennsylvania, United States

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Tipton, Pennsylvania, United States

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Anderson, South Carolina, United States

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Mt. Pleasant, South Carolina, United States

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Simpsonville, South Carolina, United States

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Cordova, Tennessee, United States

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Morristown, Tennessee, United States

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Corpus Christi, Texas, United States

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Dallas, Texas, United States

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Fort Worth, Texas, United States

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Houston, Texas, United States

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Plano, Texas, United States

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San Antonio, Texas, United States

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Temple, Texas, United States

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Texarkana, Texas, United States

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Norfolk, Virginia, United States

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Richmond, Virginia, United States

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Lakewood, Washington, United States

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Buenos Aires, , Argentina

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Córdoba, , Argentina

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La Plata, , Argentina

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Morón, , Argentina

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Pilar, , Argentina

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Rosario, , Argentina

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Salta, , Argentina

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Santa Fe, , Argentina

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Santiago, , Chile

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Brno, , Czechia

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Olomouc, , Czechia

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Prague, , Czechia

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Tartu, , Estonia

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Berlin, , Germany

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Freiburg im Breisgau, , Germany

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Görlitz, , Germany

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Hamburg, , Germany

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Mannheim, , Germany

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Mönchengladbach, , Germany

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Munich, , Germany

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Schwerin, , Germany

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Budapest, , Hungary

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Debrecen, , Hungary

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Esztergom, , Hungary

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Győr, , Hungary

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Gyula, , Hungary

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Kecskemét, , Hungary

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Warszawa, , Hungary

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Riga, , Latvia

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Kaunas, , Lithuania

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Vilnius, , Lithuania

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Vilnius-21, , Lithuania

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Distrito Federal, , Mexico

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Guadalajara, , Mexico

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Jalisco, , Mexico

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Mexico City, , Mexico

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San Luis Potosí City, , Mexico

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Zapopan, , Mexico

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Es Velp, , Netherlands

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Groningen, , Netherlands

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Leiden, , Netherlands

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Rotterdam, , Netherlands

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Zoetermeer, , Netherlands

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Lima, , Peru

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Bialystok, , Poland

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Bydgoszcz, , Poland

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Gdansk, , Poland

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Gorzów Wielkopolski, , Poland

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Grudziądz, , Poland

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Płońsk, , Poland

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Torun, , Poland

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Wroclaw, , Poland

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Włocławek, , Poland

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Moscow, , Russia

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Saint Petersburg, , Russia

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Saratov, , Russia

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Komárno, , Slovakia

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Košice, , Slovakia

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Levice, , Slovakia

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Cape Town, , South Africa

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Johannesburg, , South Africa

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Parow, , South Africa

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Western Cape, , South Africa

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Truro, Cornwall, United Kingdom

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Blackpool, Lancashire, United Kingdom

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Bolton, Lancashire, United Kingdom

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Guildford, Surrey, United Kingdom

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Countries

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United States Argentina Chile Czechia Estonia Germany Hungary Latvia Lithuania Mexico Netherlands Peru Poland Russia Slovakia South Africa United Kingdom

References

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Stein EA, Bays H, O'Brien D, Pedicano J, Piper E, Spezzi A. Lapaquistat acetate: development of a squalene synthase inhibitor for the treatment of hypercholesterolemia. Circulation. 2011 May 10;123(18):1974-85. doi: 10.1161/CIRCULATIONAHA.110.975284. Epub 2011 Apr 25.

Reference Type RESULT
PMID: 21518985 (View on PubMed)

Other Identifiers

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2004-000775-34

Identifier Type: EUDRACT_NUMBER

Identifier Source: secondary_id

U1111-1122-7619

Identifier Type: REGISTRY

Identifier Source: secondary_id

01-04-TL-475-002

Identifier Type: -

Identifier Source: org_study_id

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