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Simvastatin

Phase 3

Cardiovascular Disease | Small molecule | Cardiovascular |Merck & Company, Inc.|Last Updated: Feb 6, 2019

Target and mechanism

ModalitySmall molecule

Also known as Comparator: simvastatin

Success Probability

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Market & Valuation

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Trial Design

RandomizedDouble-BlindACTIVE_CONTROLLEDDMCBiomarker
Total Trials1
Total Enrollment25,673

FDA Designations

No designations recorded

Clinical trial landscape

Simvastatin · 6 trials · 9 indications

Phase 3 3Phase 2 2Phase 1 1
NCT00479388Study of Extended Release Niacin/Laropiprant on Lipids (0524A-067)Primary Hypercholesterolemia
COMPLETED1,216 Analytics
NCT00479882MK-0524B Lipid Study (MK-0524B-063)Primary Hypercholesterolemia
COMPLETED2,414 Analytics
NCT00461630Treatment of HDL to Reduce the Incidence of Vascular Events HPS2-THRIVECardiovascular Disease
COMPLETED25,673 Analytics
PHASE3COMPLETED
Study of Extended Release Niacin/Laropiprant on Lipids (0524A-067)
Primary HypercholesterolemiaUnlock trial analytics
PHASE3COMPLETED
MK-0524B Lipid Study (MK-0524B-063)
Primary HypercholesterolemiaUnlock trial analytics
PHASE3COMPLETED
Treatment of HDL to Reduce the Incidence of Vascular Events HPS2-THRIVE
Cardiovascular DiseaseUnlock trial analytics

Study Endpoints

Primary Endpoints

Percent Change From Baseline in Low Density Lipoprotein Cholesterol at Week 12
Baseline and 12 Weeks
Percentage Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C)
Baseline (Week 4 for Period II; Week 12 for Period III) and after 8 weeks of treatment during each period (Week 12 for Period II and Week 20 for Period III)

Blood samples taken at baseline (Week 4 for Period II; Week 12 for Period III) and after 8 weeks of treatment during each period to determine the LDL-C levels. The change from baseline after 8 weeks of treatment was recorded.

Major Vascular Event
During scheduled treatment period (median duration 3.9 years)

Non-fatal myocardial infarction or coronary death, non-fatal or fatal stroke, or revascularisation

Composite Score of Plaque Inflammation/Stability Gene Expression as Assayed by Ribonucleic Acid (RNA) Taqman Analysis
At time of carotid endarterectomy (after 4 to 12 weeks of dosing)

Excised carotid plaques were evaluated for the gene expression of 60 biomarkers associated with inflammation ("Hot" biomarkers) \& 25 biomarkers associated with stability ("Cold" biomarkers). Each biomarker was assayed using a quantitative polymerase chain reaction method and results were reported as a Cycle Threshold, (Ct). A Composite Score was calculated by averaging the Ct for each of the 25 "cold" genes, and subtracting the average Ct for the 60 "hot" genes. A higher composite score was associated with greater inflammation and a lower score was associated with stability (non-inflamed).

Plaque Instability Protein Composite Score
At time of carotid endarterectomy (after 4 to 12 weeks of dosing)

Each excised plaque was analyzed using an assay of 20 proteins that reflect plaque composition and inflammation. Each protein was assigned scaled signs, with a lower (negative) sign associated with plaque stability and a higher (positive) sign associated with plaque inflammation/instability. The Composite Score was the average amounts of all the 20 proteins with their associated signs. A higher Composite Score is associated with more plaque instability.

Total Cholesterol and Free Cholesterol Measured by Enzymatic Chromogenic Assay
At time of carotid endarterectomy (after 4 to 12 weeks of dosing)

Cholesterol ester was to be calculated by the following formula: Cholesterol Ester = Total Cholesterol - Free Cholesterol.

LDL cholesterol
8 weeks of treatment
Arachidonic Acid Level After 2 Weeks of Treatment
2 weeks

Arachidonic acid level (20:4n6) in the cholesterol ester lipid class. The mean reported was an adjusted mean, which was obtained from running a 2-period crossover model that had fixed treatment and period terms and a random participant term.

Secondary Endpoints

Percent Change From Baseline in High Density Lipoprotein Cholesterol at Week 12
Baseline and 12 Weeks
Percent Change From Baseline in Triglycerides at Week 12
Baseline and 12 Weeks
Percentage Change From Baseline in High-density Lipoprotein Cholesterol (HDL-C)
Baseline (Week 4 for Period II; Week 12 for Period III) and after 8 weeks of treatment during each period (Week 12 for Period II and Week 20 for Period III)
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Study Design & Arms

AllocationRANDOMIZED
MaskingDOUBLE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
1OTHEROne tablet of ER niacin/ laropiprant (1g) + one tablet of the run-in statin dose, titrating up to ER niacin/laropiprant (2g) at Week 4 for an additional 8 weeks, with no adjustments to the run-in statin dose.
2ACTIVE_COMPARATORStable dose of simvastatin or atorvastatin (20mg to 40mg) for 12 weeks.
Sequence 1: MK-0524B 1.8g/20mg→MK-0524A 2g+Simvastatin 20mgEXPERIMENTALAfter a 2-week placebo run-in, participants will receive MK-0524B (0.9 g/simvastatin 10 mg) for 4 weeks, then MK-0524B 1.8g /20 mg combination tablet for 8 weeks. Participant is then co-administered MK-0524A 2 g + simvastatin 20 mg for 8 weeks.
Sequence 2: MK-0524A 2g+Simvastatin 20mg →MK-0524B 1.8g/20mgEXPERIMENTALAfter a 2-week placebo run-in, participants will be co-administered MK-0524A 1g + simvastatin 10 mg for 4 weeks, then co-administered MK-0524A 2g +simvastatin 20 mg for 8 weeks. Participant then receives MK-0524B 1.8 g/20 mg combination tablet for 8 weeks.
Sequence 3: MK-0524B 1.8g/40mg→MK-0524A 2g+Simvastatin 40mgEXPERIMENTALAfter a 2-week placebo run-in, participants will receive MK-0524B 0.9g/40 mg combination tablet for 4 weeks, then MK-0524B 1.8g /40 mg combination tablet for 8 weeks. Participant is then co-administered MK-0524A 2 g + simvastatin 40 mg for 8 weeks.
Sequence 4: MK-0524A 2g+Simvastatin 40mg →MK-0524B 1.8g/40mgEXPERIMENTALAfter a 2-week placebo run-in, participants will be co-administered MK-0524A 1g + simvastatin 40 mg for 4 weeks, then co-administration MK-0524A 2g +simvastatin 40 mg for 8 weeks. Participant then receives MK-0524B 1.8 g/40 mg combination tablet for 8 weeks.
ER niacin/laropiprantEXPERIMENTAL1 g ER niacin plus 20 mg laropiprant per tablet. 2 tablets orally per day. With either 40 mg simvastatin tablet or ezetimibe/simvastatin (10 mg/40 mg) in single tablet taken once daily
PlaceboACTIVE_COMPARATORPlacebo (for ER niacin/laropiprant) 2 tablets orally per day. With either 40 mg simvastatin tablet orally per day or ezetimibe/simvastatin (10 mg/40 mg) in single tablet taken once daily
Statin 80 mg + Niacin extended-release (ER)EXPERIMENTALParticipants in Russia and Brasil will receive 80 mg Simvastatin + niacin. All other participants will receive 80 mg Atorvastatin + niacin.
Statin 10 mgACTIVE_COMPARATORParticipants in Russia and Brasil will receive 10 mg Simvastatin. All other participants will receive 10 mg Atorvastatin.
Simvastatin 40 mg first, then placeboEXPERIMENTALSimvastatin 40 mg tablets once daily for 2 weeks followed by placebo for 2 weeks
Placebo first, then simvastatin 40 mg once dailyPLACEBO_COMPARATORPlacebo for 2 weeks followed by simvastatin 40 mg once daily for 2 weeks

Interventions

NameTypeDescription
Comparator: simvastatinDRUGsimvastatin (20mg to 40mg) for 12 weeks.
niacin (+) laropiprantDRUGOne tablet of ER niacin/ laropiprant (1g); titrating up to ER niacin/laropiprant (2g) at Week 4 for an additional 8 weeks, with no adjustments to the run-in statin dose.
Comparator: atorvastatin calciumDRUGatorvastatin calcium (20mg to 40mg) for 12 weeks.
MK-0524ADRUGExtended-release(ER) niacin/Laropiprant (MK-0524) Combination tablet
PlaceboDRUG -
MK-0524BDRUG -
ER niacin/laropiprantDRUG -
simvastatinDRUG40 mg simvastatin tablet orally per day as background LDL-lowering treatment allocated at entry based on previous statin treatment and total cholesterol level
ezetimibe/simvastatinDRUG10 mg ezetimibe plus 40 mg simvastatin in single tablet taken once daily as background LDL-lowering treatment allocated at entry based on previous statin treatment and total cholesterol level
Atorvastatin/niacin extended-releaseDRUG80 mg tablet atorvastatin once daily, 10 mg tablet placebo to atorvastatin once daily, and niacin extended-release tablet starting at 500 mg daily and titrating to 2g daily. Treatment will be from 4 to 12 weeks.
AtorvastatinDRUG10 mg tablet atorvastatin once daily, 80 mg tablet placebo to atorvastatin once daily, and placebo to niacin extended-release tablet starting at 500 mg daily and titrating to 2g daily. Treatment will be from 4 to 12 weeks.
simvastatin 20 mg/ezetimibeDRUGsee protocol
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Eligibility Criteria

Age Range18 Years to 80 Years
SexALL
Healthy VolunteersNo

Inclusion Criteria: * Patients 18 to 80 years of age with Primary hypercholesterolemia or mixed dyslipidemia * Patients will be eligible for the study if their LDL-C values are within protocol specified range and meet other entry criteria Exclusion Criteria: * Patient whose LDL-C values are not w...

Countries:United Kingdom
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