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Anacetrapib

Phase 3

Heterozygous Familial Hypercholesterolemia (HeFH) | Small molecule | Metabolic |Merck & Company, Inc.|Last Updated: May 29, 2020

Success Probability

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Trial Design

RandomizedDouble-BlindPLACEBO_CONTROLLED
Total Trials1
Total Enrollment68

FDA Designations

No designations recorded

Clinical trial landscape

Anacetrapib · 10 trials · 7 indications

Phase 3 6Phase 2 1Phase 1 3
NCT01860729A Study of the Safety and Efficacy of Anacetrapib (MK-0859) Among Participants With Hypercholesterolemia When Added to Ongoing Statin Therapy (MK-0859-022)Hypercholesterolemia
COMPLETED589 Analytics
NCT01824238A Study of the Safety and Efficacy of Anacetrapib (MK-0859) When Added to Ongoing Statin Therapy in Japanese Participants With Heterozygous Familial Hypercholesterolemia (MK-0859-050)Heterozygous Familial Hypercholesterolemia (HeFH)
COMPLETED68 Analytics
NCT01760460A Study of the Safety and Efficacy of Anacetrapib (MK-0859) When Added to Ongoing Statin Therapy in Japanese Participants With Dyslipidemia (MK-0859-051 AM1)Dyslipidemia
COMPLETED307 Analytics
NCT01717300A Study of the Safety and Efficacy of Anacetrapib (MK-0859) When Added to Ongoing Statin Therapy (MK-0859-021)Hypercholesterolemia
COMPLETED459 Analytics
NCT01524289Study to Assess the Tolerability and Efficacy of Anacetrapib (MK-0859) Co-Administered With Statin in Participants With Heterozygous Familial Hypercholesterolemia (MK-0859-020)Hyperlipoproteinemia Type II
COMPLETED306 Analytics
NCT00685776Study to Assess the Tolerability and Efficacy of Anacetrapib in Patients With Coronary Heart Disease (CHD) or CHD Risk-Equivalent Disease (MK-0859-019)Coronary Heart Disease (CHD)
COMPLETED1,623 Analytics
PHASE3COMPLETED
A Study of the Safety and Efficacy of Anacetrapib (MK-0859) Among Participants With Hypercholesterolemia When Added to Ongoing Statin Therapy (MK-0859-022)
HypercholesterolemiaUnlock trial analytics
PHASE3COMPLETED
A Study of the Safety and Efficacy of Anacetrapib (MK-0859) When Added to Ongoing Statin Therapy in Japanese Participants With Heterozygous Familial Hypercholesterolemia (MK-0859-050)
Heterozygous Familial Hypercholesterolemia (HeFH)Unlock trial analytics
PHASE3COMPLETED
A Study of the Safety and Efficacy of Anacetrapib (MK-0859) When Added to Ongoing Statin Therapy in Japanese Participants With Dyslipidemia (MK-0859-051 AM1)
DyslipidemiaUnlock trial analytics
PHASE3COMPLETED
A Study of the Safety and Efficacy of Anacetrapib (MK-0859) When Added to Ongoing Statin Therapy (MK-0859-021)
HypercholesterolemiaUnlock trial analytics
PHASE3COMPLETED
Study to Assess the Tolerability and Efficacy of Anacetrapib (MK-0859) Co-Administered With Statin in Participants With Heterozygous Familial Hypercholesterolemia (MK-0859-020)
Hyperlipoproteinemia Type IIUnlock trial analytics
PHASE3COMPLETED
Study to Assess the Tolerability and Efficacy of Anacetrapib in Patients With Coronary Heart Disease (CHD) or CHD Risk-Equivalent Disease (MK-0859-019)
Coronary Heart Disease (CHD)Unlock trial analytics

Study Endpoints

Primary Endpoints

Percent Change from Baseline in LDL-C (beta-quantification [BQ] method)
Baseline and Week 24
Percent Change from Baseline in HDL-C
Baseline and Week 24
Number of Participants with Alanine Transaminase (ALT) or Aspartate Aminotransferase (AST) Consecutive Elevations ≥3x Upper Limit of Normal (ULN)
24 weeks
Number of Participants with Creatine Phosphokinase Elevations ≥10xULN with or without Muscle Symptoms
24 weeks
Number of Participants with Sodium, Chloride, or Bicarbonate Elevations >ULN or Potassium Levels <Lower Limit of Normal (LLN)
24 weeks
Number of Participants with Pre-specified Adjudicated Cardiovascular Serious Adverse Events or Death from Any Cause
24 weeks
Number of Participants with Significant Increase in Blood Pressure
24 weeks
Percentage of Participants who Experience at Least One Adverse Event (AE)
12 weeks
Number of Participants with Alanine Transaminase (ALT) or Aspartate Aminotransferase (AST) Consecutive Elevations ≥3xULN (Upper Limit of Normal)
24 Weeks
Number of Participants with Sodium, Chloride, or Bicarbonate Elevations >ULN or Potassium Levels <LLN (Lower Limit of Normal)
24 weeks
Percent Change From Baseline in Low-Density Lipoprotein Cholesterol (LDL-C) - Treatment Phase
Baseline 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 Any Adverse Event - Treatment Phase
Up 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 Phase
Up 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 With Any Serious Adverse Event - Treatment Phase
Up 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 Discontinuing Study Treatment Due to an Adverse Event - Treatment Phase
Up 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 Changes in Systolic Blood Pressure (SBP) >= 10 mm Hg
Up 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 Changes in SBP >= 15 mm Hg
Up 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 Changes in Diastolic Blood Pressure (DBP) >= 10 mm Hg
Up 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 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 Chloride Levels > ULN
Up 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 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 Bicarbonate Levels > ULN
Up 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 Consecutive Changes in Alanine Aminotransferase (ALT) and/or Aspartate Aminotransferase (AST) of >=3 x ULN
Up 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.

Percentage of Participants With Creatine Kinase (CK) Level >=10 x ULN
Up 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 CK Level >=10 x ULN With Muscle Spasms
Up 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.

Percentage of Participants Adjudicated Cardiovascular (CV) SAE
Up 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 Phase
Up 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.

Change from baseline in Low Density Lipoprotein Cholesterol
Baseline and 24 weeks
Number of participants with hepatitis-related adverse experiences
Through 88 weeks
Number of participants with Alanine Transaminase consecutive elevations greater than or equal to 3xULN (Upper Limit of Normal)
Through 88 weeks
Number of participants with Aspartate Aminotransferase consecutive elevations greater than or equal to 3xULN
Through 88 weeks
Number of participants with Creatine Phosphokinase elevations greater than or equal to 10xULN
Through 88 weeks
Number of participants with Creatine Phosphokinase elevations greater than or equal 10xULN with muscle symptoms
Through 88 weeks
Number of participants with sodium, chloride, or bicarbonate elevations greater than ULN
Through 88 weeks
Number of participants with reduction in potassium levels less than LLN (Lower Limit of Normal)
Through 88 weeks
Number of participants with myalgia
Through 88 weeks
Number of participants with rhabdomyolysis
Through 88 weeks
Number of participants with pre-specified adjudicated cardiovascular serious adverse events
Through 88 weeks
Number of participants with death from any cause
Through 88 weeks
The percent change from baseline in Low Density Lipoprotein -Cholesterol at week 8
8 weeks
Area Under the Curve (AUC(0 to infinity)) of anacetrapib
through 168 hours post dose
Difference in Production Rate (PR) and Fractional Catabolic Rate (FCR) of Low Density Lipoprotein (LDL) apoB100 following treatment with MK0859 and atorvastatin versus atorvastatin alone
12 weeks

Secondary Endpoints

Percent Change from Baseline in non-HDL-C
Baseline and Week 24
Percent Change from Baseline in Apolipoprotein B (Apo-B)
Baseline and Week 24
Percent Change from Baseline in Apolipoprotein A-I (Apo-A-I)
Baseline and Week 24
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Study Design & Arms

AllocationRANDOMIZED
MaskingDOUBLE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
AnacetrapibEXPERIMENTAL100 mg tablet, oral, once daily for 24 weeks
PlaceboPLACEBO_COMPARATORMatching tablet to Anacetrapib 100 mg, oral, once daily for 24 weeks
Anacetrapib 100 mgEXPERIMENTAL -
Anacetrapib 25 mgEXPERIMENTAL -
1EXPERIMENTALMK0859 10 mg + placebo
2EXPERIMENTALMK0859 40 mg + placebo
3EXPERIMENTALMK0859 100 mg + placebo
4EXPERIMENTALMK0859 300 mg + placebo
5EXPERIMENTALMK0859 10 mg + atorvastatin 10mg
6EXPERIMENTALMK0859 40 mg + atorvastatin 10mg
7EXPERIMENTALMK0859 100 mg + atorvastatin 10mg
8EXPERIMENTALMK0859 300 mg + atorvastatin 10mg
9PLACEBO_COMPARATORPlacebo + atorvastatin 10mg
10PLACEBO_COMPARATORPlacebo
Part 1 - Panel AEXPERIMENTALSubjects with severe renal impairment
Part 1 - Panel BEXPERIMENTALHealthy matched control subjects
Part 2 - Panel CEXPERIMENTALSubjects with moderate renal impairment
Part 2 - Panel DEXPERIMENTALHealthy matched control subjects
Part 2 - Panel EEXPERIMENTALSubjects with mild renal impairment
Part 2 - Panel FEXPERIMENTALHealthy matched control subjects
Part 1 - Group 1EXPERIMENTALModerate Hepatic Patients
Part 1 - Group 2EXPERIMENTALHealthy Subjects
Part 2 - Group 1EXPERIMENTALMild Hepatic Patients
Part 2 - Group 2EXPERIMENTALHealthy Subjects
Panel AEXPERIMENTALPeriod 1: atorvastatin + placebo to MK0859; Period 2: atorvastatin + MK0859
Panel BEXPERIMENTALPeriod 1: placebo to atorvastatin + placebo to MK0859; Period 2: MK0859 + placebo to atorvastatin

Interventions

NameTypeDescription
AnacetrapibDRUG -
PlaceboDRUG -
Placebo for anacetrapibDRUG -
Anacetrapib 100 mgDRUG100 mg tablet, oral, once daily for 24 weeks
Placebo for anacetrapib 100 mgDRUGPlacebo tablet, orally, once daily for 24 weeks
Anacetrapib 25 mgDRUG25 mg tablet, oral, once daily for 24 weeks
Placebo for anacetrapib 25 mgDRUGPlacebo tablet, orally, once daily for 24 weeks
Comparator: placeboDRUGParticipants will receive one placebo tablet once daily for 76 weeks.
Comparator: atorvastatinDRUGatorvastatin tablet, 10mg, once daily for 8 weeks
Comparator: placebo to MK0859DRUGPlacebo to MK0859 once daily for 4 weeks.
Comparator: placebo to atorvastatinDRUGPlacebo to atorvastatin once daily for 4 weeks in Period 1 and 8 weeks in Period 2.
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Eligibility Criteria

Age Range18 Years to 80 Years
SexALL
Healthy VolunteersNo

Inclusion Criteria: * If female, cannot be of reproductive potential * Has been treated with an appropriate dose of statin for at least 6 weeks * Coronary heart disease (CHD) or other atherosclerotic vascular disease with multiple risk factors (including diabetes, metabolic syndrome) and/or high LD...

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Frequently asked questions about Anacetrapib

What is Anacetrapib used for?

Anacetrapib is an investigational small molecule being developed for Coronary Heart Disease (CHD), Hypercholesterolemia, Dyslipidemia, Hyperlipoproteinemia Type II, and Heterozygous Familial Hypercholesterolemia (HeFH). It is in Phase 3 clinical development, though it is not approved and remains investigational.

Who makes Anacetrapib?

Anacetrapib is being developed by Merck & Company, Inc., traded on the New York Stock Exchange under the ticker MRK. Merck is conducting clinical trials for the drug across multiple indications in the metabolic therapeutic area.

What phase is Anacetrapib in?

Anacetrapib is in Phase 3 clinical development. It is an investigational drug and has not been approved by regulatory authorities. The drug has completed five clinical trials, with no active trials currently ongoing.

What clinical trials is Anacetrapib in?

Anacetrapib has completed five clinical trials, including NCT00977288, a Phase 2 study in Japanese patients with dyslipidemia, and NCT00990808, a Phase 1 study on lipoprotein metabolism. Other completed trials include NCT01114490 and NCT01122667, both Phase 1 pharmacokinetic studies in patients with hepatic or renal impairment.

Is Anacetrapib the same as MK0859?

Yes, Anacetrapib is also known as MK0859. Clinical trial records refer to the drug as MK0859, such as in the study titled 'A Study of Safety and Efficacy of MK0859 (Anacetrapib) in Japanese Patients With Dyslipidemia.'

What is the mechanism of Anacetrapib?

Anacetrapib is a small molecule developed by Merck for metabolic conditions. Its specific molecular target is not disclosed in the available information, so its mechanism of action is not described here.