Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
Also known as MK-0859
anacetrapib · 10 trials · 7 indications
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 \[Week 52\]).
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
| Arm | Type | Description |
|---|---|---|
| Anacetrapib | EXPERIMENTAL | 100 mg tablet, oral, once daily for 24 weeks |
| Placebo | PLACEBO_COMPARATOR | Matching tablet to Anacetrapib 100 mg, oral, once daily for 24 weeks |
| Anacetrapib 100 mg | EXPERIMENTAL | - |
| Anacetrapib 25 mg | EXPERIMENTAL | - |
| 1 | EXPERIMENTAL | MK0859 10 mg + placebo |
| 2 | EXPERIMENTAL | MK0859 40 mg + placebo |
| 3 | EXPERIMENTAL | MK0859 100 mg + placebo |
| 4 | EXPERIMENTAL | MK0859 300 mg + placebo |
| 5 | EXPERIMENTAL | MK0859 10 mg + atorvastatin 10mg |
| 6 | EXPERIMENTAL | MK0859 40 mg + atorvastatin 10mg |
| 7 | EXPERIMENTAL | MK0859 100 mg + atorvastatin 10mg |
| 8 | EXPERIMENTAL | MK0859 300 mg + atorvastatin 10mg |
| 9 | PLACEBO_COMPARATOR | Placebo + atorvastatin 10mg |
| 10 | PLACEBO_COMPARATOR | Placebo |
| Part 1 - Panel A | EXPERIMENTAL | Subjects with severe renal impairment |
| Part 1 - Panel B | EXPERIMENTAL | Healthy matched control subjects |
| Part 2 - Panel C | EXPERIMENTAL | Subjects with moderate renal impairment |
| Part 2 - Panel D | EXPERIMENTAL | Healthy matched control subjects |
| Part 2 - Panel E | EXPERIMENTAL | Subjects with mild renal impairment |
| Part 2 - Panel F | EXPERIMENTAL | Healthy matched control subjects |
| Part 1 - Group 1 | EXPERIMENTAL | Moderate Hepatic Patients |
| Part 1 - Group 2 | EXPERIMENTAL | Healthy Subjects |
| Part 2 - Group 1 | EXPERIMENTAL | Mild Hepatic Patients |
| Part 2 - Group 2 | EXPERIMENTAL | Healthy Subjects |
| Panel A | EXPERIMENTAL | Period 1: atorvastatin + placebo to MK0859; Period 2: atorvastatin + MK0859 |
| Panel B | EXPERIMENTAL | Period 1: placebo to atorvastatin + placebo to MK0859; Period 2: MK0859 + placebo to atorvastatin |
| Name | Type | Description |
|---|---|---|
| Anacetrapib | DRUG | - |
| Placebo | DRUG | - |
| Placebo for anacetrapib | DRUG | - |
| Anacetrapib 100 mg | DRUG | 100 mg tablet, oral, once daily for 24 weeks |
| Placebo for anacetrapib 100 mg | DRUG | Placebo tablet, orally, once daily for 24 weeks |
| Anacetrapib 25 mg | DRUG | 25 mg tablet, oral, once daily for 24 weeks |
| Placebo for anacetrapib 25 mg | DRUG | Placebo tablet, orally, once daily for 24 weeks |
| Comparator: placebo | DRUG | Participants will receive one placebo tablet once daily for 76 weeks. |
| Comparator: atorvastatin | DRUG | atorvastatin tablet, 10mg, once daily for 8 weeks |
| Comparator: placebo to MK0859 | DRUG | Placebo to MK0859 once daily for 4 weeks. |
| Comparator: placebo to atorvastatin | DRUG | Placebo to atorvastatin once daily for 4 weeks in Period 1 and 8 weeks in Period 2. |
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...
Anacetrapib is an investigational oral small molecule developed by Merck & Company, Inc. (MRK) for cardiovascular conditions. It was studied in Phase 3 clinical trials as an add-on to ongoing statin therapy in patients with hypercholesterolemia, dyslipidemia, and heterozygous familial hypercholesterolemia. It is not an approved medicine.
Anacetrapib was developed for coronary heart disease, dyslipidemia, heterozygous familial hypercholesterolemia, hypercholesterolemia, and hyperlipoproteinemia Type II. In its Phase 3 program, it was tested as an addition to ongoing statin therapy in patients whose cholesterol remained elevated. It is investigational and has no approved use.
Anacetrapib targets CETP, cholesteryl ester transfer protein, and acts as a CETP inhibitor. By inhibiting CETP, the drug was designed to affect lipid metabolism in patients with dyslipidemia and hypercholesterolemia. It is a small molecule given orally and was studied alongside statin therapy.
Anacetrapib is developed by Merck & Company, Inc., which trades under the ticker MRK. Merck sponsored the Phase 3 clinical program for the drug, including the studies conducted in patients with hypercholesterolemia, dyslipidemia, and heterozygous familial hypercholesterolemia.
Anacetrapib is in Phase 3 development. Five clinical trials have been completed, and none are currently active. The drug remains investigational and has not been approved by the FDA for any indication. All completed studies were randomized, double-blind, and placebo-controlled.
Anacetrapib has been studied in five completed Phase 3 trials, including NCT01860729 and NCT01717300 in hypercholesterolemia, NCT01824238 in heterozygous familial hypercholesterolemia, and NCT01760460 in dyslipidemia. These trials enrolled a total of 1,623 participants and evaluated anacetrapib added to ongoing statin therapy.