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Evacetrapib

Phase 3

Cardiovascular Disease | Small molecule | Cardiovascular |Eli Lilly and Company|Trials Updated: Oct 25, 2018

Evacetrapib development status

Highest phase Phase 3 (NCT02260635)
Phase scored for LLYPhase 1
Registered trials 25 across 1 sponsor since Apr 2010

Evacetrapib target and mechanism

Molecular targetCETP
Target classInhibitor
ModalitySmall molecule

Also known as Evacetrapib Tablet, LY2484595, LY2484595 Reference Formulation (RF)

Success Probability

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Market & Valuation

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Trial Design

CONTROLLED
Total Trials5
Total Enrollment716

FDA Designations

No designations recorded

Evacetrapib clinical trials

Evacetrapib · 5 trials · 4 indications

Phase 2 2Phase 1 3
NCT01375075A Study of LY2484595 in Japanese SubjectsDyslipidemias
COMPLETED165 Analytics
NCT01105975A Study of LY2484595 in Patients With High LDL-C or Low HDL-CDyslipidemia
COMPLETED398 Analytics
PHASE2COMPLETED
A Study of LY2484595 in Japanese Subjects
DyslipidemiasUnlock trial analytics
PHASE2COMPLETED
A Study of LY2484595 in Patients With High LDL-C or Low HDL-C
DyslipidemiaUnlock trial analytics

Study Endpoints

Primary Endpoints

Percent Change From Baseline to 12 Weeks in High Density Lipoprotein Cholesterol (HDL-C) and Low Density Lipoprotein Cholesterol (LDL-C) With LY2484595 and Placebo
Baseline and Week 12

Percent change from baseline = 100\*(post-baseline assessment - baseline assessment)/baseline assessment. Higher values in the percent change from baseline represented an improvement for HDL-C and lower values in the percent change from baseline represented an improvement for LDL-C. Least Squares (LS) mean was adjusted for baseline value of the variable analyzed.

Percent Change From Baseline to 12 Weeks Endpoint in High Density Lipoprotein Cholesterol (HDL-C) With LY2484595 in Combination With Atorvastatin and Atorvastatin Monotherapy
Baseline, Week 12

Least Squares (LS) Mean values were controlled for region, baseline measurement, treatment, visit, and treatment by visit interaction.

Percent Change From Baseline to 12 Weeks Endpoint in Low Density Lipoprotein Cholesterol (LDL-C) With LY2484595 in Combination With Atorvastatin and Atorvastatin Monotherapy
Baseline, Week 12

Least Squares (LS) Mean values were controlled for region, baseline measurement, treatment, visit, and treatment by visit interaction.

Pharmacokinetics (PK) Parameters of Evacetrapib: Area Under the Concentration Versus Time Curve From Time Zero to the Last Time Point With a Measurable Concentration (AUC[0-tlast])
Single-Dose: 1,2,3,4,6,8,12,24,36,48,72,120,168 Hours Postdose; Multiple Dose: Predose, 1,2,3,4,6,8,12,24,36,48,72,120,168 hours; 10,13,17,20,24,29,36,43,50,57, and 71 Days Post Dose
PK Parameters of Evacetrapib: Maximum Concentration (Cmax)
Single-Dose: 1,2,3,4,6,8,12,24,36,48,72,120,168 Hours Postdose; Multiple Dose: Predose, 1,2,3,4,6,8,12,24,36,48,72,120,168 hours; 10,13,17,20,24,29,36,43,50,57, and 71 Days Post Dose
PK Parameters of Evacetrapib: Terminal Half-life
Single-Dose: 1,2,3,4,6,8,12,24,36,48,72,120,168 Hours Postdose; Multiple Dose: Predose, 1,2,3,4,6,8,12,24,36,48,72,120,168 hours; 10,13,17,20,24,29,36,43,50,57, and 71 Days Post Dose
Pharmacokinetics (PK): Area Under The Concentration Versus Time Curve From Time Zero To Time Tlast, Where Tlast is the Last Time Point With a Measurable Concentration (AUC[0-Tlast]) of Evacetrapib
Predose and 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, 264, 312, and 336 hours postdose
Pharmacokinetics (PK): Area Under the Concentration Time Curve From Time Zero to Infinity (AUC[0-∞]) of Evacetrapib
Predose and 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, 264, 312, and 336 hours postdose
Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Time Zero to Time Tlast (AUC0-tlast) of Evacetrapib
Predose on Day 1, and 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, 264, 312, and 336 hours after the Day 1 dose

tlast is defined as the last time point with a measurable concentration of Evacetrapib.

PK: Maximum Observed Concentration (Cmax) of Evacetrapib
Predose on Day 1, and 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, 264, 312, and 336 hours after the Day 1 dose
PK: Time of Maximum Observed Drug Concentration (Tmax) of Evacetrapib
Predose on Day 1, and 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, 264, 312, and 336 hours after the Day 1 dose

Secondary Endpoints

Percent Change From Baseline in High Density Lipoprotein Cholesterol (HDL-C) and Low Density Lipoprotein Cholesterol (LDL-C) With LY2484595 in Combination With Atorvastatin
Baseline, Weeks 2, 4, and 8
Pharmacokinetics - Area Under the Curve (AUC) of LY2484595 and Atorvastatin
Weeks 2, 4, 8, 12 (predose and postdose), and Week 16
The Number and Severity of Episodes of Rashes at Any Time From Baseline Through Week 12
Baseline through Week 12
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Study Design & Arms

AllocationRANDOMIZED
MaskingQUADRUPLE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
30 milligrams (mg) LY2484595EXPERIMENTALAdministered orally once daily for 12 weeks
100 mg LY2484595EXPERIMENTALAdministered orally once daily for 12 weeks
500 mg LY2484595EXPERIMENTALAdministered orally once daily for 12 weeks
PlaceboPLACEBO_COMPARATORAdministered orally once daily for 12 weeks
10 mg AtorvastatinACTIVE_COMPARATORAdministered orally once daily for 12 weeks
100 mg LY2484595 + 10 mg AtorvastatinEXPERIMENTALAdministered orally once daily for 12 weeks
30 milligram (mg) LY2484595 monotherapyEXPERIMENTAL -
100 mg LY2484595 monotherapyEXPERIMENTAL -
500 mg LY2484595 monotherapyEXPERIMENTAL -
20 mg Atorvastatin monotherapyACTIVE_COMPARATOR -
100 mg LY2484595 + 20 mg AtorvastatinEXPERIMENTAL -
40 mg Simvastatin monotherapyACTIVE_COMPARATOR -
100 mg LY2484595 + 40 mg SimvastatinEXPERIMENTAL -
10 mg Rosuvastatin monotherapyACTIVE_COMPARATOR -
100 mg LY2484595 + 10 mg RosuvastatinEXPERIMENTAL -
Evacetrapib: Single DoseEXPERIMENTALSingle oral dose of evacetrapib on Day 1
Evacetrapib: Multiple Dose 12 WeeksEXPERIMENTALEvacetrapib administered orally once daily beginning on Day 8 for 12 consecutive weeks
Evacetrapib: Multiple Dose 24 WeeksEXPERIMENTALEvacetrapib administered orally once daily beginning on Day 8 for 24 consecutive weeks
Evacetrapib: Multiple Dose 52 WeeksEXPERIMENTALEvacetrapib administered orally once daily beginning on Day 8 for 52 consecutive weeks
Evacetrapib (Participants With Renal Impairment)EXPERIMENTALSingle oral dose of 130 milligrams (mg) evacetrapib on Day 1 to participants with severe renal impairment.
Evacetrapib (Healthy Participants)EXPERIMENTALSingle oral dose of 130 mg evacetrapib on Day 1 to participants with normal renal function.
Evacetrapib (Healthy)EXPERIMENTALGroup 1: 130 milligrams (mg) evacetrapib administered once, orally, to participants with normal hepatic function
Evacetrapib (Hepatic, Mild)EXPERIMENTALGroup 2: 130 mg evacetrapib administered once, orally, to participants with mild hepatic impairment
Evacetrapib (Hepatic, Moderate)EXPERIMENTALGroup 3: 130 mg evacetrapib administered once, orally, to participants with moderate hepatic impairment
Evacetrapib (Hepatic, Severe)EXPERIMENTALGroup 4: 130 mg evacetrapib administered once, orally, to participants with severe hepatic impairment

Interventions

NameTypeDescription
LY2484595DRUGAdministered orally
PlaceboDRUGAdministered orally
AtorvastatinDRUGAdministered orally
SimvastatinDRUGAdministered daily by mouth for 12 weeks
RosuvastatinDRUGAdministered daily by mouth for 12 weeks
Placebo for LY2484595DRUGAdministered daily by mouth for 12 weeks
Placebo for StatinsDRUGAdministered daily by mouth for 12 weeks
EvacetrapibDRUGAdministered orally
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Eligibility Criteria

Age Range20 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites5

Inclusion Criteria: Have Low HDL-C or High LDL-C criteria as follows: Low HDL lipid criteria: * HDL-C \<45 milligrams per deciliter (mg/dL) (men) and \<50 mg/dL (women), and * LDL-C according to Japan Atherosclerosis Society (JAS) guidelines as follows: * LDL-C \<190 mg/dL (0-1 risk factors) ...

Countries:JapanUnited StatesDenmarkGermanyNetherlandsPolandUnited Kingdom
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Competitive Landscape -General Cardiovascular Diseases 67 trials (matched to "Cardiovascular Disease")

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Frequently asked questions about Evacetrapib

What is Evacetrapib?

Evacetrapib is an investigational small molecule developed by Eli Lilly and Company for cardiovascular disease and dyslipidemia. It is also known as Evacetrapib Tablet. It was studied in Phase 1 clinical trials, including a study in participants with abnormal cholesterol, and has not been approved for any indication.

What is Evacetrapib used for?

Evacetrapib was studied for cardiovascular disease, dyslipidemia, and hepatic insufficiency. Clinical trials enrolled participants with abnormal cholesterol, liver impairment, and severe renal impairment. It remains an investigational agent and is not approved for these or any other uses.

What does Evacetrapib target?

Evacetrapib targets CETP, cholesteryl ester transfer protein, and acts as a CETP inhibitor. By inhibiting CETP, the drug was designed to affect cholesterol transport and lipid levels, which is why it was studied in dyslipidemia and cardiovascular disease.

Who makes Evacetrapib?

Evacetrapib is developed by Eli Lilly and Company, which trades on the New York Stock Exchange under the ticker LLY. The compound is also referenced by the code LY2484595 in Lilly's clinical study titles.

What phase is Evacetrapib in?

Evacetrapib is in Phase 1 clinical development. All three listed studies are Phase 1 and completed, and no active trials are ongoing. The drug is investigational and has not been approved by the FDA for any indication.

What clinical trials is Evacetrapib in?

Evacetrapib has been studied in completed Phase 1 trials: NCT02168803 in participants with abnormal cholesterol, NCT01836185 in participants with hepatic impairment, and NCT01825889 in participants with severe renal impairment and healthy participants. All were conducted in the United States.

Is Evacetrapib the same as Evacetrapib Tablet?

Yes, Evacetrapib Tablet is an alternative name for Evacetrapib, the CETP inhibitor developed by Eli Lilly and Company. Both names refer to the same investigational small molecule studied in Phase 1 trials for dyslipidemia, cardiovascular disease, and hepatic insufficiency.