The purpose of this research study is to see how ETC-1002 is tolerated in the body, to measure the amount of ETC-1002 in the blood, and to determine how ETC-1002 affects the level of LDL-cholesterol (bad cholesterol) and other markers of health and disease in blood and urine in patients with elevated LDL-cholesterol with or without statin intolerance.

Hypercholesterolemic patients either with or without a history of statin intolerance (1:1 ratio) will be randomized to receive once daily by mouth capsules containing either ETC-1002, ezetimibe, or ETC-1002 + ezetimibe. This study will explore the safety and efficacy of concomitant administration of ETC-1002 and ezetimibe, while also exploring the effect of ezetimibe on ETC-1002 systemic exposure.

Key Inclusion Criteria:

• Statin intolerant and statin tolerant
• Fasting LDL-C between 130 mg/dL and 220 mg/dL
• Fasting triglyceride less than or equal to 400 mg/dL
• Body mass index (BMI) between 18 and 45 kg/m2

Key Exclusion Criteria:

• History or current clinically significant cardiovascular disease
• History or current type 1 diabetes or uncontrolled type 2 diabetes
• Use of metformin or thiazolidinediones (TZD) within 3 months of screening
• History of joint symptoms difficult to differentiate from myalgia
• Uncontrolled hypothyroidism
• Liver disease or dysfunction
• Renal dysfunction or nephritic syndrome
• Gastrointestinal (GI) conditions or prior GI procedures
• HIV or AIDS
• History or malignancy
• History or drug or alcohol abuse within last 2 years
• Use of experimental or investigational drugs within 30 days of screening
• Use of ETC-1002 in a previous clinical study