Evaluation of ETC-1002, Ezetimibe, and the Combination in Hypercholesterolemic Patients

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