Evaluate Safety and Efficacy of AEGR-733 and Atorvastatin vs Atorvastatin Monotherapy in Hypercholesterolemia

Following a 35-day washout of current lipid-lowering medication (if any) and adherence to a
low-fat diet, subjects will receive either atorvastatin 20 mg for 8 weeks, OR AEGR-733 2.5 mg
+ atorvastatin 20 mg for 4 weeks followed by AEGR-733 5 mg + atorvastatin 20 mg for 4
additional weeks. During the entire study, subjects will be instructed to follow a
low-fat/low cholesterol diet and limit alcohol consumption to -/< 1 drink per day.

Inclusion Criteria:

- M/F 18-70

- 0-1 risk factor, mean LDL-C -/> 160 and -/< 250 mg/dL (Visit 2 & 3)

- 2+ risk factors, mean LDL-C -/> 130 & -/< 250 mg/dL (Visit 2 & 3)

- Fasting mean TGs -/< 400 mg/dL

- Understanding and compliance of protocol

- sign consent

Exclusion Criteria:

- Females pregnant, lactating, or CBP who have not been using acceptable contraceptive
methods over previous 3 months

- Uncontrolled hypertension >180/95 at screening

- Hx of chronic renal insufficiency (serum creatinine > 2.5 mg/dL)

- Hx of liver disease or transaminases > 1.5 X ULN

- Positive for Hepatitis B or C

- Major surgery within past 3 mos

- Cardiac insufficiency defined as functional Class II-Class IV

- Hx of malignancy within previous 5 years

- Participation in another investigational drug study within past 6 wks

- Serious or unstable medical or psychological condition

- Regular alcohol use > 1 drink per day

- Regular consumers of grapefruit juice or medications known to be metabolized by CYP
3A4

- Use of other lipid-lowering meds (washout permitted)

- Acute CVD

- Diabetes Mellitus

- Fasting glucose >110 mg/dL

- BMI -/> 40 kg/m2

- Significant gastrointestinal symptoms such as IBS

- Use of fish oils, niacin, herbal wt. loss products (washout permitted)