A Comparison Study of the Bioavailability of a Capsule Formulation of LGD-6972 to an Oral Solution Formulation

This is a single center, randomized, open-label, single dose study conducted in a 2-way
crossover design.

A total of 8 subjects will be enrolled in the study. The duration of participation for each
subject will be approximately 36 days, not including a Screening Period of up to 30 days.

Each treatment period, subjects will be admitted to the study site on Day -1 and observed
through the morning of Day 3 (48-hour post-dose assessment). Over 2 treatment periods,
subjects will receive each of the following treatments as a single dose orally, under
fasting conditions, per the randomization (4 subjects per treatment in each treatment
period:

Treatment A - 15 mg of LGD-6972 as capsules

Treatment B - 15 mg LGD-6972 as solution

Serial blood samples will be collected through 48 hours following each dose to determine the
concentration of LGD 6972 in plasma. Safety assessments will also occur during this time.
Subjects will be discharged from the study site after the 48 hour assessments and return to
the study site on Days 4, 7, and 14 for follow up procedures. Subjects will return to the
study site for the second treatment period after an additional 7 days. Subjects will be
discharged from the study after returning to the study site on Day 14 of the second
treatment period.

Inclusion Criteria:

1. Healthy, adult man or woman, 21 to 65 years of age. If the subject is a woman, she
must be surgically sterile (hysterectomy or bilateral oophorectomy or bilateral tubal
ligation), or naturally post menopausal for at least 12 months and with a follicle
stimulating hormone (FSH) level in the post-menopausal range (if not taking hormone
replacement therapy) to be considered for enrollment

2. Willing and able to provide written informed consent

3. Not diabetic and has a fasting blood glucose between 70 and 105 mg/dL, inclusive

4. In good health with no significant concomitant pathology based on medical history,
physical examination, ECG, routine laboratory tests (chemistry, hematology, lipid
profile, and urinalysis), and vital signs

5. Has a body mass index (BMI) between 18.5 kg/m2 and 30 kg/m2, inclusive, and must
weigh more than 45 kg

6. Male subjects must either have a vasectomy or agree that they and any female partners
will use 2 acceptable forms of contraception, one of which must be a condom, until 30
days after the last dose of study drug. Other acceptable forms of contraception
include hormonal contraceptives, intrauterine device, Depo Provera®, Norplant® System
Implants, bilateral tubal ligation, bilateral oophorectomy, hysterectomy, and
contraceptive sponge, foam, or jelly.

Exclusion Criteria:

1. History of drug and/or alcohol abuse within 2 years prior to screening

2. Unwilling to comply with tobacco, nicotine, alcohol, and caffeine restrictions
outlined in the protocol

3. Unwilling to comply with restrictions on strenuous exercise as specified in the
protocol

4. Has a history of clinically significant cardiovascular, pulmonary, renal, endocrine,
hepatic, neurologic, psychiatric, immunologic, hematologic, gastrointestinal
(including pancreatitis), or metabolic disease requiring medical treatment or has any
medical problems that pose an increased risk during the study or that may compromise
the integrity of the study data

5. Has liver transaminase levels (aspartate aminotransferase [AST] or alanine
aminotransferase [ALT]) 10% of the upper limit of normal (ULN), or has creatine
kinase (CK) levels 2 × ULN at screening or admission to site (Day 1). Abnormal values
at screening may be retested once

6. Has a serum triglyceride level 400 mg/dL at screening. If the triglyceride level is
between 400 mg/dL and 500 mg/dL, one retest is permitted

7. Recent history of uncontrolled high blood pressure or has systolic blood pressure 90
mmHg or 140 mmHg or diastolic blood pressure 50 mmHg or 90 mmHg at screening. One or
more retests of blood pressure within a reasonable period of time are permissible at
the discretion of the Investigator

8. Is taking prescription or non-prescription drugs other than those outlined in the
protocol

9. Has a positive screening for hepatitis B virus (HBV), hepatitis C virus (HCV), and/or
human immunodeficiency virus (HIV)

10. Woman of childbearing potential

11. Lactating or has a positive pregnancy test

12. Has donated 450 mL of blood within 56 days of admission to the investigational site
or has donated blood products within 30 days of admission.