Phase I Study to Assess Safety and Pharmacokinetics of GMI-1271 in Healthy Adult Subjects

Investigators will evaluate in a single ascending dose (SAD) and multiple ascending dose
(MAD) fashion, the safety, pharmacokinetics and effect on target biomarkers of coagulation,
cell adhesion, and leukocyte and platelet activation of GMI-1271, an E-selectin antagonist,
in healthy volunteers.

Inclusion Criteria:

- Age 18-75 years

- Male or female

- Medically healthy, as defined by the absence of clinically significant screening
results (e.g. laboratory profile, medical history, electrocardiogram (ECG), physical
examination)

- BMI 18-35 kg/m2

- Voluntary consent to participate in the study

- No evidence of Lower Extremity Deep Vein Thrombosis (LE DVT) at baseline by
ultrasound

Exclusion Criteria:

- Use of any prescription, investigational, herbal, supplemental, or over the counter
medications including aspirin within 14 days (for the SAD phase) and 7 days (for the
MAD phase) prior to day 1 or unwilling/unable to refrain from the use of these
medications on days 1-8 for the SAD phase and days 1-12 of the MAD phase of the study

- Previous administration of GMI-1271

- Positive drug testing at screening and baseline or positive alcohol testing at
baseline or unwilling/unable to refrain from the use of drugs or alcohol on days 1-8
for the SAD phase and days 1-12 for the MAD phase of the study

- Pregnant or breastfeeding

- Unwilling or unable to use contraception during the time of participation in the
trial and 14 days afterwards (sexual abstinence is permissible)

- Positive HIV, Hepatitis B surface antigen or Hepatitis C antibody at screening

- Hypersensitivity or allergic reaction to compounds related to GMI-1271

- Use of moderate caffeine (≥ 300 mg/day) within 48 hours prior to dosing (day 1)

- History of bleeding disorder

- Any liver function test > 1.5 times upper limit of normal or renal insufficiency with
creatinine clearance < 30 ml/min.