Safety of Larazotide Acetate in Healthy Volunteers

A Phase 1, Randomized, Double-Blind, Placebo Controlled, Multi-Dose Study to Determine the Safety, Tolerance and Pharmacokinetics of 3 Dose Levels of Larazotide Acetate (AT-1001) in Healthy Volunteers

To demonstrate the safety, tolerance and pharmacokinetics of multiple, oral doses of larazotide acetate.

CLIN1001-003 was a Phase 1, randomized, double-blind, placebo controlled multi-dose study to determine the safety, tolerance, and pharmacokinetics (including food effect) of 3 dose levels of larazotide acetate in healthy volunteers. Three (3) cohorts of 8 subjects, in which six (6) subjects in each cohort received larazotide acetate in escalating doses of 0.25 mg, 1 mg, or 4 mg TID for 10 days and two (2) subjects received placebo TID for 10 days, were studied. Subjects maintained a standard gluten-free diet. Subjects were dosed three times a day 30 minutes prior to meals except for the morning dosing on Days 1, 5, and 10. For the morning dosing on Days 1, 5, and 10 subjects, fasted overnight prior to dosing and for 2 hours post dose. Subjects were evaluated for safety (medical history, physical examination, vital signs, clinical laboratory testing, and 12-lead electrocardiograms) throughout the study. Serial blood samples were collected or pharmacokinetic determinations at baseline and 2 hours post morning dose on Days 1, 2, 5, 6 and 10.

Inclusion Criteria:

• Healthy male and female subjects
• BMI between 18 and 30.

Exclusion Criteria:

• Subjects with clinically significant abnormal clinical lab results
• Hemoglobin < 12g/dL
• Subjects with diarrhea within 3 days prior to treatment visit