PCO-02 - Safety and Pharmacokinetics Trial

Title: Phase I, pilot study in healthy volunteers, to assess the safety and pharmacokinetics of PCO-02, which active ingredient is BPC-157, a pentadecapeptide from gastric source.

Protocol Number: BPC-1A/B-1.2

Phase: I

Population: Healthy subjects, males or females, between 18 and 35 years of age.

Number of Sites: Single center, to be performed at Hospital Angeles, Tijuana.

Duration of Study: Six months, from January 01, 2015 to Jun 30, 2015.

Duration of Subject Participation: Three weeks

Intervention description:The study consists of the oral administration of PCO-02 tablets, each containing 1mg of BPC-157 or placebo. There will be two different administration schemes, which have been labeled as Phase 1a and Phase 1b.

• Phase 1a: Single dose administration of 1, 3 or 6 tablets of PCO-02 or placebo.
• Phase 1b: Oral administration of 3 tablets of PCO-02 or placebo three times daily for 2 weeks.

Study Goals:General: To assess, in healthy volunteers, the safety and pharmacokinetics of the oral administration of PCO-02, which pharmacological active product is BPC-157.

• Primary: To assess the safety of the oral administration of BPC-157.
• Secondary: To document the pharmacokinetics of BPC-157 after oral administration.

Study Design: This is a phase-I, randomized, placebo controlled, pilot study, in which a group of 42 healthy volunteers will receive orally an active compound (PCO-02) or placebo (PCO-03) to assess safety and pharmacokinetics.

Phase 1a: There will be three cohort groups, with 14 subjects each, that will receive a single oral dose of 1, 3 or 6 tablets of PCO-02, respectively or a similar dose of placebo (PCO-03). Randomization will be at a PCO-02-to-placebo ratio of 6:1 on each group, keeping a balance between men and women among groups.

For this phase, subjects will be admitted to the hospital for 24 hours and will be kept fasting before and after the administration of the study medication. Serial blood and urine samples will be obtained to document pharmacokinetics of BPC-157 peptide and the subjects from all groups will be observed for AE in order to determine the study medication's safety. A week after, subjects will return for clinical assessment and laboratory blood work to continue monitoring for AE's.

Also, the cohort that will receive 3 tablets will receive a second dose in a similar manner but after having had a meal.

Phase 1b:This second phase will initiate only once all subjects from prior phase have completed at least one week of follow-up and that there have been no SAE's related to study medication from phase 1a.

All of subjects from phase 1a will receive a single dose of 3 tablets of PCO-02 or placebo three times daily for a period of 14 days. The assignment to active (PCO-02) or placebo (PCO-02) will be the same as per the randomization for phase 1a.

This phase will be performed on an ambulatory manner, with the subjects being required to return to the clinic at days 0, 7 and 14 for safety and pharmacokinetics assessment.

Estimated Time to Complete Enrollment: One month

Study Goals:

Primary: Safety of oral administration of PCO-02, evaluated thru the systematic monitoring for adverse events during follow-up.

Secondary: Pharmacokinetics of oral BCP-157 (Tmax, Cmax, T1/2, AUC)

Clinical Assessment During Follow- Up: During phase 1a, subjects will be admitted to the hospital for 24 hours for monitoring adverse events and serial blood and urine sampling after a single dose of PCO-02 or placebo (PCO-03). Subjects will be discharged from the hospital on the next morning and will return a week after the initial dose for clinical assessment and laboratory blood work to continue monitoring for possible AE's. The first cohort will receive 1 tablet of PCO-02 or placebo. Increasing to the next dose requires the absence of severe adverse events related to the intervention in the previous dose cohort at one week of follow-up.

If there has been no AE's related to study medication, phase 1b will be started. Initial assessment of phase 1b will be the same as the final evaluation of phase 1a. All the subjects from phase 1a will receive a single dose of 3 tablets of PCO-02 three times daily, or a similar dose of placebo (PCO-03), for a period of 2 weeks. The assignment to active compound or placebo will be the same as for phase 1a.

The subject will be required to return to the clinic at days 7 and 14 for clinical, pharmacokinetics and safety assessment, including blood and urine sampling.