A Phase 1, Single-Center, Randomized, Placebo-Controlled, Ascending Single-Dose Study of the Pharmacokinetics, Safety, and Tolerability of Oral XG005 in Healthy Volunteers

This is a single-center study. The study will investigate five ascending doses of XG005 and the approximate molar equivalent doses of Naproxen and Pregabalin for clinical relevant doses of XG005. Five XG005 treatment groups of with 10 subjects/group will be enrolled sequentially. Period 1 will be single-dose, randomized, placebo-controlled, double-blind portion of the study and designed to meet the primary study objective. Period 2 will be the single-dose, open-label portion of the study designed to meet the secondary objective of the study. The four planned dose levels of XG005 are 50, 100, 250, 500, and 1000 mg. Period 1 will be double-blind and randomized with 8 subjects (1:1 allocation ratio by gender) assigned to XG005 and 2 subjects (1:1 allocation ratio by gender) assigned to placebo. Safety Monitoring Committee (SMC; consisting of three members: Investigator, Sponsor Representative, and Independent Medical Monitor) will review available safety and tolerability data from Period 1 of the current dose level before proceeding to the subsequent dose. All subjects in the dose levels of 250, 500 and 1000 mg of XG005 in Period 1 will receive Naproxen and Pregabalin in Period 2 after a washout period. In Period 2, subjects will receive the combination of approximate molar equivalents of Naproxen and Pregabalin for their corresponding XG005 doses in Period 1. Sentinel dose participants (1 for XG005 and 1 for placebo) will be included as the first dose administered at each dose level in Period 1. Safety data and available PK data will be reviewed prior to the SMC meeting. The SMC must communicate and provide approval to dose escalate prior to dosing the next dose group. The following safety data should be reviewed at each safety meeting: vital signs, ECGs, AEs, physical examination observations, safety lab data (chemistry, hematology & urinalysis) and available PK data. Based upon the data presented, a decision will be made whether to continue with dose escalation as scheduled, to alter the next dose level, or repeat the current dose level if indicated or recommend to terminate the study for safety reasons. Meeting minutes will be documented, particularly the decision to dose escalate. This document will be signed off by the Investigator and filed in the Investigator Site File. Due to the study timelines, all safety data will be reviewed in an un-monitored state, although some of the data may have been monitored by the time of the SMC meeting. Pharmacokinetic assessments will include blood (26 collection time points with 13 timepoints/Period) samples over the course of the study. A total of approximately 200 mL of blood (130 mL for PK and 70 mL for clinical labs) will be drawn from each subject during the study. The expected duration of participation for each subject following enrollment will be approximately 15 days.