XenoPort, Inc. (Nasdaq: XNPT) announced today that the first subjects have been dosed in a Phase 1, randomized, double-blind, two-period crossover, food effect comparison study of XP23829 in healthy adults. The trial is designed to assess the pharmacokinetics, safety and tolerability of a single dose of XP23829 administered in both fasted and fed conditions.
Approximately 60 subjects will be assigned to one of five cohorts with each cohort receiving one of four different formulations of XP23829 or placebo. Subjects will receive a single dose of XP23829 or placebo in both a fasted and fed state in randomized order. The trial will assess the blood levels of XP23829, its active metabolite, monomethyl fumarate (MMF), and other potential metabolites. The four XP23829 formulations will include one immediate-release formulation and three extended-release formulations that are designed for possible once-a-day dosing of XP23829.
Ronald W. Barrett, Ph.D., chief executive officer of XenoPort, said, “Dosing of the first human subject with XP23829 is an important milestone as we work to develop this potential best-in-class fumarate analog. One goal of this study is to verify that XP23829 is efficiently metabolized to produce MMF in the blood. We believe that the MMF pharmacokinetic profiles produced by the different XP23829 formulations administered with and without food will be instructive for the selection of one or more formulations to take forward into future trials.”
XP23829 is currently being studied in a Phase 1 clinical trial in healthy subjects and has potential as a treatment for relapsing-remitting multiple sclerosis (RRMS) and/or psoriasis. It is a fumaric acid ester compound that is a patented prodrug of MMF. Fumaric acid ester compounds have shown immuno-modulatory and neuroprotective effects in cell-based systems and preclinical models of disease. Dimethyl fumarate (DMF), also a fumaric acid ester compound and a prodrug of MMF, has been shown to be effective in clinical trials in patients with RRMS and psoriasis. In XenoPort’s preclinical animal studies that compared molar equivalent doses of XP23829 to DMF, XP23829 demonstrated a greater degree of efficacy in animal models of both multiple sclerosis and psoriasis. Toxicology studies conducted in two species showed that XP23829 caused less stomach irritation when compared to DMF.