Safety and pharmacokinetic profiles of MGS0274 besylate (TS-134), a novel metabotropic glutamate 2/3 receptor agonist prodrug, in healthy subjects.

ABSTRACT:

Aims

The safety and pharmacokinetics of single and multiple doses of a novel mGlu_2/3 receptor agonist prodrug, MGS0274 besylate (TS-134), were investigated in healthy subjects.

Methods

Phase 1 single-ascending dose (5-20 mg) and multiple-ascending dose titration (5-80 mg) studies were conducted in healthy male and female subjects. Both studies were randomized, double-blinded and placebo-controlled. In one cohort of single-ascending dose study (10 mg), concentrations of MGS0008, the active compound, in the cerebrospinal fluid (CSF) were measured for up to 24 hours postdose.

Results

Following single and multiple oral administrations, MGS0274 was rapidly absorbed and extensively converted into MGS0008, which reached a maximum concentration (C_max ) i

SUBMITTER: Watanabe M 

PROVIDER: S-EPMC7576618 | biostudies-literature | 2020 Nov

REPOSITORIES: biostudies-literature