SAGE-217, A Novel GABA_A Receptor Positive Allosteric Modulator: Clinical Pharmacology and Tolerability in Randomized Phase I Dose-Finding Studies.

ABSTRACT:

Background

SAGE-217, a novel γ-aminobutyric acid A (GABA_A) receptor positive allosteric modulator, was evaluated in phase I, double-blind, placebo-controlled, single ascending dose (SAD) and multiple ascending dose (MAD) studies to assess the safety and pharmacokinetics (PK) of SAGE-217 following administration as an oral solution.

Methods

In the SAD study, subjects were randomized 6:2 to a single dose of SAGE-217 or placebo. Doses ranged from 0.25 to 66 mg across nine cohorts. In the MAD study, subjects were randomized 9:3 and received SAGE-217 (15, 30, or 35 mg) or placebo once daily for 7 days. In both studies, PK, maximum tolerated dose (MTD; against predetermined criteria), safety, and tolerability were assessed.

Results

A total of 108 healthy voluntee

SUBMITTER: Hoffmann E 

PROVIDER: S-EPMC6994455 | biostudies-literature | 2020 Jan

REPOSITORIES: biostudies-literature