Results and evaluation of a first-in-human study of RG7342, an mGlu5 positive allosteric modulator, utilizing Bayesian adaptive methods.

ABSTRACT:

Aim

The objectives of this first-in-human study were to evaluate the safety and tolerability, pharmacokinetics and pharmacodynamics, and maximum tolerated dose (MTD) of single ascending oral doses of RG7342, a positive allosteric modulator (PAM) of the metabotropic glutamate receptor 5 (mGlu5) for the treatment of schizophrenia, in healthy male subjects.

Methods

This was a single-centre, randomized, double-blind, adaptive study of 37 subjects receiving single ascending oral doses of RG7342 (ranging from 0.06-1.2 mg, n = 27) or placebo (n = 10). A modified continual reassessment method, with control for the probability of overdosing based on the occurrence of dose-limiting events (DLEs), was applied to inform the subsequent dose decisions for RG7342.

Results

DLEs consi

SUBMITTER: Sturm S 

PROVIDER: S-EPMC5809351 | biostudies-literature | 2018 Mar

REPOSITORIES: biostudies-literature