NCT00448890

Single-Blind, Randomised, Placebo-Controlled Two-Part Study to Evaluate Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Single Oral Escalating Doses and Repeat Doses of GSK729327 in Healthy Volunteers

Completed Phase 1 Last updated 14 October 2010

What this trial tests

Phase 1 trial testing GSK729327 in Schizophrenia in 79 participants. Completed in 1 January 2009.

Timeline

1 November 2006

Primary endpoint
1 December 2008

1 January 2009

Quick facts

Lead sponsor	GlaxoSmithKline
Phase	Phase 1
Status	Completed
Study type	INTERVENTIONAL
Allocation	randomized
Design	crossover
Masking	single
Primary purpose	treatment
Enrollment	79
Start date	1 November 2006
Primary completion	1 December 2008
Estimated completion	1 January 2009
Sites	2 locations across Germany, United Kingdom

Drugs / interventions tested

• GSK729327 — full drug profile →
• Placebo

Conditions studied

• Schizophrenia — all drugs for Schizophrenia →

Sponsor

GlaxoSmithKline — full company profile →

Who can join

Adults 18 to 55, any sex, with Schizophrenia. Healthy volunteers can join.

What's being measured

Primary outcomes are the specific endpoints the trial is designed to prove or disprove.

• Safety and tolerability endpoints of AEs; EEG; ECGs; neurological assessments; vital signs and clinical laboratory values.Part A PK parameters of Cmax,AUC,t1/2,Tmax,Ae(0-t).Part B PK parameters of Cmax,Tmax,t1/2,AUC and accumulation ratio.
  Time frame: throughout the study

Sponsor's own description

GSK729327 is a selective positive allosteric modulator of AMPA-type ionotropic glutamate receptors, exhibiting equivalent potency at all AMPA receptor subtypes. On the basis of preclinical studies it is expected that this compound will improve cognitive measures in schizophrenic patients with acceptable safety. This is a First Time in Human Study (FTIH) to assess the safety, tolerability, pharmacokinetics and preliminary pharmacodynamics of GSK729327 in healthy volunteers. The study will be conducted in 2 parts, with single doses being explored in Part A and multiple doses over 28 days in Part B. Part A will be a single blind, placebo controlled, single oral dose, dose-rising cross-over study in healthy male volunteers. Subjects will be randomized into two cohorts with an alternate panel design. There will be up to nine dosing sessions in total in order to investigate up to 7 different doses. The initial dose will be 0.25 mg and subsequent doses will be determined based on the pharmacokinetic and safety results from the previous dose. Part B will be a randomised, single blind, placebo-controlled, parallel group study of repeat oral dosing of GSK729327. Up to 4 cohorts of 15 (12 subjects receiving active dose and 3 subjects receiving placebo) healthy male and females of (non-childbearing potential) volunteers will be enrolled in Part B.

Publications & conference data

3 peer-reviewed publications reference this trial (live from Europe PMC):

1. Allosteric Modulation of Ionotropic Glutamate Receptors: An Outlook on New Therapeutic Approaches To Treat Central Nervous System Disorders.
   Brogi S, Campiani G, Brindisi M, Butini S. · · 2019 · cited 31× · PMID 30891118 · DOI 10.1021/acsmedchemlett.8b00450
2. Positive AMPA and Kainate Receptor Modulators and Their Therapeutic Potential in CNS Diseases: A Comprehensive Review.
   Vialko A, Chałupnik P, Szymańska E. · · 2025 · cited 1× · PMID 40650226 · DOI 10.3390/ijms26136450
3. Amplification of the therapeutic potential of AMPA receptor potentiators from the nootropic era to today.
   Radin DP, Lippa A, Rana S, Fuller DD, et al · · 2025 · cited 1× · PMID 39894310 · DOI 10.1016/j.pbb.2025.173967