Replies to post #19728 on RespireRx Pharmaceuticals Inc (fka RSPI)

[erbse24448]

Hi spyderboi,

Vorbereitung Phase 1 means preparation and testing before Phase 1

Have a nice day
Erbse

[gfp927z]

Spyderboi, Just wondering if you were aware of this Glaxo Phase 1 study using an AMPA upmodulator? (see below). They're escalating doses starting at 0.25 mg, so it sounds exceedingly potent. Any thoughts on what compound family this might be from? We know Glaxo has been collaborating with NeuroSearch for compounds, and NeuroSearch has patents for Benzothiadiazides (Servier's family), Quinoxalines, and I've seen a 2007 Glaxo patent for Pyrazoles (Lilly, Sanofi Aventis, and Organon also have some Pyrazole related patents). In the trial summary below, they say this compound exhibits 'equivalent potency at all AMPA receptor subtypes', though this doesn't seem likely. They also have as an exclusion criteria 'consumption of grapefruit juice during the trial' (perhap the compound is sensitive to acids, or some other interaction?) Thanks for any insights -

http://www.clinicaltrials.gov/ct2/show/NCT00448890?term=gsk+729327&rank=1


>>> Evaluation of Single and Repeat Doses of GSK729327 in Healthy Volunteers

This study is currently recruiting participants.
Verified by GlaxoSmithKline, April 2008

Sponsored by: GlaxoSmithKline

Information provided by: GlaxoSmithKline
ClinicalTrials.gov Identifier: NCT00448890

Purpose

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. <<<

[erbse24448]

Hi spiderboi, here a new sheet from the Cortex Pipeline Update.

I think, so it is better