Delving into the Latest Updates on WAY-256805 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

NET

Action

inhibitors

Mechanism

NET inhibitors(Norepinephrine transporter inhibitors)

Therapeutic Areas

Nervous System DiseasesOther Diseases

Active Indication-

Inactive Indication

Depressive DisorderPain

Originator Organization

Wyeth Research

Active Organization-

Inactive Organization

Neotropix, Inc.

Bristol Myers Squibb Co.EnVivo Pharmaceuticals

+ [2]

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Author: Stack, Gary P. ; Johnston, Grace H. ; Ho, Douglas M. ; Mugford, Cheryl A. ; Cohn, Stephen T. ; Vu, An T. ; Cosmi, Scott A. ; Gavrin, Lori K. ; Ye, Fei ; Leventhal, Liza ; Belardi, Justin K. ; Santilli, Arthur A. ; Leiter, Jennifer ; Smith, Valerie A. ; Trybulski, Eugene J. ; Deecher, Darlene C. ; Zhang, Yingru ; Platt, Brian ; Koury, Elizabeth J. ; Burroughs, Kevin D. ; Bray, Jenifer A. ; Mahaney, Paige E. ; Sabatucci, Joseph P. ; Rosenzweig-Lipson, Sharon J.

Further exploration of the cycloalkanol ethylamine scaffold, of which venlafaxine ( 1) is a member, was undertaken to develop novel and selective norepinephrine reuptake inhibitors (NRIs) for evaluation in a variety of predictive animal models. These efforts led to the discovery of a piperazine-containing analogue, 17g (WY-46824), that exhibited potent norepinephrine reuptake inhibition, excellent selectivity over the serotonin transporter, but no selectivity over the dopamine transporter. Synthesis and testing of a series of cyclohexanol ethylpiperazines identified ( S)-(-)- 17i (WAY-256805), a potent norepinephrine reuptake inhibitor (IC 50 = 82 nM, K i = 50 nM) that exhibited excellent selectivity over both the serotonin and dopamine transporters and was efficacious in animal models of depression, pain, and thermoregulatory dysfunction.

100 Deals associated with WAY-256805

Login to view more data

R&D Status

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Depressive Disorder	Preclinical	United States	Bristol Myers Squibb Co.	01 Jul 2008
Depressive Disorder	Preclinical	United States	Encysive Pharmaceuticals, Inc.	01 Jul 2008
Depressive Disorder	Preclinical	United States	EnVivo Pharmaceuticals	01 Jul 2008
Depressive Disorder	Preclinical	United States	Neotropix, Inc.	01 Jul 2008
Depressive Disorder	Preclinical	United States	Wyeth Research	01 Jul 2008
Pain	Preclinical	United States	EnVivo Pharmaceuticals	01 Jul 2008
Pain	Preclinical	United States	Encysive Pharmaceuticals, Inc.	01 Jul 2008
Pain	Preclinical	United States	Neotropix, Inc.	01 Jul 2008
Pain	Preclinical	United States	Bristol Myers Squibb Co.	01 Jul 2008
Pain	Preclinical	United States	Wyeth Research	01 Jul 2008