Delving into the Latest Updates on CYM-50202 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

κ opioid receptor

Action

antagonists

Mechanism

κ opioid receptor antagonists(Kappa opioid receptor antagonists)

Therapeutic Areas

Nervous System DiseasesOther Diseases

Active Indication-

Inactive Indication

Migraine DisordersStress-related problem

Originator Organization

The Scripps Research Institute

Active Organization-

Inactive Organization

The Scripps Research Institute

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC18H26BrN3O3

InChIKeyAJYHHWYDOWTOKZ-HOTGVXAUSA-N

CAS Registry1565852-90-5

κ opioid receptor (KOR) antagonists are potential pharmacotherapies for the treatment of migraine and stress-related mood disorders including depression, anxiety, and drug abuse, thus the development of novel KOR antagonists with an improved potency/selectivity profile and medication-like duration of action has attracted the interest of the medicinal chemistry community. In this paper, we describe the discovery of 1-(6-ethyl-8-fluoro-4-methyl-3-(3-methyl-1,2,4-oxadiazol-5-yl)quinolin-2-yl)- N-(tetrahydro-2 H-pyran-4-yl)piperidin-4 amine (CYM-53093, BTRX-335140) as a potent and selective KOR antagonist, endowed with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rat pharmacodynamic experiments. Orally administered CYM-53093 showed robust efficacy in antagonizing KOR agonist-induced prolactin secretion and in tail-flick analgesia in mice. CYM-53093 exhibited a broad selectivity over a panel of off-target proteins. This compound is in phase 1 clinical trials for the treatment of neuropsychiatric disorders wherein dynorphin is thought to contribute to the underlying pathophysiology.

100 Deals associated with CYM-50202

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Migraine Disorders	Preclinical	United States	The Scripps Research Institute	01 Feb 2019
Stress-related problem	Preclinical	United States	The Scripps Research Institute	01 Feb 2019