Identification

Generic Name
ADX10059
DrugBank Accession Number
DB05070
Background

ADX10059 is a metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator (NAM). The orally available small molecule drug candidate, which is highly specific for mGluR5, was discovered at Addex in 2003. It is developed for the treatment of GERD, migraine and anxiety.

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available

Pharmacology

Indication

Investigated for use/treatment in anxiety disorders, gastroesophageal reflux disease (GERD), and migraine and cluster headaches.

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Contraindications & Blackbox Warnings
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Pharmacodynamics

Not Available

Mechanism of action

ADX10059 is a selective mGluR5 negative allosteric modulator, it may have the possibility to reduce inappropriate esophageal sphincter relaxations and prevent reflux in man. Glutamate is largely responsible for signal transmission in the neural circuit involved in migraine, and mGluR5 receptors are found at strategic points along the pathway. Inhibition of mGluR5 might therefore prevent the initiation of the migraine circuit, or interrupt it once established. mGluR5 are also found in brain regions implicated in anxiety.

TargetActionsOrganism
UMetabotropic glutamate receptor 5Not AvailableHumans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
Not Available

Categories

Drug Categories
Not Available
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
66UCJ8Z8L1
CAS number
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

References

General References
Not Available
PubChem Substance
347909927

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentGastroesophageal Reflux2
2TerminatedPreventionMigraine1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
Not Available
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

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Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Glutamate receptor activity
Specific Function
G-protein coupled receptor for glutamate. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down...
Gene Name
GRM5
Uniprot ID
P41594
Uniprot Name
Metabotropic glutamate receptor 5
Molecular Weight
132467.635 Da

Drug created at October 21, 2007 22:23 / Updated at June 12, 2020 16:52