Identification

Generic Name
LY2140023
DrugBank Accession Number
DB05096
Background

LY2140023 is an investigational drug from Lilly, which is being developed as a new treatment option for schizophrenia. LY2140023 is an oral "prodrug," meaning it is devoid of intrinsic biological activity and, once administered, is metabolized to provide the active mGlu2/3 receptor agonist called LY404039. Most currently approved antipsychotic medications work by affecting the neurotransmitters dopamine or serotonin. For LY2140023, the active substance, LY404039, is thought to work by reducing the presynaptic release of another neurotransmitter, glutamate, in brain regions where mGlu2/3 receptors are expressed. Further studies are planned or are ongoing to learn more about the safety and effectiveness, including determining an optimal therapeutic dose for LY2140023.

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available

Pharmacology

Indication

Investigated for use/treatment in psychosis and schizophrenia and schizoaffective disorders.

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Contraindications & Blackbox Warnings
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Pharmacodynamics

Not Available

Mechanism of action

LY2140023 is an antipsychotic agent that is a metabotropic glutamate 2/3 receptor agonist. This agent has a new mechanism of action that is efficacious in treating schizophrenia and potentially other neuropsychiatric conditions. Once absorbed, LY2140023 is efficiently hydrolyzed to produce the active mGlu2/3 receptor agonist LY404039. LY404039 and other mGlu2/3 agonists do not directly interact with dopamine or serotonin (5-HT2A) receptors. However, 'functional' 5-HT2A receptor antagonism in the prefrontal cortex may represent a common mechanism shared by clinically effective atypical antipsychotics and mGlu2/3 receptor agonists, and may contribute to the antipsychotic actions of LY2140023.

TargetActionsOrganism
UMetabotropic glutamate receptor 2Not AvailableHumans
UMetabotropic glutamate receptor 3Not 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
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
3V85EZ3KFQ
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
347909943
Wikipedia
LY2140023

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3CompletedTreatmentSchizophrenia1
3TerminatedTreatmentSchizophrenia3
2CompletedTreatmentSchizophrenia5
2TerminatedTreatmentSchizophrenia1
2, 3TerminatedTreatmentSchizophrenia1
1CompletedBasic ScienceHealthy Subjects (HS)2
1CompletedBasic ScienceHepatic Insufficiency1
1CompletedBasic ScienceSchizophrenia1
1CompletedOtherHealthy Volunteer Study1
1CompletedOtherSchizophrenia1

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
Group ii metabotropic 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
GRM2
Uniprot ID
Q14416
Uniprot Name
Metabotropic glutamate receptor 2
Molecular Weight
95566.715 Da
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Group ii metabotropic 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
GRM3
Uniprot ID
Q14832
Uniprot Name
Metabotropic glutamate receptor 3
Molecular Weight
98878.05 Da

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