This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

Generic Name
EVT 201
DrugBank Accession Number
DB05721
Background

EVT 201 is a novel partial positive allosteric modulator of the GABAA receptor complex which is being developed as a treatment for insomnia. It is being developed by Evotec Inc.

Type
Small Molecule
Groups
Investigational
Structure
Thumb
Weight
Average: 372.81
Monoisotopic: 372.1101515
Chemical Formula
C17H17ClN6O2
Synonyms
Not Available
External IDs
  • EVT 201
  • EVT-201
  • EVT201

Pharmacology

Indication

Investigated for use/treatment in insomnia.

Pharmacology
Reduce drug development failure rates
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Contraindications & Blackbox Warnings
Contraindications
Avoid life-threatening adverse drug events
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Pharmacodynamics

In two Phase I/II studies using the traffic noise model of insomnia in healthy male volunteers, EVT 201 significantly reduced "wake after sleep onset" (WASO) while significantly increasing "total sleep time" (TST) and quality of sleep with no subjective residual effects. The compound was well tolerated without significant adverse events.

Mechanism of action

EVT 201 is a partial positive allosteric modulator (pPAM) of the GABAA receptor complex and consequently works through a proven pathway in the treatment of insomnia. However, EVT 201’s partial agonist activity gives it a differentiated pre-clinical profile and mechanism of action compared to many currently marketed sleep-promoting agents.

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
Adverseeffects
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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
6J8AF7CLE4
CAS number
308239-86-3
InChI Key
JCYLWUVDHLVGER-UHFFFAOYSA-N
InChI
InChI=1S/C17H17ClN6O2/c1-22(2)8-13-20-16(21-26-13)15-12-7-23(3)17(25)14-10(18)5-4-6-11(14)24(12)9-19-15/h4-6,9H,7-8H2,1-3H3
IUPAC Name
11-chloro-5-{5-[(dimethylamino)methyl]-1,2,4-oxadiazol-3-yl}-8-methyl-2,4,8-triazatricyclo[8.4.0.0^{2,6}]tetradeca-1(10),3,5,11,13-pentaen-9-one
SMILES
CN(C)CC1=NC(=NO1)C1=C2CN(C)C(=O)C3=C(C=CC=C3Cl)N2C=N1

References

General References
Not Available
ChemSpider
8061514

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentSleep Initiation and Maintenance Disorders2

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
PropertyValueSource
Water Solubility0.267 mg/mLALOGPS
logP1.77ALOGPS
logP1.78ChemAxon
logS-3.1ALOGPS
pKa (Strongest Basic)6.81ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area80.29 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity119.64 m3·mol-1ChemAxon
Polarizability38.04 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Drug created at November 18, 2007 18:27 / Updated at May 10, 2021 12:36