Brilaroxazine

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

Identification

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Name
Brilaroxazine
Accession Number
DB09226
Type
Small Molecule
Groups
Investigational
Description

Brilaroxazine (RP5063) is an investigational atypical antipsychotic which is under development by Reviva Pharmaceuticals for the treatment of schizophrenia and schizoaffective disorder. Reviva Pharmaceuticals also intends to investigate RP5063 for the treatment of bipolar disorder, major depressive disorder, psychosis/agitation associated with Alzheimer's disease, Parkinson's disease psychosis, attention deficit hyperactivity disorder (ADD/ADHD), and autism. As of May 2015, it is in phase III clinical trials for schizophrenia.

Structure
Thumb
Synonyms
  • 6-(4-(4-(2,3-Dichlorophenyl)-piperazin-1-yl)-butoxy)-2H-benzo(b)(1,4)oxazin-3(4H)-one
  • Brilaroxazina
  • Brilaroxazine
  • Brilaroxazinum
External IDs
RP-5000 / RP-5063 / RP5000 / RP5063
Product Ingredients
IngredientUNIICASInChI Key
Brilaroxazine hydrochlorideI440YY0HX01708960-04-6GMTQOJSRMVAFIF-UHFFFAOYSA-N
Categories
UNII
X8L60BA01I
CAS number
1239729-06-6
Weight
Average: 450.36
Monoisotopic: 449.1272971
Chemical Formula
C22H25Cl2N3O3
InChI Key
PMKMNTBZJOXTJW-UHFFFAOYSA-N
InChI
InChI=1S/C22H25Cl2N3O3/c23-17-4-3-5-19(22(17)24)27-11-9-26(10-12-27)8-1-2-13-29-16-6-7-20-18(14-16)25-21(28)15-30-20/h3-7,14H,1-2,8-13,15H2,(H,25,28)
IUPAC Name
6-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy}-3,4-dihydro-2H-1,4-benzoxazin-3-one
SMILES
ClC1=C(Cl)C(=CC=C1)N1CCN(CCCCOC2=CC=C3OCC(=O)NC3=C2)CC1

Pharmacology

Indication

Investigated for the treatment of schizophrenia and schizoaffective disorder.

Pharmacodynamics
Not Available
Mechanism of action
Not Available
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
Toxicity
Not Available
Affected organisms
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.
DrugInteraction
(R)-warfarinThe risk or severity of adverse effects can be increased when Brilaroxazine is combined with (R)-warfarin.
(S)-WarfarinThe risk or severity of adverse effects can be increased when Brilaroxazine is combined with (S)-Warfarin.
2,5-Dimethoxy-4-ethylamphetamineBrilaroxazine may decrease the stimulatory activities of 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamineBrilaroxazine may decrease the stimulatory activities of 2,5-Dimethoxy-4-ethylthioamphetamine.
3,5-DinitrocatecholThe therapeutic efficacy of 3,5-Dinitrocatechol can be decreased when used in combination with RP-5063.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of adverse effects can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Brilaroxazine.
4-hydroxycoumarinThe risk or severity of adverse effects can be increased when Brilaroxazine is combined with 4-hydroxycoumarin.
4-MethoxyamphetamineThe risk or severity of adverse effects can be increased when 4-Methoxyamphetamine is combined with Brilaroxazine.
5-methoxy-N,N-dimethyltryptamineThe risk or severity of adverse effects can be increased when Brilaroxazine is combined with 5-methoxy-N,N-dimethyltryptamine.
7-NitroindazoleThe risk or severity of adverse effects can be increased when 7-Nitroindazole is combined with Brilaroxazine.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
Not Available

References

General References
Not Available
External Links
PubChem Substance
347910419
ChemSpider
64853808
BindingDB
312188
Wikipedia
RP5063

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentAcute Schizophrenia / Schizoaffective Disorders1

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 Solubility0.0339 mg/mLALOGPS
logP5.06ALOGPS
logP4.14ChemAxon
logS-4.1ALOGPS
pKa (Strongest Acidic)11.42ChemAxon
pKa (Strongest Basic)7.47ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area54.04 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity120.98 m3·mol-1ChemAxon
Polarizability47.59 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not classified

Drug created on October 22, 2015 14:46 / Updated on February 06, 2020 12:58