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

Identification

Generic Name
Brilaroxazine
DrugBank Accession Number
DB09226
Background

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.

Type
Small Molecule
Groups
Investigational
Structure
Weight
Average: 450.36
Monoisotopic: 449.1272971
Chemical Formula
C22H25Cl2N3O3
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

Pharmacology

Indication

Investigated for the treatment of schizophrenia and schizoaffective disorder.

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Contraindications & Blackbox Warnings
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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

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.
DrugInteraction
1,2-BenzodiazepineThe risk or severity of adverse effects can be increased when Brilaroxazine is combined with 1,2-Benzodiazepine.
AcenocoumarolThe risk or severity of adverse effects can be increased when Brilaroxazine is combined with Acenocoumarol.
AcetazolamideThe risk or severity of adverse effects can be increased when Acetazolamide is combined with Brilaroxazine.
AcetophenazineThe risk or severity of adverse effects can be increased when Acetophenazine is combined with Brilaroxazine.
AclidiniumBrilaroxazine may increase the central nervous system depressant (CNS depressant) activities of Aclidinium.
AgomelatineThe risk or severity of adverse effects can be increased when Agomelatine is combined with Brilaroxazine.
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Brilaroxazine.
AlimemazineThe risk or severity of adverse effects can be increased when Alimemazine is combined with Brilaroxazine.
AlmotriptanThe risk or severity of adverse effects can be increased when Almotriptan is combined with Brilaroxazine.
AlosetronThe risk or severity of adverse effects can be increased when Alosetron is combined with Brilaroxazine.
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Food Interactions
Not Available

Products

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Product Ingredients
IngredientUNIICASInChI Key
Brilaroxazine hydrochlorideI440YY0HX01708960-04-6GMTQOJSRMVAFIF-UHFFFAOYSA-N

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
X8L60BA01I
CAS number
1239729-06-6
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

References

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

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3RecruitingTreatmentSchizophrenia1
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

Drug created at October 22, 2015 20:46 / Updated at February 21, 2021 18:52