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Brexpiprazole

Brexpiprazole structure

CAS No:
913611-97-9
Formula:
C25H27N3O2S
Chemical Name:
Brexpiprazole
Synonyms:
Brexpiprazole impurity a;CS-1678;OPC 34712; OPC34712; OPC-34712;Brexpiprazole(OPC34712);7-{4-[4-(1-Benzothiophen-4-yl)piperazin-1-yl]butoxy}quinolin-2(1H)-one;Brexpiprazole;OPC-34712;7-[4-(4-benzo[b]thien-4-yl-1-piperazinyl)butoxy]- 2(1H)-Quinolinone
Categories:
Specialty Chemicals

Description

Brexpiprazole is a N-arylpiperazine.|Brexpiprazole is a novel D2 dopamine and serotonin 1A partial agonist, called serotonin-dopamine activity modulator (SDAM), and a potent antagonist of serotonin 2A receptors, noradrenergic alpha 1B and 2C receptors. Brexpiprazole is approved for the treatment of schizophrenia, and as an adjunctive treatment for major depressive disorder (MDD). Although it failed Phase II clinical trials for ADHD, it has been designed to provide improved efficacy and tolerability (e.g., less akathisia, restlessness and/or insomnia) over established adjunctive treatments for major depressive disorder (MDD).|Brexpiprazole is an Atypical Antipsychotic.|Brexpiprazole is an atypical antipsychotic used in the treatment of schizophrenia and major depressive disorders. Brexpiprazole has been associated with a low rate of serum aminotransferase elevations during therapy, but has not been linked to instances of clinically apparent acute liver injury.

Brexpiprazole Basic Attributes

Molecular Weight：

433.57

Exact Mass：

433.57

EC Number：

811-628-7

UNII：

2J3YBM1K8C

DSSTox ID：

DTXSID40238527

Color/Form：

White to Off-White

ATC Code：

N05AX16|N - Nervous system

Characteristics

Density：

1.245±0.06 g/cm3(Predicted)

Melting Point：

179 - 181oC

Boiling Point：

675.2±55.0 °C(Predicted)

PKA：

11.22±0.70(Predicted)

Critical Temperature & Pressure：

Refrigerator

Safety Information

GHS Classification：

|Danger|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P201, P202, P260, P263, P264, P270, P273, P281, P301+P312, P308+P313, P314, P330, P391, P405, and P501|Aggregated GHS information provided by 4 companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.|Warning|H361 (100%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]|P201, P202, P281, P308+P313, P405, and P501|The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.

Toxicity

Toxicity Summary：

The most commonly observed adverse effects include: weight increase, akathisia, somnolence, tremor and nasopharyngitis. Neonates are at risk for extrapyramidal and/or withdrawal symptoms if exposed to an antipsychotic drug during the third trimester of development.

Hepatotoxicity：

Liver test abnormalities were reported to occur in ~1% of patients on long term therapy with brexpiprazole, but similar rates occurred in patients on placebo or with comparator agents. There have been no published reports of clinically apparent acute liver injury due to brexpiprazole and only rare instances have been reported with the much more frequently used aripiprazole. Thus, liver injury due to brexpiprazole must be rare, if it occurs at all.

Protein Binding：

>99% protein bound in plasma to serum albumin and α1-acid glycoprotein. Based on in vitro studies, protein binding is not affected by warfarin, diazepam, or digitoxin.

Drug Information

Drug Indication：

As an adjunctive treatment of major depressive disorder (MDD) and for treatment of schizophrenia.|FDA Label|Treatment of schizophrenia.|Treatment of schizophrenia

LiverTox Summary：

Brexpiprazole is an atypical antipsychotic used in the treatment of schizophrenia and major depressive disorders. Brexpiprazole has been associated with a low rate of serum aminotransferase elevations during therapy, but has not been linked to instances of clinically apparent acute liver injury.

Drug Classes：

Antipsychotic Agents

MeSH：

Drugs that bind to and activate dopamine receptors. (See all compounds classified as Dopamine Agonists.)|Drugs used for their effects on serotonergic systems. Among these are drugs that affect serotonin receptors, the life cycle of serotonin, and the survival of serotonergic neurons. (See all compounds classified as Serotonin Agents.)

Absorption：

Brexpiprazole reaches peak plasma concentration within 4 hours of administration, and steady state occurs within 10-12 days of dosing. Oral bioavailability is 95%, and can be administered with or without food.|Approximately 25% urinary and 46% fecal excretion. <1% and ~14% of the unchanged drug was recovered in the urine and feces, respectively.|Intravenous volume of distribution is 1.56L/kg.|19.8mL/h/kg

Metabolism/Metabolites：

Metabolized mainly by CYP3A4 and CYP2D6 enzymes into its major metabolite, DM-3411. DM-3411 is not considered to contribute any therapeutic effect.

Biological Half-Life：

Brexpiprazole and its major metabolite, DM-3411 have half lives of 91 and 96 hours respectively.

Mechanism of Action：

Although the mechanism of action of brexpiprazole in the treatment of MDD and schizophrenia is unclear, the efficacy of brexpiprazole may be attributed to partial agonist activity at serotonin 1A and dopamine D2 receptors, and antagonist activity at serotonin 2A receptors.

MeSH Entry Terms：

7-(4-(4-(1-benzothiophen-4-yl)piperazin-1-yl)butoxy)quinolin-2(1H)-one

Brexpiprazole Use and Manufacturing

Uses

Brexpiprazole is a kind of atypical antipsychotic. It is a dopamine D2 receptor partial agonist. As a novel serotonin-dopamine activity modulator, it can be used for the treatment of schizophrenia, and for the adjunctive treatment for depression. It can also provide efficacy and tolerability over established adjunctive treatments formajor depressive disorder(MDD).Recent study has also suggested it can ameliorate PCP-induced cognitive deficits in mice via 5-HT1A receptors.

Use Classification：

Human drugs -> Rxulti -> EMA Drug Category|Psycholeptics -> Human pharmacotherapeutic group|Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

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