Brexpiprazole

Brexpiprazole was approved by the U.S. Food and Drug Administration (FDA) on Jul 10, 2015. It was codeveloped by Otsuka and Lundbeck, then marketed as Rexulti® by Otsuka in US.

Brexpiprazole was mediated through a combination of partial agonist activity at serotonin 5-HT1A and dopamine D2 receptors, and antagonist activity at serotonin 5-HT2A receptors. It is indicated for the treatment of schizophrenia and as an add-on treatment for major depressive disorder (MDD).

Rexulti® is available as tablet for oral use, containing 0.25 mg/0.5 mg/1 mg/2 mg/3 mg/4 mg of Brexpiprazole. For major depressive disorder, initially take 0.5 mg or 1 mg once daily, and the recommended dose is 2 mg once daily, and maximum dose is 3 mg once daily. For schizophrenia, initially take 1 mg once daily, and the recommended dose is 2 to 4 mg once daily, and maximum dose is 4 mg once daily. 

General Information

Update Date:2016-03-14

Drug Name:
Brexpiprazole
Research Code:
OPC-34712
Trade Name:
Rexulti®
MOA:
5-HT1A agonist; Dopamine D2 agonist; 5-HT2A antagonist
Indication:
Major depressive disorder (MDD); Schizophrenia
Status:
Approved
Company:
Otsuka (Originator), Lundbeck (Originator)
Sales:
$55.4 Million (Y2015)
ATC Code:
Approved Countries or Area

Update Date:2015-07-29

Approval Date Approval Type Trade Name Indication Dosage Form Strength Company Review Classification
2015-07-10 First approval Rexulti Schizophrenia,Major depressive disorder (MDD) Tablet 0.25 mg/0.5 mg/1 mg/2 mg/3 mg/4 mg Otsuka
Chemical Structure

Update Date:2015-08-27

Molecular Weight 433.57
Formula C25H27N3O2S
CAS No. 913611-97-9 (Brexpiprazole);
Chemical Name 7-{4-[4-(1-Benzothiophen-4-yl)piperazin-1-yl]butoxy}quinolin2(1H)-one
Brexpiprazole (Free Acid/Base)Parameters:
MW HD HA FRB* PSA* cLogP*
433.57 1 5 7 73.1 3.409±1.192
*:Calculated by ACD/Labs software V11.02.
Related Patents

Update Date:2015-11-17

Synthesis & Impurities

Update Date:2016-02-21


1. WO2006112464A1.


1. CN104557896A.


1. WO2013015456A1.


1. CN105061414A.

Impurity database is being updated!