Drug intelligence / Profile preview

brexpiprazole + sertraline

Development stage
Unknown
Lead developer
Otsuka Holdings
Modality
Small Molecules
Administration
Oral
01

Overview

Brexpiprazole + sertraline is an oral fixed-dose combination therapy consisting of **brexpiprazole**, an atypical antipsychotic, and **sertraline**, a selective serotonin reuptake inhibitor (SSRI), investigated for the treatment of posttraumatic stress disorder (PTSD). Brexpiprazole functions as a partial agonist at dopamine D2/D3 and serotonin 5-HT1A receptors, and as an antagonist at serotonin 5-HT2A, adrenergic alpha-1, and alpha-2 receptors. Sertraline is a selective serotonin reuptake inhibitor (SSRI) that increases serotonin levels in the central nervous system by inhibiting its reuptake. Clinical trials have found this combination provides statistically significant improvements in PTSD symptoms versus sertraline alone, with good overall tolerability and a safety profile consistent with brexpiprazole’s known effects. The combination is being developed by Otsuka and Lundbeck, who have submitted a supplemental New Drug Application (sNDA) to the FDA based on phase 3 trial data[1][2][3][4][5][6][7].

Other names
brexpiprazole + stimulant therapybrexpiprazole + sertraline
02

Targets

HTR2A (Serotonin receptor 5-HT2A)ADRA1B (α1B)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))SERT (Sodium-dependent serotonin transporter)ADRA2C (α2C)DRD2 (Dopamine D2 Receptor)DRD3 (Dopamine receptor D3)

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