Brexpiprazole
Brexpiprazole, sold under the brand name Rexulti among others, is a medication used for the treatment of major depressive disorder, schizophrenia, and agitation associated with dementia due to Alzheimer's disease. It is an atypical antipsychotic.
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| Pronunciation | /brɛkˈspɪprəzoʊl/ brek-SPIP-rə-zohl |
| Trade names | Rexulti, Rxulti, others |
| Other names | OPC-34712 |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a615046 |
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| Routes of administration | By mouth |
| Drug class | Atypical antipsychotic |
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| Bioavailability | 95% (Tmax = 4 hours) |
| Protein binding | >99% |
| Metabolism | Liver (mainly mediated by CYP3A4 and CYP2D6) |
| Elimination half-life | 91 hours (brexpiprazole), 86 hours (major metabolite) |
| Excretion | Feces (46%), urine (25%) |
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| ECHA InfoCard | 100.242.305 |
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| Formula | C25H27N3O2S |
| Molar mass | 433.57 g·mol−1 |
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The most common side effects include akathisia (a constant urge to move) and weight gain. The most common side effects among people with agitation associated with dementia due to Alzheimer's disease include headache, dizziness, urinary tract infection, nasopharyngitis, and sleep disturbances (both somnolence and insomnia).
Brexpiprazole was developed by Otsuka and Lundbeck, and is considered to be a successor to aripiprazole (Abilify). It was approved for medical use in the United States in July 2015. A generic version was approved in August 2022. Brexpiprazole is the first treatment approved by the US Food and Drug Administration (FDA) for agitation associated with dementia due to Alzheimer's disease.