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Brexpiprazole (Rexulti)

Raw research findings for this medication. Mostly single studies, not curated or confirmed robust.

About Brexpiprazole

What it is

Brexpiprazole is an antipsychotic related to aripiprazole: it partly activates dopamine D2 and serotonin 5-HT1A receptors and blocks 5-HT2A receptors. It is used for schizophrenia, as an add-on in major depression, and for agitation in Alzheimer's dementia. It is sold as Rexulti.

How genes come into it

Brexpiprazole is broken down by the liver enzymes CYP2D6 and CYP3A4. People with no working CYP2D6 copies (poor metabolizers) have clearly higher exposure, and the US drug label addresses them. DPWG has published a guideline on CYP2D6 and brexpiprazole, and the US FDA lists the pair. Only a few studies have looked at genes for this medicine.

Published guidelines

Clinical guidelines that name a gene for Brexpiprazole. They sort people into groups by the gene copies they carry.

DPWG guideline: CYP2D6. CYP2D6 activity score 0 to 6 or more. 2024.

US FDA: CYP2D6. CYP2D6 activity score 0.

US FDA: CYP2D6. CYP2D6 activity score 0. Data that Support Therapeutic Management Recommendations.

What research found

Every published finding on gene variants and Brexpiprazole. Upload your DNA file to see which of these rows apply to you.

Metabolism (5 findings)

Studies of how quickly the body processes this medication.

CYP2D6 CYP2D6*1, CYP2D6*2: CYP2D6 *2 is associated with decreased metabolism of brexpiprazole as compared to CYP2D6 *1.

CYP2D6 CYP2D6*1, CYP2D6*9, CYP2D6*10, CYP2D6*14, CYP2D6*17, CYP2D6*29, CYP2D6*41: CYP2D6 *9 +*10 + *14 + *17 + *29 + *41 is associated with decreased metabolism of brexpiprazole as compared to CYP2D6 *1.

CYP2D6 CYP2D6 intermediate metabolizer: CYP2D6 intermediate metabolizer is associated with decreased metabolism of brexpiprazole in people with Schizophrenia as compared to CYP2D6 normal metabolizer.

CYP2D6 CYP2D6 intermediate metabolizer: CYP2D6 intermediate metabolizer is associated with decreased metabolism of brexpiprazole in people with Schizophrenia as compared to CYP2D6 normal metabolizer.

Study findings and evidence levels: PharmGKB (CC BY-SA 4.0). Guidelines: CPIC and DPWG, as bundled in PharmCAT. Most studies were done mainly in people of European ancestry.

Related Drugs

More drugs from the same category

Abilify (Antipsychotics)

Antipsychotics (class) (Antipsychotics)

Bromperidol (Antipsychotics)

Not a prescribing recommendation. This page is educational information about pharmacogenomic research and clinical guidelines - it is not medical or dosing advice, and not a prediction of how any medication will work for you. Never start, stop, or change a medication or dose based on it; talk to your doctor or pharmacist, who can order clinical-grade testing if appropriate.

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Content updated September 2026.

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