Brexpiprazole

REXULTI

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Pronunciation: brex-PIP-ra-zoel (rex-UL-tee)

Brexpiprazole ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Brexpiprazole ballicule

Brexpiprazole REXULTI mascot mnemonic cartoon — Visual mnemonic: Brexpiprazole mascot
**“B-Rex Salty”**
Polka dots on pink → α1 blocker → syncope if titrated too quickly (hit the floor)

What it isDopamine D2 partial agonist; schizophrenia, adjunctive depression and agitation in Alzheimer dementia.

Why this oneLess akathisia than aripiprazole at equivalent efficacy, and it is the only agent approved for agitation in Alzheimer dementia.

What limits itWeight gain is greater than aripiprazole. CYP2D6 and CYP3A4 dependent; akathisia and restlessness remain.

Brexpiprazole molecular structure (skeletal formula) — Molecular structure: Brexpiprazole

FDA-approved for

schizophrenia (2015)
adjunct for depression (2015)
agitation in Alzheimer dementia (2023)

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Increased mortality in elderly patients with dementia-related psychosis; increased risk of suicidal thoughts and behaviors in children, adolescents, and young adults.

FDA dosing	Population	Start	Target	Max
Major depressive disorder (adjunctive to antidepressant)	Adults	0.5–1 mg QD	2 mg QD	3 mg QD
Schizophrenia	Adults	1 mg QD	2–4 mg QD	4 mg QD
Schizophrenia	Adolescents 13–17 yr	0.5 mg QD	2–4 mg QD	4 mg QD
Agitation associated with Alzheimer's dementia	Adults	0.5 mg QD	2 mg QD	3 mg QD

Titration Increase dosage at weekly intervals

Renal CrCl <60 mL/min: max 2 mg QD (MDD or agitation) or 3 mg QD (schizophrenia)

Hepatic Moderate-to-severe impairment (Child-Pugh ≥7): max 2 mg QD (MDD or agitation) or 3 mg QD (schizophrenia)

Instructions

Take once daily with or without food
Adjust dose for CYP2D6 poor metabolizers and with CYP inhibitors/inducers

Available strengths

tab 0.25, 0.5, 1, 2, 3, 4 mg

Cautions

Cerebrovascular reactions in elderly with dementia (stroke, TIA)
Neuroleptic malignant syndrome
Tardive dyskinesia
Metabolic changes (hyperglycemia/diabetes, dyslipidemia, weight gain)
Pathological gambling and other compulsive behaviors
Leukopenia, neutropenia, agranulocytosis
Orthostatic hypotension and syncope
Seizures
Body temperature dysregulation
Dysphagia
Cognitive and motor impairment

Adverse reactions

Weight increased
Akathisia
Somnolence
Extrapyramidal symptoms (adolescents)

Pregnancy No adequate studies; third-trimester exposure risks extrapyramidal/withdrawal symptoms in neonates; pregnancy registry available

Lactation Present in rat milk; human data lacking; weigh benefits against maternal need

Cost

Brexpiprazole (REXULTI)

What pharmacies pay · NADAC 9/30/26

Strength		#/mo	generic $/mo	brand $/mo	CostPlus
0.25 mg	tab	30 qd	—	$1,484.91	not offered
0.5 mg	tab	30 qd	—	$1,484.58	not offered
1 mg	tab	30 qd	—	$1,486.79	not offered
2 mg	tab	30 qd	—	$1,485.76	not offered
3 mg	tab	30 qd	—	$1,485.27	not offered
4 mg	tab	30 qd	—	$1,484.02	not offered

Generic entry2029 est.

⚠ BOXED WARNINGS

Increased mortality in elderly patients with dementia-related psychosis
Suicidal thoughts and behaviors in patients under 25

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4

Overdose danger2 / 4

Weight-gain liability2 / 4

Sedation liability2 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Legacy pregnancy categoryUnknown / historical label unavailable

Defining liabilityMetabolic effects, extrapyramidal symptoms/tardive dyskinesia and agent-specific QT or orthostatic risk.

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Memory aids: interaction avatars

CYP2D6 substrate

CYP3A4 substrate

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