This page shows what was measured, who it was measured in, and what that does not settle.
What Brexpiprazole does in the body
Depression that has not responded to an antidepressant alone, schizophrenia, and agitation in Alzheimer disease
Brexpiprazole is a close chemical relative of aripiprazole and works the same way: instead of switching the dopamine receptor off, it turns it partly on. It was engineered to turn it on less than aripiprazole does, on the theory that this would cause less of the inner restlessness that makes people stop taking aripiprazole. It also acts on two serotonin receptors, turning one partly on and blocking the other. Its own label states that nobody knows how it produces its effects and offers that combination as a possibility rather than an explanation.
What happened in people
A positive-symptom standardised mean difference of -0.17 (95% CrI -0.31 to -0.04), the weakest of 32 antipsychotics across 402 studies
✎ Source-linked record
Where this came from
A person wrote this into the record with the study named beside it. No reviewer has signed it off.
The recorded finding that sits closest to something a person would notice. Written into the record, not signed off, and it carries no population or interval.
NCT01862640 — 12-week fixed-dose trial of brexpiprazole in agitation associated with dementia due to Alzheimer disease, posted results (NCT01862640) · a recorded source, not a stored snapshot
NCT03548584 — 12-week fixed-dose trial of brexpiprazole 2 mg and 3 mg in agitation associated with dementia due to Alzheimer disease, posted results (NCT0354… · a recorded source, not a stored snapshot
The limit that matters most
The first and so far only drug approved in the United States for agitation associated with dementia due to Alzheimer disease
Where it acts
Mesolimbic and mesocortical dopamine synapses, and, for the newest indication, the same circuits in a brain already undergoing Alzheimer neurodegeneration
Kind of result
Symptoms and quality of life
Supervision
Professional supervision is normally required. A regulator classifies this substance in a way that restricts how it is supplied.
What the registries record it as
The substance registry classes this as chemical.
FDA substance registry · 2J3YBM1K8C · read 2026-08-29
Its recorded molecular formula is C25H27N3O2S, weighing 433.57.
US prescribing information · 993b584c-7fe6-4551-899f-39146c8508ac · read 2026-08-30
Where each sentence above came from
No recorded sentence describes the change this makes in a way that stands on its own. The page opens with what it is taken for instead, and the recorded explanation follows below.
Shown as the opening line on this page.
A limit recorded against this substance. Not signed off as a reviewed claim.
The four opening statements run to 132 words.
Words this page uses
Four words worth knowing first
Chosen from what this page shows, with each one explained before the word it depends on.
Stand-in result
A stand-in result is a number measured because the real result takes too long.
A picture of it, and where the picture fails
It is like judging a journey by the speedometer rather than by arriving.
Where that stops being true. Speed does predict arrival. Many stand-in results do not predict the real one.
What people get wrong. A stand-in result is often reported as the result itself.
A surrogate endpoint substituted for a clinical endpoint, valid only where the substitution has been shown to hold.
Randomisation
Randomisation means chance decides who gets which treatment.
A picture of it, and where the picture fails
It is like a coin toss deciding the groups.
Where that stops being true. A coin toss is fair once. Fairness here comes from doing it for everyone.
What people get wrong. It is thought to make groups identical. It makes them similar on average, including on things nobody measured.
Allocation of participants to arms by a chance process, so that unmeasured factors are balanced in expectation.
Absolute difference
An absolute difference is how many more people in a hundred were affected.
A picture of it, and where the picture fails
It is like counting heads in two rooms of a hundred.
Where that stops being true. Heads are easy to count. Study results carry a margin of error too.
What people get wrong. It is confused with a percentage change, which can look far larger.
The arithmetic difference in event rates between arms.
Confidence interval
A confidence interval is the range the true answer is likely to sit in.
A picture of it, and where the picture fails
It is like a weather forecast giving a range rather than one number.
Where that stops being true. A forecast range covers tomorrow. This one covers what the study could resolve.
What people get wrong. The middle number is read as the answer. A range crossing zero means no change is still possible.
An interval estimate that would contain the true parameter in a stated proportion of repeated studies.
What happened in people◇Read from sources, not yet reviewed
What was measured, goal by goal
One row for each goal a registered study measured something for. One column for each kind of thing that could be measured.
Registered studies list 21 outcome measures that RNAWiki could read. A registered study says what someone planned to measure. It does not say what they found. 0 of the matched studies tested this substance, and 0 posted a result.
There is no single score. A strong test result and a weak life result are different facts.
Goals down the side, kinds of measurement across the top. Each cell says what kind of thing was registered, not what was found.
Goal
Life outcome
What a body can do
How a person feels
A test result
A step in the body
Harms
How long
Who was studied
Mood
∅Nothing in the sources checkedNo registered study lists a life outcome for this goal.
∅Nothing in the sources checkedNo registered study lists a performance measure for this goal.
…Waiting for a reviewer2 registered symptom measure.
∅Nothing in the sources checkedNo registered study lists a test result for this goal.
∅Nothing in the sources checkedNo registered study lists a body-step measure for this goal.
—Not recordedHarms were not a registered measure for this goal.
—Not recordedNo finished study window is recorded.
…Waiting for a reviewerWho was studied is listed further down the page.
Which registered measures put each goal on this table
2 mg arm -21.6 against placebo -17.8, difference -3.77 (95% CI -7.38 to -0.17), p=0.0404; 1 mg arm -17.6, difference +0.23 (95% CI -3.40 to 3.86), p=0.9015
Repeated elsewhere
Partially Replicated
What this does not prove. Meeting one endpoint in one population does not carry to other goals or other people.
The limits of this study, and where it came from
Main limit. One of the two active arms was numerically worse than placebo. The upper confidence limit for the successful arm is -0.17, which excludes no effect by seventeen hundredths of a point on a 29-to-203 scale.
How far it carries. This study is recorded from the curated record, not from the registry match.
Form and route. Oral tablet taken once daily
Interval reported. 95% CI -7
Written into the record, not signed off as a reviewed claim.
NCT01862640 — 12-week fixed-dose trial of brexpiprazole in agitation associated with dementia due to Alzheimer disease, posted results (NCT01862640) · a recorded source, not a stored snapshot
NCT03548584 — 12-week fixed-dose trial of brexpiprazole 2 mg and 3 mg in agitation associated with dementia due to Alzheimer disease, posted results (NCT0354… · a recorded source, not a stored snapshot
NCT01922258 — 12-week flexible-dose trial of brexpiprazole in agitation associated with dementia, posted results showing p=0.1454 (NCT01922258) · a recorded source, not a stored snapshot
Change from baseline to week 12 in Cohen-Mansfield Agitation Inventory total score, in agitation associated with dementia due to Alzheimer disease
Combined 2 mg and 3 mg arm -22.6 against placebo -17.3, difference -5.32 (95% CI -8.77 to -1.87), p=0.0026
Repeated elsewhere
Partially Replicated
What this does not prove. Meeting one endpoint in one population does not carry to other goals or other people.
The limits of this study, and where it came from
Main limit. The two active amounts were pooled into a single arm for the primary comparison, so the trial does not report whether either separated from placebo on its own.
How far it carries. This study is recorded from the curated record, not from the registry match.
Form and route. Oral tablet taken once daily
Interval reported. 95% CI -8
Written into the record, not signed off as a reviewed claim.
NCT01862640 — 12-week fixed-dose trial of brexpiprazole in agitation associated with dementia due to Alzheimer disease, posted results (NCT01862640) · a recorded source, not a stored snapshot
NCT03548584 — 12-week fixed-dose trial of brexpiprazole 2 mg and 3 mg in agitation associated with dementia due to Alzheimer disease, posted results (NCT0354… · a recorded source, not a stored snapshot
NCT01922258 — 12-week flexible-dose trial of brexpiprazole in agitation associated with dementia, posted results showing p=0.1454 (NCT01922258) · a recorded source, not a stored snapshot
Change from baseline to week 12 or early termination in Cohen-Mansfield Agitation Inventory total score
-18.9 against placebo -16.5, difference -2.34 (95% CI -5.49 to 0.82), p=0.1454
Repeated elsewhere
Failed to Replicate
What this does not prove. A study that did not show an effect does not show that no effect exists anywhere.
The limits of this study, and where it came from
Main limit. This trial does not appear in the efficacy description in section 14.3 of the label, which states the indication was demonstrated in two studies.
How far it carries. This study is recorded from the curated record, not from the registry match.
Form and route. Oral tablet taken once daily
Interval reported. 95% CI -5
Written into the record, not signed off as a reviewed claim.
NCT01862640 — 12-week fixed-dose trial of brexpiprazole in agitation associated with dementia due to Alzheimer disease, posted results (NCT01862640) · a recorded source, not a stored snapshot
NCT03548584 — 12-week fixed-dose trial of brexpiprazole 2 mg and 3 mg in agitation associated with dementia due to Alzheimer disease, posted results (NCT0354… · a recorded source, not a stored snapshot
NCT01922258 — 12-week flexible-dose trial of brexpiprazole in agitation associated with dementia, posted results showing p=0.1454 (NCT01922258) · a recorded source, not a stored snapshot
Mean change in MADRS total score from the end of the eight-week antidepressant lead-in to week 14, brexpiprazole added to an antidepressant in major depressive disorder
NCT01862640 — 12-week fixed-dose trial of brexpiprazole in agitation associated with dementia due to Alzheimer disease, posted results (NCT01862640) · a recorded source, not a stored snapshot
NCT03548584 — 12-week fixed-dose trial of brexpiprazole 2 mg and 3 mg in agitation associated with dementia due to Alzheimer disease, posted results (NCT0354… · a recorded source, not a stored snapshot
NCT01922258 — 12-week flexible-dose trial of brexpiprazole in agitation associated with dementia, posted results showing p=0.1454 (NCT01922258) · a recorded source, not a stored snapshot
Change in MADRS total score with brexpiprazole or extended-release quetiapine added to an antidepressant, against placebo
✓ The study showed what it set out to show
Who was studied
NCT01727726
How many people
2182
Study design
Phase 3 randomised double-blind placebo- and active-controlled flexible-dose trial
Compared against
A dummy treatment
Kind of result
A number that stands in for health
What was found
MADRS -6.04 on brexpiprazole, -4.86 on extended-release quetiapine, -4.57 on placebo; brexpiprazole against quetiapine -1.48 (95% CI -2.56 to -0.39), p=0.0078; quetiapine against placebo -0.30 (95% CI -1.63 to 1.04), p=0.6642
Repeated elsewhere
Partially Replicated
What this does not prove. Meeting one endpoint in one population does not carry to other goals or other people.
The limits of this study, and where it came from
Main limit. The active comparator, which holds this indication itself, did not separate from placebo, which is the standard sign of a trial with weak assay sensitivity. No drug-against-placebo analysis for the primary endpoint appears among the posted analyses.
How far it carries. This study is recorded from the curated record, not from the registry match.
Form and route. Oral tablet taken once daily
Interval reported. 95% CI -2
Written into the record, not signed off as a reviewed claim.
NCT01862640 — 12-week fixed-dose trial of brexpiprazole in agitation associated with dementia due to Alzheimer disease, posted results (NCT01862640) · a recorded source, not a stored snapshot
NCT03548584 — 12-week fixed-dose trial of brexpiprazole 2 mg and 3 mg in agitation associated with dementia due to Alzheimer disease, posted results (NCT0354… · a recorded source, not a stored snapshot
NCT01922258 — 12-week flexible-dose trial of brexpiprazole in agitation associated with dementia, posted results showing p=0.1454 (NCT01922258) · a recorded source, not a stored snapshot
Change in overall symptoms against placebo in adults with multi-episode schizophrenia, with positive symptoms, negative symptoms, discontinuation, weight, prolactin and QTc as further outcomes
✓ The study showed what it set out to show
Who was studied
Huhn 32-drug network meta-analysis
How many people
53463
Study design
Network meta-analysis of 402 studies
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Brexpiprazole standardised mean difference for positive symptoms -0.17 (95% CrI -0.31 to -0.04), the weakest of the 32 drugs, against -0.69 (95% CrI -0.86 to -0.52) for amisulpride
Repeated elsewhere
Replicated
What this does not prove. Meeting one endpoint in one population does not carry to other goals or other people.
The limits of this study, and where it came from
Main limit. The authors state that confidence in the evidence was often low or very low, and that efficacy differences between antipsychotics are mostly gradual rather than discrete.
How far it carries. This study is recorded from the curated record, not from the registry match.
Form and route. Oral tablet taken once daily
Interval reported. Not recorded in this summary
Written into the record, not signed off as a reviewed claim.
NCT01862640 — 12-week fixed-dose trial of brexpiprazole in agitation associated with dementia due to Alzheimer disease, posted results (NCT01862640) · a recorded source, not a stored snapshot
NCT03548584 — 12-week fixed-dose trial of brexpiprazole 2 mg and 3 mg in agitation associated with dementia due to Alzheimer disease, posted results (NCT0354… · a recorded source, not a stored snapshot
NCT01922258 — 12-week flexible-dose trial of brexpiprazole in agitation associated with dementia, posted results showing p=0.1454 (NCT01922258) · a recorded source, not a stored snapshot
What we know
RNAWiki holds 6 written-up human studies for this substance, each with the question it asked.
How we know it
Each card names the study, the number of people and what the study set out to measure.
What this does not prove
These summaries were written by a person and have not been signed off as reviewed claims.
Why it matters
A study that failed is as informative as one that worked, and both are here.
What we still do not know
No reviewed claim exists, so no exact population, effect size or interval is published yet.
What happened in people◇Read from sources, not yet reviewed
How close this is to real life
The top step is something a person would feel or care about. The bottom is a guess from software. Filled steps are where evidence exists for this substance.
□Living longer, or avoiding a major eventNo evidence recorded. Death, a heart attack, a stroke, a hospital stay.No registered study measures this.
□What a body can do day to dayNo evidence recorded. Walking, dressing, breathing, recovering.No registered study measures this.
□Measured performanceNo evidence recorded. How much was lifted, how far was run, how fast.No registered study measures this.
■Symptoms and quality of lifeEvidence recorded. Pain, tiredness, mood, sleep, as the person rated it.4 registered measures of this kind.
■A number that stands in for healthEvidence recorded. Cholesterol, blood sugar, bone density. A stand-in, not the thing itself.3 registered measures of this kind.
■A step measured inside a personEvidence recorded. Something measured in human tissue or human cells.A human record sits on the stored organism ladder.
□AnimalsNo evidence recorded. Mice, rats, dogs. Useful for ideas, not proof about people.No animal record is stored.
■Cells in a dishEvidence recorded. Cells or chemistry on a bench, far from a whole body.Stored mechanism abstracts describe steps measured in cells or tissue.
□A guess from softwareNo evidence recorded. Nobody measured it. RNAWiki never publishes one as a finding.RNAWiki stores no prediction for this record. Software can suggest a link. RNAWiki does not publish one as a finding.
Higher on these steps means closer to something a person would feel. It does not mean better done.
What it changes in the body◇Read from sources, not yet reviewed
The path through the body
From what a person takes to what changes. A solid line is a step measured in people. A dashed line is a step nobody has measured that way.
Start
Brexpiprazole
What a person takes: Oral tablet taken once daily.
The measurement behind this step
There is no injectable and no long-acting form. The label's Limitations of Use state that it is not indicated as an as-needed treatment for agitation associated with dementia due to Alzheimer disease, which matters because as-needed use is how antipsychotics are most often given for agitation in practice. Metabolism is primarily by CYP2D6 and CYP3A4, with label adjustments for CYP2D6 poor metabolisers and for strong inhibitors of either enzyme.
Getting in
A once-daily tablet
Brexpiprazole is a tablet taken once a day. For agitation in dementia the label is explicit that it is not to be used as an as-needed treatment when someone is agitated.
╌╌Described, with no measurement named. No measurement is named for this step, so it is drawn as an unconfirmed link.
The measurement behind this step
The Limitations of Use in section 1 state that REXULTI is not indicated as an as-needed treatment for agitation associated with dementia due to Alzheimer disease. In the registration trials it was introduced over two to four weeks of stepped increases before the target amount was reached, and the endpoint was measured at twelve weeks.
NCT01862640 — 12-week fixed-dose trial of brexpiprazole in agitation associated with dementia due to Alzheimer disease, posted results (NCT01862640) · a recorded source, not a stored snapshot
NCT03548584 — 12-week fixed-dose trial of brexpiprazole 2 mg and 3 mg in agitation associated with dementia due to Alzheimer disease, posted results (NCT0354… · a recorded source, not a stored snapshot
Reaching the cell
It crosses into the brain and is cleared by two liver enzymes
The drug reaches the brain and is broken down by two liver enzymes, one of which varies substantially between people for genetic reasons.
╌╌Described, with no measurement named. No measurement is named for this step, so it is drawn as an unconfirmed link.
The measurement behind this step
Metabolism is primarily by CYP2D6 and CYP3A4, and the label carries amount adjustments for CYP2D6 poor metabolisers and for concurrent strong inhibitors of either enzyme. In an elderly population taking several other medicines, which is the population of the newest indication, that interaction surface is larger than it is in the schizophrenia population the pharmacokinetics were first described in.
NCT01862640 — 12-week fixed-dose trial of brexpiprazole in agitation associated with dementia due to Alzheimer disease, posted results (NCT01862640) · a recorded source, not a stored snapshot
NCT03548584 — 12-week fixed-dose trial of brexpiprazole 2 mg and 3 mg in agitation associated with dementia due to Alzheimer disease, posted results (NCT0354… · a recorded source, not a stored snapshot
What it acts on
It turns the dopamine receptor partly on, less than aripiprazole does
Like aripiprazole it occupies the dopamine receptor and produces a weak signal instead of blocking it entirely. It was engineered to produce a weaker signal still.
╌╌Described, with no measurement named. No measurement is named for this step, so it is drawn as an unconfirmed link.
The measurement behind this step
Partial agonism at D2 with lower intrinsic activity than aripiprazole, partial agonism at 5-HT1A and antagonism at 5-HT2A, with alpha-1B and alpha-2C antagonism. Section 12.1 states the mechanism in major depressive disorder or schizophrenia is unknown and offers this combination as a possible mediator rather than an established one.
NCT01862640 — 12-week fixed-dose trial of brexpiprazole in agitation associated with dementia due to Alzheimer disease, posted results (NCT01862640) · a recorded source, not a stored snapshot
NCT03548584 — 12-week fixed-dose trial of brexpiprazole 2 mg and 3 mg in agitation associated with dementia due to Alzheimer disease, posted results (NCT0354… · a recorded source, not a stored snapshot
The change it makes
In a brain with Alzheimer disease the same receptors are in different tissue
The newest indication gives this drug to people whose brains are progressively degenerating. The receptors it acts on are still there, but the tissue around them, and the person's ability to report a side effect, are not what they were in the schizophrenia trials.
──Measured in people. Written by a person from the study named beside the step. Not signed off as a reviewed claim.
The measurement behind this step
The agitation trials enrolled patients with probable Alzheimer disease by NINCDS-ADRDA criteria and Mini-Mental State Examination scores between 5 and 22, mean age 74, range 51 to 90. The class mortality evidence in this population, restated in section 5.1, is a death rate of about 4.5% against 2.6% on placebo over a typical ten-week trial, with most deaths cardiovascular or infectious.
NCT01862640 — 12-week fixed-dose trial of brexpiprazole in agitation associated with dementia due to Alzheimer disease, posted results (NCT01862640) · a recorded source, not a stored snapshot
NCT03548584 — 12-week fixed-dose trial of brexpiprazole 2 mg and 3 mg in agitation associated with dementia due to Alzheimer disease, posted results (NCT0354… · a recorded source, not a stored snapshot
What that does for a person
Agitation falls a few points beyond placebo, symptoms fall least of 32 drugs
In dementia agitation the drug adds three to five points on top of a seventeen-point placebo improvement. In schizophrenia it produced the smallest measured effect on hallucinations and delusions of any antipsychotic in a 32-drug comparison.
╌╌Described, with no measurement named. No measurement is named for this step, so it is drawn as an unconfirmed link.
The measurement behind this step
CMAI differences against placebo of -3.77 (95% CI -7.38 to -0.17) and -5.32 (95% CI -8.77 to -1.87) in the two positive trials. Positive symptom standardised mean difference of -0.17 (95% CrI -0.31 to -0.04) in the 32-drug network, the weakest included. MADRS difference of -1.52 points in the positive arm of the fixed-dose adjunctive depression trial.
NCT01862640 — 12-week fixed-dose trial of brexpiprazole in agitation associated with dementia due to Alzheimer disease, posted results (NCT01862640) · a recorded source, not a stored snapshot
NCT03548584 — 12-week fixed-dose trial of brexpiprazole 2 mg and 3 mg in agitation associated with dementia due to Alzheimer disease, posted results (NCT0354… · a recorded source, not a stored snapshot
No suggested links are held for this record, so nothing is hidden from this path.
What we know
The record describes 5 steps from taking it to an effect in a person.
How we know it
Each step names the study behind it in the technical detail beside it.
What this does not prove
A change inside the body is a reason to look. It is not a result in a person.
Why it matters
A reader can see exactly where the chain stops being measured in people.
What we still do not know
No reviewed claim binds any of these steps to a named population.
What it would be like to take◇Read from sources, not yet reviewed
Felt, measured, or meaningful
Three different things that get called the same word. Registered studies measured all three, and mixing them is how a blood test becomes a health claim.
Felt
Things a person could notice without a test.
montgomery asberg depression rating scale
montgomery asberg depression rating scale total
quality of life
positive and negative syndrome scale total
Measured
Things only a test, a scale or a device shows.
maximum plasma concentration
average steady state plasma concentration
area under the plasma concentration time curve
Meaningful
Things that change how a life goes, not only a number.
No registered study measured anything of this kind.
A registered study says what someone planned to measure. It does not say what they found. A number moving is not the same as a life going better. The two are shown apart here.
Felt, but not shown to help. A person notices a change. No study showed it leads anywhere good.
Measured, but not felt. A number moves. The person notices nothing. Both can be true.
Measured, but not shown to matter. A number moves in the good direction. Nobody showed that lives went better.
Matters, but takes years. The result that counts may take longer than anyone would keep watching.
Names that fit none of the three (14)
adverse events all
adverse events
safety and tolerability
treatment emergent adverse events
resting pupil diameter
serious treatment emergent adverse events
terminal phase elimination half life
visual analog scale
adverse event
treatment emergent adverse events by severity
frequency of treatment emergent adverse events
half life
clinician administered ptsd scale for dsm 5 total
safety information
These are harms, study-process measures, or names the rules did not recognise. They are shown rather than dropped.
What is missing or unclear◇Read from sources, not yet reviewed
Were people like you studied?
RNAWiki cannot tell whether a study fits you. It can show who was in it, and where the result stops carrying.
Who was studied
People similar to this profile were included.
Adults with depression that has not responded to an antidepressant, adults and adolescents with schizophrenia, and people with Alzheimer disease who are agitated. The third group is the one with the least capacity to weigh the trade being made on their behalf.
Who is missing from the studies
Which groups were under-represented in the studies has not been recorded for this substance. Pregnancy, breastfeeding, children, older adults, and people with liver or kidney conditions are commonly excluded from trials; nothing here says whether they were.
What the label states about particular groups
On pediatric, the label states: “Major Depressive Disorder Safety and effectiveness in pediatric patients with major depressive disorder have not been established.”
US prescribing information · 993b584c-7fe6-4551-899f-39146c8508ac · read 2026-08-30
On older people, the label states: “Clinical studies of the efficacy of brexpiprazole tablets did not include any patients aged 65 or older to determine whether they respond differently from younger patients.”
US prescribing information · 993b584c-7fe6-4551-899f-39146c8508ac · read 2026-08-30
On people who are pregnant, the label states: “Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to brexpiprazole tablets during pregnancy.”
US prescribing information · 993b584c-7fe6-4551-899f-39146c8508ac · read 2026-08-30
On people who are breastfeeding, the label states: “Risk Summary Lactation studies have not been conducted to assess the presence of brexpiprazole in human milk, the effects of brexpiprazole on the breastfed infant, or the effects of brexpiprazole on milk production.”
US prescribing information · 993b584c-7fe6-4551-899f-39146c8508ac · read 2026-08-30
On people with reduced liver function, the label states: “Reduce the maximum recommended dosage in patients with moderate to severe hepatic impairment (Child-Pugh score greater than or equal to 7).”
US prescribing information · 993b584c-7fe6-4551-899f-39146c8508ac · read 2026-08-30
On people with reduced kidney function, the label states: “Reduce the maximum recommended dosage in patients with moderate, severe, or end-stage renal impairment (CrCl less than 60 mL/minute).”
US prescribing information · 993b584c-7fe6-4551-899f-39146c8508ac · read 2026-08-30
Where the result stopped carrying
NCT01922258, the 270-patient flexible-dose agitation trial, returned p=0.1454 and does not appear in the label's efficacy section
The 1 mg arm of NCT01862640 was numerically worse than placebo, at p=0.9015
The 1 mg arm of the fixed-dose adjunctive depression trial did not reach significance, at p=0.0925
This is a scope explorer, not a diagnosis engine.
It shows who was studied so you can see whether people similar to you were included.
RNAWiki cannot tell whether a study fits you. It can show who was in it.
What it would be like to take◇Read from sources, not yet reviewed
Why it might seem to do nothing
A real effect and a noticed effect are different things. These are the recorded reasons the two come apart.
It was studied for a different goal
The studies measured something else entirely.
On this record: Some registered studies measured things that match no goal on this page.
It was studied in different people
The people in the studies were not much like the reader.
On this record: Which groups were under-represented in the studies has not been recorded for this substance. Pregnancy, breastfeeding, children, older adults, and people with liver or kidney conditions are commonly excluded from trials; nothing here says whether they were.
The evidence may simply be wrong
Small early studies often do not hold up.
On this record: RNAWiki has not yet published a reviewed conclusion for this use.
Other reasons RNAWiki checked and found nothing for (10)
A different form was studied
The studied form is not the form on the shelf. Nothing in this record points to this reason.
There was nothing to correct
Where a level is already normal, topping it up may change nothing. Nothing in this record points to this reason.
Something else had to happen too
In the studies it was paired with training, a diet or another treatment. Nothing in this record points to this reason.
The change is too small to feel
A real change can still sit below what a person notices. Nothing in this record points to this reason.
Day-to-day swing hides it
Sleep, food, stress and time of day move most numbers more than this would. Nothing in this record points to this reason.
Not enough time yet
The studies ran longer than the person has waited. Nothing in this record points to this reason.
It was not taken as studied
Missed days change the result, and studies count them. Nothing in this record points to this reason.
Something else changed at the same time
Two changes at once cannot be told apart afterwards. Nothing in this record points to this reason.
The product may not be what it says
Contents of a sold product are not always what the label states. Nothing in this record points to this reason.
No recorded reason
RNAWiki has nothing stored that would explain it. Nothing in this record points to this reason.
None of these is a reason to take more. Taking more is not a step this page ever suggests.
What it would be like to take◇Read from sources, not yet reviewed
What taking it involves
The recorded facts about getting hold of it and using it. Nothing here is a suggestion about what you should do.
How it is supplied
Prescription only
❝ Quoted from a source
Where this came from
Copied from a source RNAWiki stored, with the source named.
Read from the recorded approval status.
No source is stored against this line.
Form and route
Oral tablet taken once daily
✎ Source-linked record
Where this came from
A person wrote this into the record with the study named beside it. No reviewer has signed it off.
The form and route recorded on this substance.
No source is stored against this line.
Who oversees it
Professional supervision is normally required. A regulator classifies this substance in a way that restricts how it is supplied.
❝ Quoted from a source
Where this came from
Copied from a source RNAWiki stored, with the source named.
Suppression classes recorded: S6.
No source is stored against this line.
What is in the pack
There is no injectable and no long-acting form.
✎ Source-linked record
Where this came from
A person wrote this into the record with the study named beside it. No reviewer has signed it off.
Recorded notes on how this is sold. The rest of the recorded wording: The label's Limitations of Use state that it is not indicated as an as-needed treatment for agitation associated with dementia due to Alzheimer disease, which matters because as-needed use is how antipsychotics are most often given for agitation in practice. Metabolism is primarily by CYP2D6 and CYP3A4, with label adjustments for CYP2D6 poor metabolisers and for strong inhibitors of either enzyme.
No source is stored against this line.
Where it is registered
Regulatory records are listed in the technical disclosure at the foot of this page.
# Counted from records
Where this came from
A count of rows RNAWiki holds. It describes our records, not your body.
Register entries are stored per jurisdiction and shown with their dates.
No source is stored against this line.
Why people stop
Not recorded.
∅ Nothing recorded
Where this came from
RNAWiki holds nothing here and says so rather than guessing.
No record of why people stopped taking it is stored for this substance.
No source is stored against this line.
What it would be like to take◇Read from sources, not yet reviewed
What can go wrong
Sorted by where each line came from. A regulator's label and a report somebody sent in are not the same kind of fact.
·Worth asking a clinician aboutWritten into the record from the studies named on this page
The United States label carries boxed warnings for increased mortality in elderly patients with dementia-related psychosis and for suicidal thoughts and behaviours in children, adolescents and young adults. The first of these now states that the drug is not approved for dementia-related psychosis without agitation associated with dementia due to Alzheimer disease. Section 5.1 restates the class evidence: about 4.5% death on drug against about 2.6% on placebo over a typical ten-week trial, risk 1.6 to 1.7 times placebo, most deaths cardiovascular or infectious. Akathisia and weight gain are the characteristic adverse reactions. Neuroleptic malignant syndrome, tardive dyskinesia, metabolic changes, leukopenia, neutropenia and agranulocytosis, orthostatic hypotension, seizures, dysphagia and cognitive and motor impairment are all in the label.
Nobody counted how many people took this and were fine, so this cannot be turned into a rate.
NCT01862640 — 12-week fixed-dose trial of brexpiprazole in agitation associated with dementia due to Alzheimer disease, posted results (NCT01862640) · a recorded source, not a stored snapshot
NCT03548584 — 12-week fixed-dose trial of brexpiprazole 2 mg and 3 mg in agitation associated with dementia due to Alzheimer disease, posted results (NCT0354… · a recorded source, not a stored snapshot
Reports sent to a regulator
These are reports people sent to a regulator. They do not show the medicine caused the reaction.
Nobody counted how many people took the medicine and reported nothing.
The same event can be reported more than once, and many reports are incomplete.
News coverage, lawsuits and new warnings change how often people report.
A count is not a rate and not a risk.
Brexpiprazole appears in spontaneous reports to regulators. Across the 10 most-reported reaction terms, 1024 reaction mentions were counted. One report can name several reactions.
The recorded terms (10)
weight increased — 274 reaction mentions
akathisia — 166 reaction mentions
anxiety — 103 reaction mentions
restlessness — 80 reaction mentions
suicidal ideation — 76 reaction mentions
tremor — 73 reaction mentions
depression — 71 reaction mentions
feeling abnormal — 63 reaction mentions
tardive dyskinesia — 60 reaction mentions
wrong technique in product usage process — 58 reaction mentions
open-targets-adr · recorded 2026-06-24 · a recorded source, not a stored snapshot
Over a long time. No completed tested study window is recorded, so long-term effects are not established by the registry record.
Groups the studies covered thinly. Which groups were under-represented in the studies has not been recorded for this substance. Pregnancy, breastfeeding, children, older adults, and people with liver or kidney conditions are commonly excluded from trials; nothing here says whether they were.
What is missing or unclear◇Read from sources, not yet reviewed
Does the exact form matter?
Evidence belongs to the exact thing that was tested. A different salt, a different mixture or a different preparation is a different question.
The form that was studied
Oral tablet taken once daily
✎ Source-linked record
Where this came from
A person wrote this into the record with the study named beside it. No reviewer has signed it off.
The form used in the studies cited on this page.
No source is stored against this line.
What is sold
A recorded note compares this form with the others that are sold. It is kept below, word for word.
§ A fixed RNAWiki sentence
Where this came from
Wording RNAWiki always uses, not a finding about this substance.
The recorded note, unchanged: The label's Limitations of Use state that it is not indicated as an as-needed treatment for agitation associated with dementia due to Alzheimer disease, which matters because as-needed use is how antipsychotics are most often given for agitation in practice. Metabolism is primarily by CYP2D6 and CYP3A4, with label adjustments for CYP2D6 poor metabolisers and for strong inhibitors of either enzyme.
No source is stored against this line.
What is recorded as being sold
36 products list this as an active ingredient in the United States drug directory. 36 of them contain it and nothing else.
FDA National Drug Code directory · 64220-205 · read 2026-08-29
They are sold as powder and tablet, taken oral.
FDA National Drug Code directory · 64220-205 · read 2026-08-29
The regulator's established pharmacologic class for it is atypical antipsychotic [epc].
FDA National Drug Code directory · 64220-205 · read 2026-08-29
4 published labels name it as an active ingredient. 4 of them describe this substance alone, which is where its own label text on this page comes from.
US prescribing information · df891816-3fdb-4347-8bf0-c18bc40f1d70 · read 2026-08-29
Those labels are classed as human prescription drug.
US prescribing information · df891816-3fdb-4347-8bf0-c18bc40f1d70 · read 2026-08-29
Brexpiprazole is oral at 3 DOSAGE FORMS AND STRENGTHS Brexpiprazole tablets are available in 6 strengths: 0.25 mg tablets are brown colored, round, biconvex, film-coated tablet, debossed with “BX” on one side and “6” on other side. 0.5 mg table…, recorded as fda label in effect 2022-12-13 in the United States.
US prescribing information · 993b584c-7fe6-4551-899f-39146c8508ac · read 2026-08-30
Evidence carries across two names for one substance. It does not carry across a salt, a mirror form or a mixture.
What it would be like to take◇Read from sources, not yet reviewed
What you could measure
This one is decided with a clinician, so this section holds questions to ask rather than a plan to run.
Self-experiment planning is not offered for a prescription or clinician-supervised medicine. The questions below are for a clinician or pharmacist.
Questions worth asking
Which of the trials of Brexpiprazole studied people like me?
What was measured, and for how long?
Was the result a laboratory value or a health outcome?
What would we watch for, and when would we stop?
Tracking can show whether something changed for you. It cannot show what caused it.
RNAWiki records evidence. It does not say whether this substance is right for you.
What is missing or unclear◇Read from sources, not yet reviewed
Claims that go past the evidence
Things said about this substance that sound reasonable, and the exact step that is missing between the evidence and the claim.
✗Goes past the evidence
That the class mortality risk in dementia does not apply to this indication — the boxed warning was narrowed by wording, not by mortality evidence in that population
Why it sounds right. It follows from something real on this page: a body step, an animal result or a related finding.
The missing step. Nobody measured this in people for this use, or the study that did measure it did not show it.
What would change this
A study in people, for this exact use, measuring this exact thing, that a reviewer signs off.
RNAWiki has not yet published a reviewed conclusion for this use.
✗Goes past the evidence
That brexpiprazole causes less akathisia than aripiprazole — the two have never been compared in a randomised trial
Why it sounds right. It follows from something real on this page: a body step, an animal result or a related finding.
The missing step. Nobody measured this in people for this use, or the study that did measure it did not show it.
What would change this
A study in people, for this exact use, measuring this exact thing, that a reviewer signs off.
RNAWiki has not yet published a reviewed conclusion for this use.
✗Goes past the evidence
That the improvement seen by families in the agitation trials is the drug — placebo groups improved by three to five times the drug increment
Why it sounds right. It follows from something real on this page: a body step, an animal result or a related finding.
The missing step. Nobody measured this in people for this use, or the study that did measure it did not show it.
What would change this
A study in people, for this exact use, measuring this exact thing, that a reviewer signs off.
RNAWiki has not yet published a reviewed conclusion for this use.
✗Goes past the evidence
That its price reflects a clinical advantage over generic aripiprazole — no head-to-head trial of the two exists
Why it sounds right. It follows from something real on this page: a body step, an animal result or a related finding.
The missing step. Nobody measured this in people for this use, or the study that did measure it did not show it.
What would change this
A study in people, for this exact use, measuring this exact thing, that a reviewer signs off.
RNAWiki has not yet published a reviewed conclusion for this use.
What is missing or unclear◇Read from sources, not yet reviewed
What nobody knows yet
Open questions, each with why it is open and what would close it.
Missing populations
Which groups were under-represented in the studies has not been recorded.
Why it matters. Recorded by the evidence model as a gap on this record.
What would answer it
A study that measures it, and a reviewer to sign it off.
Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.
Missing long-term data
No completed tested study window is recorded.
Why it matters. Recorded by the evidence model as a gap on this record.
What would answer it
A study that measures it, and a reviewer to sign it off.
Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.
No reviewed conclusion
RNAWiki has not yet published a reviewed conclusion for this use.
Why it matters. Recorded by the evidence model as a gap on this record.
What would answer it
A study that measures it, and a reviewer to sign it off.
Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.
Missing interaction studies
No interaction was found in the registers checked. Not finding one is not the same as showing there is none.
Why it matters. Recorded by the evidence model as a gap on this record.
What would answer it
A study that measures it, and a reviewer to sign it off.
Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.
Formulation uncertainty
Several salts, forms or products of Brexpiprazole are recorded. Results from one form may not transfer to another.
Why it matters. Recorded by the evidence model as a gap on this record.
What would answer it
A study that measures it, and a reviewer to sign it off.
Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.
Mechanism not reviewed
No reviewed mechanism story exists for this substance.
Why it matters. Recorded by the evidence model as a gap on this record.
What would answer it
A study that measures it, and a reviewer to sign it off.
Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.
What happened in people◇Read from sources, not yet reviewed
Check any of this yourself
Every line above traced back to the study it came from. This is the technical layer, and the vocabulary changes here.
Every line above can be traced to the study named beside it. Follow the link and read it.
The boxed warning about deaths in dementia was rewritten around the indication
In plain words
Every antipsychotic carries a boxed warning that these drugs increase the risk of death in elderly people with dementia. Brexpiprazole now carries that warning with a clause carved out of it for the dementia indication it holds.
What was measured
That the class mortality risk in dementia does not apply to this indication — the warning's scope was narrowed by wording, and the supporting trials were designed to measure agitation over twelve weeks
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
The boxed warning states that elderly patients with dementia-related psychosis treated with antipsychotic drugs are at increased risk of death, and then: "REXULTI is not approved for the treatment of patients with dementia-related psychosis without agitation associated with dementia due to Alzheimer's disease." Section 5.1 repeats the class evidence in full — analyses of seventeen placebo-controlled trials of modal duration ten weeks, largely of atypical antipsychotics, showing a risk of death 1.6 to 1.7 times placebo, about 4.5% against about 2.6% over a typical ten-week trial, with most deaths cardiovascular or infectious — and then repeats the same carve-out sentence. The warning has not been withdrawn or contradicted; a population has been excised from its scope by wording rather than by new mortality evidence in that population. Whether the two trials supporting the indication were powered to detect a mortality difference of the size the class warning describes is a separate question from whether they showed a benefit on agitation, and only the second was their design objective.
Source
United States prescribing information for REXULTI (brexpiprazole), Boxed Warning and section 5.1, via the openFDA drug label endpoint
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
contested
Review state
Written into the record, not signed off as a reviewed claim
The placebo groups improved by about 17 points; the drug added 3.77 and 5.32
In plain words
In the two trials that worked, agitation scores fell by around 22 points on the drug and around 17 on placebo. Most of the improvement in these trials happened in people taking nothing.
What was measured
Least-squares mean CMAI difference against placebo at week 12: -3.77 (95% CI -7.38 to -0.17) and -5.32 (95% CI -8.77 to -1.87), against placebo improvements of 17.8 and 17.3 points
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
NCT01862640 enrolled 433 patients with a mean age of 74 and measured change in Cohen-Mansfield Agitation Inventory total score at week 12. The 2 mg group changed by -21.6 against -17.8 on placebo, a least-squares mean difference of -3.77 (95% CI -7.38 to -0.17), p=0.0404. NCT03548584 enrolled 345 patients and gave -22.6 on the combined 2 mg and 3 mg arm against -17.3 on placebo, difference -5.32 (95% CI -8.77 to -1.87), p=0.0026. The CMAI runs from 29 to 203. The placebo improvements of 17.8 and 17.3 points are three to five times the size of the drug increment, and the confidence interval in the first trial reaches -0.17, which is to say it excludes no benefit by seventeen hundredths of a point. Both facts are compatible with a real drug effect. Neither is compatible with describing the drug as the source of the improvement patients experience.
Source
NCT01862640 and NCT03548584 — posted results; United States prescribing information section 14.3
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
verified
Review state
Written into the record, not signed off as a reviewed claim
A third agitation trial failed, and so did one dose arm of a successful one
In plain words
Three trials tested this drug for agitation in dementia. One of them found nothing, and in another the lower amount tested was identical to placebo.
What was measured
CMAI difference against placebo: -2.34 (p=0.1454) in the flexible-dose trial and +0.23 (p=0.9015) in the 1 mg fixed-dose arm
Effect estimate
No reviewed effect estimate exists for this record.
Limits
This entry records a failure.
From the source
NCT01922258, a phase 3 twelve-week flexible-dose trial in 270 patients, gave a CMAI change of -18.9 against -16.5 on placebo, a difference of -2.34 (95% CI -5.49 to 0.82), p=0.1454. In NCT01862640, the 1 mg fixed-dose arm gave -17.6 against -17.8 on placebo, a difference of +0.23 (95% CI -3.40 to 3.86), p=0.9015 — a result numerically favouring placebo. So of four active arms across three trials and 1,048 patients, two separated and two did not, and the label describes the indication as demonstrated in two studies without the third appearing in the efficacy section. All three results are posted on ClinicalTrials.gov.
Source
NCT01922258 and NCT01862640 — posted results, Otsuka Pharmaceutical Development & Commercialization
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
caution
Review state
Written into the record, not signed off as a reviewed claim
The weakest measured effect on positive symptoms of 32 antipsychotics
In plain words
A network meta-analysis of 402 studies and 53,463 patients ranked how much each antipsychotic reduced hallucinations and delusions. Brexpiprazole came last.
What was measured
Standardised mean difference against placebo for positive symptom reduction: -0.17 (95% CrI -0.31 to -0.04), weakest of 32 drugs
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
In the Huhn network meta-analysis, standardised mean differences against placebo for reduction of positive symptoms, across 31,179 participants, varied from -0.69 (95% CrI -0.86 to -0.52) for amisulpride at the strongest end to -0.17 (95% CrI -0.31 to -0.04) for brexpiprazole at the weakest. The interval still excludes zero, so the effect is present rather than absent. The authors' overall interpretation is that efficacy differences between antipsychotics are mostly gradual rather than discrete and that differences in side-effects are more marked, and they note the confidence in the evidence was often low or very low. What is not gradual is the price: brexpiprazole is a brand-only product at about fifty dollars a tablet, and the drug at the strongest end of the same ranking, amisulpride, is a generic that the United States has never approved as an antipsychotic at all.
Written into the record, not signed off as a reviewed claim
In the depression programme the lower dose failed and the higher gave 1.52 points
In plain words
A 1,539-patient trial tested two amounts of brexpiprazole added to an antidepressant. The lower one did not beat placebo. The higher one did, by about one and a half points on a depression scale.
What was measured
MADRS difference against placebo: -1.19 (95% CI -2.58 to 0.20), p=0.0925 for the 1 mg arm and -1.52 (95% CI -2.92 to -0.13), p=0.0327 for the 3 mg arm
Effect estimate
No reviewed effect estimate exists for this record.
Limits
This entry records a failure.
From the source
NCT01360632, a phase 3 fixed-dose adjunctive trial in 1,539 patients, measured change in MADRS total score from the end of an eight-week antidepressant lead-in to week 14. The 1 mg arm changed by -7.65 against -6.45 on placebo, difference -1.19 (95% CI -2.58 to 0.20), p=0.0925. The 3 mg arm changed by -7.98, difference -1.52 (95% CI -2.92 to -0.13), p=0.0327. A 1.52-point MADRS difference on a 60-point scale is at the low end of what has ever supported an antidepressant-adjunct indication, and the lower dose arm of the same trial did not reach significance at all.
Source
NCT01360632 — phase 3 fixed-dose trial of brexpiprazole as adjunctive therapy in major depressive disorder, posted results
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
caution
Review state
Written into the record, not signed off as a reviewed claim
In one trial the approved active comparator did not beat placebo either
In plain words
A 2,182-patient trial compared brexpiprazole, extended-release quetiapine and placebo, all added to an antidepressant. Quetiapine, which already had that indication, did not separate from placebo.
What was measured
MADRS: -6.04 on brexpiprazole, -4.86 on extended-release quetiapine, -4.57 on placebo; quetiapine against placebo -0.30 (95% CI -1.63 to 1.04), p=0.6642
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
NCT01727726 was a phase 3 placebo- and active-controlled flexible-dose trial in 2,182 patients. Least-squares mean MADRS changes were -6.04 on brexpiprazole, -4.86 on extended-release quetiapine and -4.57 on placebo. The posted analyses give brexpiprazole against quetiapine as a difference of -1.48 (95% CI -2.56 to -0.39), p=0.0078, and quetiapine against placebo as -0.30 (95% CI -1.63 to 1.04), p=0.6642. A drug-against-placebo analysis for the primary endpoint is not among the posted analyses on the registry record. An active comparator that fails to separate from placebo is the classic sign of a trial with poor assay sensitivity, and in a field where placebo response is the dominant source of variance it is a reason to treat any comparison drawn inside that trial with caution — including the favourable one.
Source
NCT01727726 — phase 3 placebo- and active-controlled trial of flexible-dose brexpiprazole as adjunctive therapy in major depressive disorder, posted results
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
caution
Review state
Written into the record, not signed off as a reviewed claim
Lower intrinsic activity was the design goal, not a demonstrated outcome
In plain words
Brexpiprazole was built to turn the dopamine receptor on less strongly than aripiprazole does, so as to cause less restlessness. The molecules have never been compared in a trial.
What was measured
That brexpiprazole is better tolerated than aripiprazole — the comparison is between separate trial programmes, not between randomised arms
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
The structural change from aripiprazole is the substitution of a benzothiophene for a dichlorophenyl group on the arylpiperazine, and it lowers intrinsic activity at D2 in functional assays. That is a laboratory measurement and it is real. The clinical claim built on it is that patients experience less akathisia, and it rests on cross-trial comparison of separate registration programmes rather than on any head-to-head randomised trial. Meanwhile the same reduction in intrinsic activity is a candidate explanation for the drug placing last of 32 on positive symptom reduction. The design goal and the efficacy result may be two views of the same property, and a head-to-head trial against generic aripiprazole — which costs about one three-hundred-eightieth as much — has never been run.
This order is fixed in code and does not count clicks or time on the page.
What is not here
4 questions this page could not answer
These sections were prepared and left out because there was nothing to put in them. They are listed rather than hidden, so the gaps in this record are visible.
How long anything takes — found nothing in the sources checked.
What it may clash with — found nothing in the sources checked.
Other ways to the same goal — found nothing in the sources checked.
What changed on this page — found nothing in the sources checked.
The record as stored
The full record, for auditing
Everything above is built from what is below. This layer keeps the technical vocabulary, record identifiers and every stored row, so a reader who wants to check the page can.
The older medicine-wide conclusion held in this record
Written for a clinical reader, and about the medicine as a whole rather than about one indication, population and set of trials. RNAWiki does not treat it as a programme conclusion and no reviewer has signed it off in that form. It is here word for word because it is what the record holds.
A dopamine partial agonist designed as a lower-intrinsic-activity successor to aripiprazole, which had the weakest measured effect on positive symptoms of any drug in a 402-study network of 53,463 patients (standardised mean difference -0.17), reduced dementia agitation by 3.77 and 5.32 points beyond a placebo response of about 17 in its two positive trials while a third trial and a second dose arm failed, and became the first drug approved for agitation in Alzheimer disease by having its boxed warning about deaths in dementia rewritten around the indication.
Recorded evidence blocks (12)
Q2
What did Brexpiprazole's largest trial (2944 people) and its longest (9.6 years) measure?
2944 people in Brexpiprazole's largest registered study, 9.6 years in its longest registered window, measuring Unbound Area Under the Concentration (AUC) Time Curve Calculated to the Last Observable Concentration Brexpiprazole (AUCt,u). ClinicalTrials.gov · 2026-09-01
44 phase3, 16 phase2, 12 phase1, 6 phase4, 4 na or unstated, 1 na; NCT04569448; 2030-12; no ageing endpoint recorded. Last human test completed 2026, NCT05169268.
Interpretation These counts include studies where Brexpiprazole was a comparison treatment, a background treatment or an exposure in an observational study, and the longest window may be a planned end date. Trial roles have not yet been classified for this record.
Show the evidence
phase3
44
phase2
16
phase1
12
phase4
6
na or unstated
4
na
1
1 more recorded row
Last recorded human testNCT05169268
2026-01-31
recorded 2026-09-01 · last checked 2026-09-04
Q3
Brexpiprazole was tested only in human — what did it show?
Interpretation Unbound Area Under the Concentration (AUC) Time Curve Calculated to the Last Observable Concentration Brexpiprazole (AUCt,u). — the recorded outcome words.
Show the evidence
humanNCT01289080
biomarker; Unbound Area Under the Concentration (AUC) Time Curve Calculated to the Last Observable Concentration Brexpiprazole (AUCt,u).; 79
recorded 2026-09-01 · last checked 2026-09-04
Q4
8 of Brexpiprazole's trials stopped: safety, accrual/recruitment, funding/business, other?
safety (2), accrual/recruitment (4), funding/business (1) and other (1): Brexpiprazole's stop wording, clustered. ClinicalTrials.gov · 2026-09-01
"The study was terminated because of recruitment challenges"; 8 of 79 registered studies
Show the evidence
Trial
NCT01837797
terminated; "The study was terminated because of recruitment challenges"
NCT01944969
terminated; "The study was terminated because the lead-in study (14571A) in elderly was terminated; see Detailed Description."
NCT01987960
terminated; "The study was terminated due to challenges with patient eligibility; the decision to terminate was not based on any safety concerns"
NCT02212613
withdrawn; "Low enrollment"
NCT02758067
withdrawn; "This study was withdrawn for administrative reasons. There were no safety concerns."
NCT02934932
terminated; "Terminated due to slow enrollment."
2 further recorded trials
NCT03487198
terminated; "In consideration of the progress now and the expected enrollment in the next few years,the NDA will not be acquired before the patent went out."
NCT05504486
withdrawn; "Sponsor strategic decision"
recorded 2026-09-01 · last checked 2026-09-04
Q5
Human studies of Brexpiprazole used OPC-34712 (4mg) — over how long?
Number of drinks consumed in natural environment; Change from Baseline Depressive Symptoms as Assessed by MADRS at 8 weeks; latest 2030-12
Show the evidence
Trial
NCT04066192
"Brexpiprazole in Alcohol Use Disorder"; n 250; "Number of drinks consumed in natural environment"; 2026-08-31
NCT04569448
"Brexpiprazole Treatment for Bipolar I Depression"; n 58; "Change from Baseline Depressive Symptoms as Assessed by MADRS at 8 weeks"; 2030-12
NCT05017311
"Optimized Predictive Treatment In Medications for Unipolar Major Depression (OPTIMUM-D)"; n 400; "Change in Montgomery Asberg Depression Rating Scale (MADRS) scores from baseline"; 2029-04-30
NCT05962216
"Real-life Assessment of Brexpiprazole (Rexulti) in Schizophrenia and in Depressive Disorders"; n 40; "Change in Brief Psychiatric Rating Scale-24 in 6 months"; 2026-12-31
NCT06875986
"REXULTI Drug General Use-results Survey (Excessive Motor Activity or Physically/Verbally Aggressive Behavior Due to Rapid Changes in Mood, Irritability, and/or Outbursts Associated With Dementia Due to Alzheimer's Disease)"; n 200; "Safety Information (Adverse Event)"; 2028-09-23
NCT07715253
"Longitudinal PET Imaging of Antipsychotic Binding to the Dopamine-3 Receptor in Schizophrenia"; n 100; "Acute D2 and D3 Receptor Occupancy"; 2030-11-30
1 further recorded trialNCT07723079
"Single-case Intervention Study for Visual Screening Assessment for Proof of Concept and Prediction of Clinical Response to Brexiprazole as Adjunctive Treatment in Adults With Major Depressive Disorder."; n 1; "Association between baseline eye-tracking measures and clinical response to naltrexone"; 2026-08-01
recorded 2026-09-01 · last checked 2026-09-04
Q8
Which 7 trials of Brexpiprazole posted no result?
Posted no result
7 of 7 completed trials
Registrations
NCT00805454, NCT02411695, NCT03292848, NCT03734354, NCT03734302 and NCT03874494, and 1 more
Completion dates
oldest 2009-07; newest 2022-12-31
Show the evidence
Trial
NCT00805454
2009-07
NCT02411695
2017-01-01
NCT03292848
2018-05-21
NCT03734354
2020-05-18
NCT03734302
2020-06-10
NCT03874494
2021-09-06
1 further recorded trialNCT04162522
2022-12-31
Q9
At the median, Brexpiprazole's trials enrolled 200 people — anything larger?
Median enrolment
200
Largest enrolment
2944
Registered trials counted
79
Q10
What do 1024 spontaneous reports say about Brexpiprazole — and not say?
These are reports people sent to a regulator. They do not show the medicine caused the reaction. Nobody counted how many people took the medicine and reported nothing. The same event can be reported more than once, and many reports are incomplete. News coverage, lawsuits and new warnings change how often people report. A count is not a rate and not a risk.
Brexpiprazole appears in spontaneous reports to regulators. Across the 10 most-reported reaction terms, 1024 reaction mentions were counted: weight increased 274; akathisia 166; anxiety 103; restlessness 80. open-targets-adr · CHEMBL2105760 · 2026-06-24
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weight increased
274
akathisia
166
anxiety
103
restlessness
80
suicidal ideation
76
tremor
73
4 more recorded rows
depression
71
feeling abnormal
63
tardive dyskinesia
60
wrong technique in product usage process
58
recorded 2026-06-24 · last checked 2026-09-04
Q11
Brexpiprazole and CYP2D6, CYP3A4 and BCRP: shared by which compounds?
CYP2D6, CYP3A4 and BCRP appear in Brexpiprazole's recorded interaction sentences, 9 in all. openfda-label+europepmc · 2026-08-30
Interpretation pharmacokinetics
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CYP1A1pharmacokinetics
Elimination Metabolism Based on in vitro metabolism studies of brexpiprazole using recombinant human cytochrome P450 (CYP1A1, 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A4), the metabolism of brexpiprazole was shown to be mainly mediated by CYP3A4 and CYP2D6.
CYP2D6
pharmacokinetics
Elimination Metabolism Based on in vitro metabolism studies of brexpiprazole using recombinant human cytochrome P450 (CYP1A1, 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A4), the metabolism of brexpiprazole was shown to be mainly mediated by CYP3A4 and CYP2D6.
pharmacokinetics
In vivo brexpiprazole is metabolized primarily by CYP3A4 and CYP2D6 enzymes.
pharmacokinetics
Based on simulation, a 5.1-fold increase in AUC values at steady-state is expected when extensive metabolizers of CYP2D6 are administered with both strong CYP2D6 and CYP3A4 inhibitors.
pharmacokinetics
A 4.8-fold increase in mean AUC values at steady-state is expected in poor metabolizers of CYP2D6 administered with strong CYP3A4 inhibitors [see Drug Interactions ( 7.1 )].
CYP3A4
pharmacokinetics
Elimination Metabolism Based on in vitro metabolism studies of brexpiprazole using recombinant human cytochrome P450 (CYP1A1, 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A4), the metabolism of brexpiprazole was shown to be mainly mediated by CYP3A4 and CYP2D6.
pharmacokinetics
In vivo brexpiprazole is metabolized primarily by CYP3A4 and CYP2D6 enzymes.
pharmacokinetics
Based on simulation, a 5.1-fold increase in AUC values at steady-state is expected when extensive metabolizers of CYP2D6 are administered with both strong CYP2D6 and CYP3A4 inhibitors.
pharmacokinetics
A 4.8-fold increase in mean AUC values at steady-state is expected in poor metabolizers of CYP2D6 administered with strong CYP3A4 inhibitors [see Drug Interactions ( 7.1 )].
recorded 2026-08-30 · last checked 2026-09-04
Q12
Was Brexpiprazole studied with fasting and exercise?
fasting and exercise are named in Brexpiprazole's label sentences: "By contrast, compared with placebo, lurasidone and cariprazine respectively reduce fasting glucose and LDL-cholesterol, while aripiprazole and brexpiprazole increase HDL-cholesterol." openfda-label+europepmc · 2026-08-30
2 recorded statements; fasting, exercise
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fasting
By contrast, compared with placebo, lurasidone and cariprazine respectively reduce fasting glucose and LDL-cholesterol, while aripiprazole and brexpiprazole increase HDL-cholesterol.
exercise
In mixed age groups, in bipolar disorder aripiprazole was metabolically neutral; in depression, SSRIs lowered blood pressure versus placebo and serotonin-noradrenaline reuptake inhibitors (small ES); brexpiprazole augmentation caused WG and was less tolerated (small ES); exercise improved PHQoL (moderate ES).
recorded 2026-08-30 · last checked 2026-09-04
Q13
What is recorded about Brexpiprazole and AMPK?
"Brexpiprazole inhibited cell proliferation and de novo lipogenesis through AMPK/SREBP1 pathway in CRC." — where Brexpiprazole and AMPK appear together. Europe PMC · pathway abstract search · 2023-06-22
AMPK; PMID 37347510, 36750570
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AMPK
PMID 37347510
"Brexpiprazole inhibited cell proliferation and de novo lipogenesis through AMPK/SREBP1 pathway in CRC."
PMID 36750570
"Therefore, the present study determined the chronic effects of clozapine (high risk of weight gain) and brexpiprazole (relatively low risk of weight gain) on intracellular and extracellular levels of β-aminoisobutyric acid (BAIBA) enantiomers, which are endogenous activators of AMP-activated protein kinase (AMPK)."
recorded 2023-06-22 · last checked 2026-09-04
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