milsaperidone

Antipsychotic

Brands: Bysanti

Last reviewed 2026-02-28

Reviewed by PsychMed Editorial Team.

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Quick answers

What is milsaperidone?
Milsaperidone (brand BYSANTI) is a second-generation antipsychotic approved by the FDA in February 2026 for adult schizophrenia and acute manic or mixed episodes associated with bipolar I disorder.
What is Bysanti?
Bysanti is a brand name for milsaperidone.
What is Bysanti (milsaperidone) used for?
Label indications include: Schizophrenia (adults); Acute manic/mixed episodes in bipolar I disorder (adults).
What drug class is Bysanti (milsaperidone)?
Antipsychotic.
What is the mechanism of action of Bysanti (milsaperidone)?
Dopamine D2, serotonin 5-HT2A, and adrenergic α1 antagonist (active metabolite of iloperidone) requiring titration to mitigate orthostatic effects.
What strengths does Bysanti (milsaperidone) come in?
Tablets: 1 mg, 2 mg, 4 mg, 6 mg, 8 mg, 10 mg, 12 mg.
Is Bysanti (milsaperidone) a controlled substance?
No — it is not scheduled as a controlled substance under U.S. federal law.
What is Bysanti (milsaperidone) dosing for schizophrenia?
Schizophrenia titration: Day 1 1 mg BID → Day 2 2 mg BID → Day 3 4 mg BID → Day 4 6 mg BID → Day 5 8 mg BID → Day 6 10 mg BID → Day 7 12 mg BID; maintenance target 6–12 mg BID.

Snapshot

Class: Antipsychotic
Common US brands: Bysanti
Therapeutic drug monitoring not routinely recommended.
Last reviewed: 2026-02-28

Clinical Highlights

Milsaperidone (brand BYSANTI) is a second-generation antipsychotic approved by the FDA in February 2026 for adult schizophrenia and acute manic or mixed episodes associated with bipolar I disorder. It is the active metabolite of iloperidone (Fanapt) and interconverts with iloperidone in vivo, sharing a similar receptor-binding profile with potent antagonism at dopamine D2, serotonin 5-HT2A, and adrenergic α1 receptors.

Tablet strengths from 1 mg to 12 mg enable fine-tuned dosing; therapy must restart at 1 mg twice daily if treatment is interrupted for three or more consecutive days.
Like its parent compound, milsaperidone requires gradual titration to mitigate orthostatic hypotension, syncope, and tachycardia, and carries a QTc prolongation warning.
Schizophrenia (adults) (FDA 2026)
Acute manic/mixed episodes in bipolar I disorder (adults) (FDA 2026)
Brand only: BYSANTI is marketed by Vanda Pharmaceuticals; commercial availability is expected in Q3 2026.
The compare tool and the evidence library, together with the Schizophrenia hub, support side-by-side review of related SGAs and follow-up planning.

Dosing & Formulations

Tablets: 1 mg, 2 mg, 4 mg, 6 mg, 8 mg, 10 mg, 12 mg. Schizophrenia titration: Day 1 1 mg BID → Day 2 2 mg BID → Day 3 4 mg BID → Day 4 6 mg BID → Day 5 8 mg BID → Day 6 10 mg BID → Day 7 12 mg BID; maintenance target 6–12 mg BID.

Bipolar I mania titration: Day 1 2 mg BID → Day 2 4 mg BID → Day 3 8 mg BID → Day 4 10 mg BID → Day 5 12 mg BID; target 12 mg BID.
CYP2D6 poor metabolizers: reduce dose by 50%. Half-life extends to approximately 37 hours in poor metabolizers compared to 26 hours in extensive metabolizers.
Strong CYP2D6 inhibitors (fluoxetine, paroxetine) or strong CYP3A4 inhibitors (ketoconazole, clarithromycin): dose reduction by ~50% is recommended, with QTc monitoring.
If therapy is interrupted for ≥3 consecutive days, titration is typically restarted at 1 mg twice daily to reduce orthostatic events.

Monitoring & Risks

Boxed warning: Antipsychotics increase mortality in elderly patients with dementia-related psychosis; milsaperidone is not approved for this population. Orthostatic hypotension/syncope: Most pronounced during titration; counseling often includes hydration and slow position changes.

Tachycardia: Heart rate increases are common, particularly early in treatment; pulse is often monitored alongside QTc-prolonging co-medications.
Somnolence and dizziness: May improve after the first week; shifting a larger portion to bedtime when tolerated is a common strategy.
Weight gain: Modest average gain is expected; routine metabolic monitoring (fasting glucose, lipids, weight/BMI) is recommended.
Dry mouth: Common; supportive care is usually sufficient.

Drug Interactions

Strong CYP2D6 inhibitors or poor metabolizer status often require halving the milsaperidone dose. Strong CYP3A4 inhibitors elevate exposure—dose reduction by ~50% is common, with QTc monitoring often considered.

Strong CYP3A4 inducers can markedly reduce serum levels and are generally avoided due to potential loss of efficacy.
Additive QTc prolongation with drugs such as amiodarone, sotalol, or methadone; ECG monitoring is often considered or alternatives may be preferred.
Concomitant antihypertensives, alcohol, or CNS depressants may potentiate hypotension and sedation.

Practice Notes

Orthostatic vitals are often checked at baseline, during titration, and after dose increases. Patient education often includes restarting titration if therapy is interrupted and reporting presyncope, palpitations, or dizziness.

Milsaperidone's dual-indication approval (schizophrenia and bipolar I mania) broadens its clinical role compared to iloperidone, which carries only a schizophrenia indication.
Steady state is achieved within 3–4 days; hepatic impairment warrants slower titration and closer monitoring.

References

BYSANTI (milsaperidone) prescribing information — Vanda Pharmaceuticals (2026)
Vanda Pharmaceuticals announces FDA approval of BYSANTI (milsaperidone) for schizophrenia and bipolar I disorder — Vanda Pharmaceuticals (2026)
The American Psychiatric Association Practice Guideline for the Treatment of Patients With Schizophrenia — American Psychiatric Association (2020)Guidelineschizophreniaclinical
Canadian Network for Mood and Anxiety Treatments (CANMAT) and International Society for Bipolar Disorders (ISBD) 2018 guidelines for the management of patients with bipolar disorder — Bipolar Disorders (2018)
FANAPT (iloperidone) prescribing information — DailyMed (2024)