milsaperidone

General information

• Class: Antipsychotic
• Common US brands: Bysanti
• Typical dose range: Schizophrenia titration (adults): 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.
• Therapeutic drug monitoring not routinely recommended.
• Last reviewed: 2026-02-28

Dosing & forms

• Forms/strengths: Tablets: 1 mg, 2 mg, 4 mg, 6 mg, 8 mg, 10 mg, 12 mg.
• Frequency: Schizophrenia titration (adults): 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.
• Food: With or without food.
• Typical range: Schizophrenia titration (adults): 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.

Mechanism (brief)

Dopamine D2, serotonin 5-HT2A, and adrenergic α1 antagonist (active metabolite of iloperidone) requiring titration to mitigate orthostatic effects.

Metabolism & Half‑life

• Metabolism: CYP2D6, CYP3A4
• Half‑life: Single-dose mean 26 h; Steady-state mean 33 h

Therapeutic Drug Monitoring (TDM)

Recommended: No

Sources

• 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)
• 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)