brexpiprazole

General information

• Class: Antipsychotic
• Common US brands: REXULTI
• Typical dose range: Schizophrenia (adults): titrate from 1 mg once daily (days 1–4) to 2 mg (days 5–7), then 4 mg once daily; therapeutic range 2–4 mg/day.
• Therapeutic drug monitoring not routinely recommended.
• Last reviewed: 2025-09-23

Dosing & forms

• Forms/strengths: Oral tablets: 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg (scored for flexible titration).
• Frequency: Schizophrenia (adults): titrate from 1 mg once daily (days 1–4) to 2 mg (days 5–7), then 4 mg once daily; therapeutic range 2–4 mg/day.
• Typical range: Schizophrenia (adults): titrate from 1 mg once daily (days 1–4) to 2 mg (days 5–7), then 4 mg once daily; therapeutic range 2–4 mg/day.

Mechanism (brief)

D2/D3 partial agonist; 5‑HT1A partial agonist; 5‑HT2A antagonist.

Metabolism & Half‑life

• Metabolism: CYP3A4, CYP2D6
• Half‑life: Steady-state mean 91 h

Therapeutic Drug Monitoring (TDM)

Recommended: No

Sources

• REXULTI label — DailyMed
• The American Psychiatric Association Practice Guideline for the Treatment of Patients With Schizophrenia — American Psychiatric Association (2020)
• AGNP Consensus Guidelines for Therapeutic Drug Monitoring in Neuropsychopharmacology — Pharmacopsychiatry (2018)
• Efficacy and safety of brexpiprazole for the treatment of acute schizophrenia: a randomized, double-blind, placebo-controlled trial — Schizophrenia Research (2015)
• Adjunctive brexpiprazole 1 and 3 mg/d for patients with major depressive disorder: a randomized, double-blind, placebo-controlled study — The Journal of Clinical Psychiatry (2015)