Maximum Dose of Rexulti (Brexpiprazole) for Schizophrenia
The maximum recommended dose of brexpiprazole for adults with schizophrenia is 4 mg once daily. 1
Dosing Algorithm for Schizophrenia
Initial titration schedule:
- Start at 1 mg orally once daily on Days 1-4 1
- Increase to 2 mg once daily on Days 5-7 1
- On Day 8, may increase to the maximum of 4 mg once daily based on clinical response and tolerability 1
Target dose range:
- The recommended target dosage is 2-4 mg once daily 1
- Clinical trials demonstrated efficacy at 2-4 mg/day with a pooled response rate of 45.5% versus 31.0% for placebo 2, 3
Dose Reductions Required in Specific Populations
Hepatic impairment (moderate to severe, Child-Pugh score ≥7):
- Maximum dose is 3 mg once daily 1
Renal impairment (CrCl <60 mL/minute):
- Maximum dose is 3 mg once daily 1
CYP2D6 poor metabolizers:
- Administer half of the recommended dosage (maximum 2 mg daily) 1
Concomitant strong CYP2D6 or CYP3A4 inhibitors:
- Administer half of the recommended dosage (maximum 2 mg daily) 1
Concomitant strong/moderate CYP2D6 AND CYP3A4 inhibitors (or known CYP2D6 poor metabolizers taking strong/moderate CYP3A4 inhibitors):
- Administer a quarter of the recommended dosage (maximum 1 mg daily) 1
Concomitant strong CYP3A4 inducers:
- Double the recommended dosage over 1-2 weeks (maximum 8 mg daily) 1
Clinical Efficacy at Maximum Dose
The 4 mg dose demonstrated significant efficacy in maintenance treatment, with only 13.5% of patients relapsing compared to 38.5% on placebo over 52 weeks, yielding a number needed to treat of 4. 2, 3 However, doses above 4 mg have not been studied and provide no established additional benefit. 1
Common Pitfall
Do not exceed 4 mg daily in standard patients, as higher doses have not demonstrated additional efficacy and may increase adverse effects. 1 The FDA label explicitly states 4 mg as the maximum recommended daily dosage for schizophrenia in adults without dose-modifying factors. 1