Rexulti

REXULTI- brexpiprazole tablet
Otsuka America Pharmaceutical, Inc.

WARNING: INCREASED MORTALITY IN ELDERLY PATIENTS WITH DEMENTIA-RELATED PSYCHOSIS and SUICIDAL THOUGHTS AND BEHAVIORS

Increased Mortality in Elderly Patients with Dementia-Related Psychosis

Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. REXULTI is not approved for the treatment of patients with dementia-related psychosis [see Warnings and Precautions (5.1)].

Suicidal Thoughts and Behaviors

Antidepressants increased the risk of suicidal thoughts and behaviors in patients aged 24 years and younger in short-term studies. Monitor closely for clinical worsening and for emergence of suicidal thoughts and behaviors. The safety and effectiveness of REXULTI have not been established in pediatric patients with MDD [see Warnings and Precautions (5.2), Use in Specific Populations (8.4)].

1 INDICATIONS AND USAGE

REXULTI is indicated for:

  • Adjunctive treatment of major depressive disorder (MDD) in adults.
  • Treatment of schizophrenia in adults and pediatric patients ages 13 years and older

2 DOSAGE AND ADMINISTRATION

2.1 Adjunctive Treatment of Major Depressive Disorder (Adults)

The recommended starting dosage for REXULTI as adjunctive treatment of MDD in adults is 0.5 mg or 1 mg once daily, taken orally with or without food [see Clinical Pharmacology (12.3)].

Titrate to 1 mg once daily, then up to the target dosage of 2 mg once daily. Dosage increases should occur at weekly intervals based on the patient’s clinical response and tolerability. The maximum recommended daily dosage is 3 mg. Periodically reassess to determine the continued need and appropriate dosage for treatment.

2.2 Treatment of Schizophrenia (Adults and Pediatric Patients 13 to 17 Years)

Adults

The recommended starting dosage for REXULTI for the treatment of schizophrenia in adults is 1 mg once daily on Days 1 to 4, taken orally with or without food [see Clinical Pharmacology (12.3)]. Titrate to 2 mg once daily on Day 5 through Day 7, then to 4 mg on Day 8 based on the patient’s clinical response and tolerability. The recommended target REXULTI dosage is 2 mg to 4 mg once daily. The maximum recommended daily dosage is 4 mg.

Pediatric Patients (13 to 17 years of age)

The recommended starting dosage for REXULTI for the treatment of schizophrenia in pediatric patients 13 to 17 years of age is 0.5 mg once daily on Days 1 to 4, taken orally with or without food [see Clinical Pharmacology (12.3)]. Titrate to 1 mg once daily on Day 5 through Day 7, then to 2 mg on Day 8 based on the patient’s clinical response and tolerability. Weekly dose increases can be made in 1 mg increments. The recommended target REXULTI dosage is 2 mg to 4 mg once daily. The maximum recommended daily dosage is 4 mg.

2.3 Dosage Adjustments for Hepatic Impairment

For patients with moderate to severe hepatic impairment (Child-Pugh score ≥7), the maximum recommended dosage is 2 mg once daily for patients with MDD, and 3 mg once daily for patients with schizophrenia [see Use in Specific Populations (8.7), Clinical Pharmacology (12.3)].

2.4 Dosage Adjustments for Renal Impairment

For patients with moderate, severe, or end-stage renal impairment (creatinine clearance CrCl<60 mL/minute), the maximum recommended dosage is 2 mg once daily for patients with MDD and 3 mg once daily for patients with schizophrenia [see Use in Specific Populations (8.8), Clinical Pharmacology (12.3)].

2.5 Dosage Modifications for CYP2D6 Poor Metabolizers and for Concomitant Use with CYP Inhibitors or Inducers

Dosage adjustments are recommended in patients who are known cytochrome P450 (CYP) 2D6 poor metabolizers and in patients taking concomitant CYP3A4 inhibitors or CYP2D6 inhibitors or strong CYP3A4 inducers (see Table 1). If the coadministered drug is discontinued, adjust the REXULTI dosage to its original level. If the coadministered CYP3A4 inducer is discontinued, reduce the REXULTI dosage to the original level over 1 to 2 weeks [see Drug Interactions (7.1), Clinical Pharmacology (12.3)].

Table 1 Dosage Adjustments of REXULTI for CYP2D6 Poor Metabolizers and for Concomitant Use with CYP3A4 and CYP2D6 Inhibitors and/or CYP3A4 Inducers
Factors Adjusted REXULTI Dosage
*
In the clinical trials examining the adjunctive use of REXULTI in the treatment of MDD, dosage was not adjusted for strong CYP2D6 inhibitors (e.g., paroxetine, fluoxetine). Thus, CYP considerations are already factored into general dosing recommendations, and REXULTI may be administered without dosage adjustment in patients with MDD.
CYP2D6 Poor Metabolizers
CYP2D6 poor metabolizers Administer half of the usual dose.
Known CYP2D6 poor metabolizers taking strong/moderate CYP3A4 inhibitors Administer a quarter of the usual dose.
Patients Taking CYP2D6 Inhibitors and/or CYP3A4 Inhibitors
Strong CYP2D6 inhibitors * Administer half of the usual dose.
Strong CYP3A4 inhibitors Administer half of the usual dose.
Strong/moderate CYP2D6 inhibitors with strong/moderate CYP3A4 inhibitors Administer a quarter of the usual dose.
Patients Taking CYP3A4 Inducers
Strong CYP3A4 inducers Double usual dose over 1 to 2 weeks.

3 DOSAGE FORMS AND STRENGTHS

REXULTI tablets are available in 6 strengths:

  • 0.25 mg tablets are light brown, round, shallow convex, bevel-edged body with “BRX” and “0.25” imprinted on one side
  • 0.5 mg tablets: are light orange, round, shallow convex, bevel-edged body with “BRX” and “0.5” imprinted on one side
  • 1 mg tablets are light yellow, round, shallow convex, bevel-edged body with “BRX” and “1” imprinted on one side
  • 2 mg tablets are light green, round, shallow convex, bevel-edged body with “BRX” and “2” imprinted on one side
  • 3 mg tablets are light purple, round, shallow convex, bevel-edged body with “BRX” and “3” imprinted on one side
  • 4 mg tablets are white, round, shallow convex, bevel-edged body with “BRX” and “4” imprinted on one side

4 CONTRAINDICATIONS

REXULTI is contraindicated in patients with a known hypersensitivity to brexpiprazole or any of its components. Reactions have included rash, facial swelling, urticaria, and anaphylaxis.

5 WARNINGS AND PRECAUTIONS

5.1 Increased Mortality in Elderly Patients with Dementia-Related Psychosis

Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Analyses of 17 placebo-controlled trials (modal duration of 10 weeks), largely in patients taking atypical antipsychotic drugs, revealed a risk of death in drug-treated patients of between 1.6 to 1.7 times the risk of death in placebo-treated patients. Over the course of a typical 10-week controlled trial, the rate of death in drug-treated patients was about 4.5%, compared to a rate of about 2.6% in the placebo group.

Although the causes of death were varied, most of the deaths appeared to be either cardiovascular (e.g., heart failure, sudden death) or infectious (e.g., pneumonia) in nature. REXULTI is not approved for the treatment of patients with dementia-related psychosis [see Boxed Warning, Warnings and Precautions (5.3)].

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