Annotation of FDA Label for aripiprazole and CYP2D6

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PharmGKB ID

PA166104839

Summary

The FDA-approved drug labels for aripiprazole (ABILIFY, ABILIFY MAINTENA and ABILIFY ASIMTUFII) provide dosage adjustments for patients who are CYP2D6 poor metabolizers (PMs). CYP2D6 PMs taking ABILIFY should receive half the usual dose; CYP2D6 PMs taking ABILIFY MAINTENA should have their dose reduced to 300 mg from the recommended dose of 400 mg; CYP2D6 PMs taking ABILIFY ASIMTUFII should have their dose reduced to 720 mg from the recommended dose of 960 mg. Also, CYP2D6 PMs taking concomitant CYP3A4 inhibitors should not be given ABILIFY ASIMTUFII.

Prescribing

Excerpt from the ABILIFY drug label:

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FactorsDosage Adjustments for ABILIFY
Known CYP2D6 Poor MetabolizersAdminister half of usual dose
Known CYP2D6 Poor Metabolizers taking concomitant strong CYP3A4 inhibitors (e.g., itraconazole, clarithromycin)Administer a quarter of usual dose

Excerpt from the ABILIFY MAINTENA drug label (Table 1):

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FactorsAdjusted Dose
Known CYP2D6 Poor Metabolizers300mg
Known CYP2D6 Poor Metabolizers taking concomitant CYP3A4 inhibitors200 mg

Excerpt from the ABILIFY ASIMTUFII drug label (Table 1):

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FactorsDosage Recommendation
Known CYP2D6 Poor Metabolizers720 mg once every 2 months
Known CYP2D6 Poor Metabolizers taking concomitant CYP3A4 inhibitorsAvoid use

Annotation

Aripiprazole (ABILIFY, ABILIFY MAINTENA and ABILIFY ASIMTUFII) is an atypical antipsychotic medication. ABILIFY formulations include tablet, solution, orally disintegrating tablet and injection. ABILIFY MAINTENA and ABILIFY ASIMTUFII are extended-release injectable suspensions for intramuscular use.

Excerpts from the ABILIFY (aripiprazole) drug label:

Known CYP2D6 Poor Metabolizers...Administer half of usual dose...

Dosage adjustment is recommended in known CYP2D6 poor metabolizers due to high aripiprazole concentrations. Approximately 8% of Caucasians and 3–8% of Black/African Americans cannot metabolize CYP2D6 substrates and are classified as poor metabolizers (PM) [...]

Excerpt from the ABILIFY MAINTENA (aripiprazole) drug label:

Known CYP2D6 poor metabolizers: Recommended starting and maintenance dose is 300 mg administered monthly as a single injection.

Excerpt from the ABILIFY ASIMTUFII (aripiprazole) drug label:

Known CYP2D6 poor metabolizers: Recommended dosage is 720 mg administered once every 2 months as a single injection

For the complete drug label texts with sections containing pharmacogenetic information highlighted, see the aripiprazole (ABILIFY) drug label, the aripiprazole (ABILIFY MAINTENA) drug label and the aripiprazole (ABILIFY ASIMTUFII) drug label.

*Disclaimer: The contents of this page have not been endorsed by the FDA and are the sole responsibility of PharmGKB.

FDA PGx Associations

From the FDA Table of Pharmacogenetic Associations(opens in new window):
CategoryDrugGeneAffected SubgroupInteraction Description
RecommendationsAripiprazoleCYP2D6poor metabolizers

Results in higher systemic concentrations and higher adverse reaction risk. Dosage adjustment is recommended. Refer to FDA labeling for specific dosing recommendations.

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Evidence for Clinical Annotations

This annotation has been used as evidence for the following clinical annotations.

    Sources

    1. Drugs@FDA: Drug Product Abilify Asimtufii (Aripiprazole), Otsuka America Pharmaceutical, Inc - NDA217006/SUPPL-2, 01/22/2025
      Has PGx
      ABILIFY ASIMTUFII
    2. Drugs@FDA: Drug Product ABILIFY (ARIPIPRAZOLE), NDA021436, Rebel Distributors Corp.
      Has PGxDrug-Drug Interactions 19Drug-Gene Interactions 2
      ABILIFY
    3. Drugs@FDA: Drug Product ABILIFY MAINTENA (aripiprazole), NDA202971, Otsuka America Pharmaceutical, Inc.
      Has PGxDrug-Drug Interactions 15Drug-Gene Interactions 1
      ABILIFY MAINTENA

    History

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