Aripiprazole Lauroxil

Aripiprazole lauroxil is a prodrug of aripiprazole. Following intramuscular injection, aripiprazole lauroxil is likely converted by enzyme-mediated hydrolysis to N-hydroxymethyl aripiprazole, which is then hydrolyzed to aripiprazole.

• ARISTADA is indicated for the treatment of schizophrenia in adults [see Clinical Studies ( 14 )]. ARISTADA is an atypical antipsychotic indicated for the treatment of schizophrenia in adults ( 1 ).ICD-10: F20.9

• ARISTADA is contraindicated in patients with a known hypersensitivity reaction to aripiprazole. Hypersensitivity reactions have ranged from pruritus/urticaria to anaphylaxis [see Adverse Reactions ( 6 )].contraindicated

Administer ARISTADA by intramuscular injection in the deltoid (441 mg dose only) or gluteal (441 mg, 662 mg, 882 mg or 1064 mg) muscle by a healthcare professional ( 2.1 ). For patients naïve to aripiprazole, establish tolerability with oral aripiprazole prior to initiating treatment with ARISTADA ( 2.1 ). There are two options for initiating treatment with ARISTADA: Option #1: Administer one injection of 675 mg of ARISTADA INITIO ® and one 30 mg dose of oral aripiprazole in conjunction with the first ARISTADA injection. ( 2.1 ). Option #2: Administer 21 consecutive days of oral aripiprazole in conjunction with the first ARISTADA injection ( 2.1 ). ARISTADA can be initiated at a dose of 441 mg, 662 mg or 882 mg administered monthly, 882 mg dose every 6 weeks, or 1064 mg dose every 2 months ( 2.1 ). Dosing regimen adjustments may be required for missed doses ( 2.2 ). Dose adjustments are required for 1) known CYP2D6 poor metabolizers and 2) for patients taking CYP3A4 inhibitors, CYP2D6 inhibitors, or CYP3A4 inducers for more than 2 weeks ( 2.4 ). 2.1 Recommended Dosage ARISTADA is only to be administered as an intramuscular injection by a healthcare professional. For patients who have never taken aripiprazole, establish tolerability with oral aripiprazole prior to initiating treatment with ARISTADA. Due to the half-life of oral aripiprazole, it may take up to 2 weeks to fully assess tolerability. Refer to the prescribing information of oral aripiprazole for the recommended dosage and administration of the oral formulation.

Cerebrovascular Adverse Reactions in Elderly Patients with Dementia-Related Psychosis: Increased incidence of cerebrovascular adverse reactions (e.g., stroke, transient ischemia attack, including fatalities) ( 5.2 ). Potential for Dosing and Medication Errors : Substitution and dispensing errors between ARISTADA and ARISTADA INITIO could occur. Do not substitute ARISTADA INITIO for ARISTADA ( 5.3 ). Neuroleptic Malignant Syndrome : Manage with immediate discontinuation and close monitoring ( 5.4 ). Tardive Dyskinesia : Discontinue if clinically appropriate ( 5.5 ). Metabolic Changes : Monitor for hyperglycemia, dyslipidemia, and weight gain ( 5.6 ). Pathological Gambling and Other Compulsive Behaviors : Consider dose reduction or discontinuation ( 5.7 ). Orthostatic Hypotension : Monitor heart rate and blood pressure and warn patients with known cardiovascular or cerebrovascular disease, and risk of dehydration or syncope ( 5.8 ). Leukopenia, Neutropenia, and Agranulocytosis : Perform complete blood counts in patients with a history of a clinically significant low white blood cell (WBC) count. Consider discontinuation if clinically significant decline in WBC in the absence of other causative factors ( 5.10 ). Seizures : Use cautiously in patients with a history of seizures or with conditions that lower the seizure threshold ( 5.11 ). Potential for Cognitive and Motor Impairment : Use caution when operating machinery ( 5.12 ).

The following are discussed in more details in other sections of the labeling: Increased Mortality in Elderly Patients with Dementia-related Psychosis [see Boxed Warning , Warnings and Precautions ( 5.1 )] Cerebrovascular Adverse Reactions, Including Stroke [see Boxed Warning , Warnings and Precautions ( 5.2 )] Neuroleptic Malignant Syndrome [see Warnings and Precautions ( 5.4 )] Tardive Dyskinesia [see Warnings and Precautions ( 5.5 )] Metabolic Changes [see Warnings and Precautions ( 5.6 )] Pathological Gambling and Other Compulsive Behaviors [see Warnings and Precautions ( 5.7 )] Orthostatic Hypotension [see Warnings and Precautions ( 5.8 )] Falls [see Warnings and Precautions ( 5.9 )] Leukopenia, Neutropenia, and Agranulocytosis [see Warnings and Precautions ( 5.10 )] Seizures [see Warnings and Precautions ( 5.11 )] Potential for Cognitive and Motor Impairment [see Warnings and Precautions ( 5.12 )] Body Temperature Regulation [see Warnings and Precautions ( 5.13 )] Dysphagia [see Warnings and Precautions ( 5.14 )] Most commonly observed adverse reaction with ARISTADA (incidence ≥5% and at least twice that for placebo) was akathisia ( 6.1 ). To report SUSPECTED ADVERSE REACTIONS, contact Alkermes, Inc. at 1-866-274-7823 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Studies Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Pregnancy: May cause extrapyramidal and/or withdrawal symptoms in neonates in women exposed during the third trimester of pregnancy ( 8.1 ). Lactation: Monitor the breastfed infant for dehydration and lack of appropriate weight gain ( 8.2 ). 8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to ARISTADA during pregnancy. For more information, contact the National Pregnancy Registry for Atypical Antipsychotics at 1-866-961-2388 or visit http://womensmentalhealth.org/clinical-and-research-programs/pregnancyregistry/. Risk Summary Neonates exposed to antipsychotic drugs, including ARISTADA, during the third trimester of pregnancy are at risk for extrapyramidal and/or withdrawal symptoms following delivery. Limited published data on aripiprazole use in pregnant women are not sufficient to inform any drug-associated risks for birth defects or miscarriage (see Clinical Considerations ) . Overall available data from published epidemiologic studies of pregnant women exposed to aripiprazole have not established a drug-associated risk of major birth defects, miscarriage, or adverse maternal outcomes. There are risks to the mother associated with untreated schizophrenia and with exposure to antipsychotics, including ARISTADA, during pregnancy (see Clinical Considerations ) .

Metabolism

ARISTADA is a prodrug of aripiprazole and its activity is primarily due to aripiprazole, and to a lesser extent dehydro-aripiprazole (major metabolite of aripiprazole), which has been shown to have affinities for D 2 receptors similar to aripiprazole and represents 30-40% of the aripiprazole exposure in plasma. Absorption After single intramuscular injection the appearance of aripiprazole in the systemic circulation starts from 5 to 6 days and continues to be released for an additional 36 days.

10.1 Human Experience Common adverse reactions (reported in at least 5% of all overdose cases) reported with oral aripiprazole overdosage (alone or in combination with other substances) include vomiting, somnolence, and tremor. Other clinically important signs and symptoms observed in one or more patients with aripiprazole overdoses (alone or with other substances) include acidosis, aggression, aspartate aminotransferase increased, atrial fibrillation, bradycardia, coma, confusional state, convulsion, blood creatine phosphokinase increased, depressed level of consciousness, hypertension, hypokalemia, hypotension, lethargy, loss of consciousness, QRS complex prolonged, QT prolonged, pneumonia aspiration, respiratory arrest, status epilepticus, and tachycardia. 10.2 Management of Overdosage In case of overdosage, call the Poison control center immediately at 1-800-222-1222.

• Oct 5, 2015NDANDA207533Alkermes Inc
• Jun 29, 2018NDANDA209830Alkermes Inc

1. 1Off Label Use1,09024%
2. 2Needle Issue60914%
3. 3Injection Site Pain4329.7%
4. 4Drug Ineffective2686.0%
5. 5Weight Increased2154.8%
6. 6Product Administered At Inappropriate Site2064.6%
7. 7Incorrect Dose Administered1794.0%
8. 8Therapeutic Response Shortened1784.0%
9. 9Hallucination, Auditory1733.9%
10. 10Underdose1693.8%
11. 11Syringe Issue1563.5%
12. 12Fatigue1523.4%
13. 13Anxiety1503.4%
14. 14Injection Site Mass1443.2%
15. 15Hospitalisation1433.2%

The 10 most recently updated of 10 ClinicalTrials.gov registrations naming Aripiprazole Lauroxil as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• C-Cog in Early Course Schizophrenia Study
  Terminated · Phase 4 · Interventional · 1 enrolled · University of Miami
  NCT05662306updated 2026-02-06
• National Pregnancy Registry for Psychiatric Medications
  Recruiting · Observational · 5,000 enrolled · Massachusetts General Hospital
  NCT01246765updated 2025-10-24
• VA Aripiprazole vs Esketamine for Treatment Resistant Depression
  Withdrawn · Phase 4 · Interventional · 0 enrolled · VA Office of Research and Development
  NCT05554627updated 2024-01-05
• Aripiprazole Lauroxil for Preventing Psychotic Relapse After an Initial Schizophrenia Episode
  Terminated · Phase 4 · Interventional · 15 enrolled · University of California, Los Angeles
  NCT04203056updated 2023-11-28
• Observational Study of Long Acting Injectable Medications (LAIs) in Schizophrenia (OASIS)
  Completed · Observational · 338 enrolled · Alkermes, Inc.
  NCT03919994updated 2023-02-02
• A Study of Aripiprazole Lauroxil or Paliperidone Palmitate for the Treatment of Schizophrenia
  Completed · Phase 3 · Interventional · 200 enrolled · Alkermes, Inc.
  NCT03345979updated 2020-08-11
• A Study to Evaluate the Efficacy and Safety of ALKS 9072 (Also Known as Aripiprazole Lauroxil, ALKS 9070, or ARISTADA) in Subjects With Schizophrenia
  Completed · Phase 3 · Interventional · 623 enrolled · Alkermes, Inc.
  NCT01469039updated 2019-01-30
• A Study of Aripiprazole Lauroxil (Also Known as ARISTADA TM) in Subjects With Schizophrenia
  Completed · Phase 4 · Interventional · 51 enrolled · Alkermes, Inc.
  NCT02634320updated 2018-12-04
• An Open-Label Study of Aripiprazole Lauroxil in Subjects With Stable Schizophrenia
  Completed · Phase 1 · Interventional · 140 enrolled · Alkermes, Inc.
  NCT02320032updated 2018-08-29
• A Study of Aripiprazole Lauroxil in Subjects With Schizophrenia or Schizoaffective Disorder
  Completed · Phase 1 · Interventional · 47 enrolled · Alkermes, Inc.
  NCT02636842updated 2016-07-14

CPIC-curated drug–gene pairs for Aripiprazole Lauroxil. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

• CYP2D6CPIC B/C (provisional)FDA label: Actionable PGx

Frequently asked questions

How does Aripiprazole Lauroxil work?

Aripiprazole lauroxil is a prodrug of aripiprazole. Following intramuscular injection, aripiprazole lauroxil is likely converted by enzyme-mediated hydrolysis to N-hydroxymethyl aripiprazole, which is then hydrolyzed to aripiprazole.

What is Aripiprazole Lauroxil used for?

According to FDA labeling, Aripiprazole Lauroxil carries indications including: ARISTADA is indicated for the treatment of schizophrenia in adults [see Clinical Studies ( 14 )]. ARISTADA is an atypical antipsychotic indicated for the treatment of schizophrenia in adults ( 1 ).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Aripiprazole Lauroxil?

Aripiprazole Lauroxil is classified as Dopamine Receptor Interactions, Serotonin Receptor Interactions, Decreased Dopamine Activity, Decreased Serotonin Activity.

What are the brand names for Aripiprazole Lauroxil?

Aripiprazole Lauroxil is marketed under brand names including Aristada.

What are the contraindications for Aripiprazole Lauroxil?

Aripiprazole Lauroxil labeling lists contraindications including: ARISTADA is contraindicated in patients with a known hypersensitivity reaction to aripiprazole. Hypersensitivity reactions have ranged from pruritus/urticaria to anaphylaxis [see Adverse Reactions ( 6 )].. Always consult the full prescribing information and a clinician.