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Aripiprazole lauroxil

Generic Name
Aripiprazole lauroxil
Brand Names
Aristada
Drug Type
Small Molecule
Chemical Formula
C36H51Cl2N3O4
CAS Number
1259305-29-7
Unique Ingredient Identifier
B786J7A343

Overview

Aripiprazole lauroxil is a long-acting injectable atypical antipsychotic drug used in the treatment of schizophrenia in adult patients. It is a prodrug of aripiprazole, which acts as a partial agonist at the D2 and 5-HT1A receptors, and as an antagonist at the 5-HT2A receptors . Affecting about 1% of the adult population in the United States and approximately 26 million people worldwide, schizophrenia is a chronic neurological disorder that may result in impairments in cognition and executive functions . The quality of life in patients is greatly reduced due to negative health outcomes, and oftentimes the patients are faced with social stigma and discriminations. Schizophrenia is characterized by positive symptoms such as delusions, hallucinations, thought disorders, and catanoia, and negative symptoms that include social withdrawal, anhedonia, and flattening of emotional responses . D2 receptors have been the most common target for antipsychotic agents used in the treatment of schizophrenia: the positive symptoms are thought to arise from overactivity in the mesolimbic dopaminergic pathway activating D2 receptors, whereas negative symptoms may result from a decreased activity in the mesocortical dopaminergic pathway with D1 receptors predominating . In a randomized, double-blind clinical trial, treatment of aripiprazole lauroxil in adult patients with schizophrenia resulted in improvement of positive and negative symptoms scores at day 85 of treatment . Aripiprazole lauroxil was initially approved by the FDA in October 2015 under the market name Aristada for the treatment of schizophrenia. It is administered via intramuscular injection, and requires the establishment of tolerability prior to dosing in treatment-naïve patients . On July 2nd, a different formulation of aripiprazole lauroxil marketed as Aristada Initio was FDA-approved for immediate initiation of Aristada at any dose. The patients may receive Aristada Initio in combination with a single 30 mg oral dose of aripiprazole to achieve appropriate levels of aripiprazole more rapidly. Long-acting injectable aripiprazole lauroxil displayed comparable efficacy and safety to aripiprazole , and reduced dosing frequency improves patient adherence.

Indication

Aripiprazole lauroxil is indicated for the treatment of schizophrenia and related psychotic disorders.

Associated Conditions

  • Schizophrenia

FDA Drug Approvals

Approved Product
Manufacturer
NDC Code
Route
Strength
Effective Date
Alkermes, Inc.
65757-401
INTRAMUSCULAR
441 mg in 1.6 mL
1/15/2021
Alkermes, Inc.
65757-404
INTRAMUSCULAR
1064 mg in 3.9 mL
1/15/2021
Alkermes, Inc.
65757-402
INTRAMUSCULAR
662 mg in 2.4 mL
1/15/2021
Alkermes, Inc.
65757-500
INTRAMUSCULAR
675 mg in 2.4 mL
1/15/2021
Alkermes, Inc.
65757-403
INTRAMUSCULAR
882 mg in 3.2 mL
1/15/2021

EMA Drug Approvals

Approved Product
Authorization Holder
Status
Issued Date
No EMA approvals found for this drug.

HSA Drug Approvals

Approved Product
Manufacturer
Approval Number
Dosage Form
Strength
Approval Date
No HSA approvals found for this drug.

NMPA Drug Approvals

Approved Product
Company
Approval Number
Drug Type
Dosage Form
Approval Date
No NMPA approvals found for this drug.

PPB Drug Approvals

Approved Product
Registration No.
Company
Licence No.
Strength
Registration Date
No PPB approvals found for this drug.

TGA Drug Approvals

Approved Product
ARTG ID
Sponsor
Registration Type
Status
Registration Date
No TGA approvals found for this drug.

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