Drug name
Last update: Apr 2026Aripiprazole
Developer(s)
Drug information
Aripiprazole Lauroxil
ARISTADA
Small molecule
Not provided
1) ARISTADA (Aripiprazole Lauroxil) is a long-acting antipsychotic (partial agonist—D2, D3, 5-HT1A, and 5-HT2A receptor) used for the treatment of schizophrenia and related psychotic disorders. 2) The efficacy of ARISTADA is produced by aripiprazole and dehydro-aripiprazole (major metabolite). 3) Pharmacokinetic parameters: t1/2—53.9 days to 57.2 days; Vd—268 L; 4) > 99% bound to albumin 5) The levels of Cmax and AUC values are 2.5% higher for extensive metabolizers of CYP2D6
ARISTADA is approved by US FDA
ARISTADA is approved by US FDA
Therapeutic area(s)
- Mental Health Disorders (incl. schizophrenia, bipolar disorders, Schiz. Aff. Dis.)
- Treatment
Administration route
Intramuscular
Associated long-acting platforms
Inorganic nanoparticles
Use of drug
- Administered by a nurse
- Monthly
- Every 2 months
- Every 6 weeks
Dosage
injectable suspensions of 441mg/1.6ml (275.63mg/ml); 662mg/2.4ml (275.83mg/ml); 882mg/3.2ml (275.63mg/ml)
1064 mg single dose as intramuscular injection
Option 1: Administer one intramuscular injection of ARISTADA INITIO 675 mg (in either the deltoid or gluteal muscle) and one dose of oral aripiprazole 30 mg in conjunction with the first ARISTADA injection. The first ARISTADA injection may be administered on the same day as ARISTADA INITIO or up to 10 days thereafter. See the ARISTADA INITIO prescribing information for additional information regarding administration of ARISTADA INITIO. o Avoid injecting both ARISTADA INITIO and ARISTADA concomitantly into the same deltoid or gluteal muscle. Option 2: Administer 21 consecutive days of oral aripiprazole in conjunction with the first ARISTADA injection.
Not provided
Associated compounds, formulations and regimens
Not provided
Associated technologies
Not provided
Additional information
Developer(s)
Alkermes
Drug structure
Scale-up and manufacturing prospects
Not provided
Reactor vessel; heating systems; Nitrogen atmosphere setup; Filtration apparatus; Vacuum distillation setup
Manufacturing can be divided into two steps: 1) Formation of Aripiprazole Intermediate (Hydroxymethyl Aripiprazole) using paraformaldehyde, organic solvent (e.g., toluene), and base (e.g., DBU or potassium carbonate). 2) Esterification to form Aripiprazole lauroxil using lauric acid, DCC (activator), DMAP (catalyst), solvent (e.g., dichloromethane)
1. High-Performance Liquid Chromatography (HPLC) 2. Mass Spectrometer
Excipients & delivery device(s)
Not provided
Not provided
Not provided
No delivery device
Safety, Efficacy and Evidence Summary
Not provided
Not provided
Not provided
Not provided
Methods for administering aripiprazole
The present invention relates to pharmaceutical compositions comprising a compound of Formula (I) that are useful for the intramuscular delivery of antipsychotic drugs using rapid injection rates.
US8759351B2
Formulation
Alkermes Pharma Ireland Ltd
Not provided
March 13, 2035
Active
Pharmaceutical compositions comprising sorbitan esters
The present invention relates to a pharmaceutical composition comprising sorbitan esters of carboxylic acids that are useful for the delivery of anti-psychotic drugs.
US20240131024A1
Formulation
Alkermes Pharma Ireland Ltd
Not provided
Not provided
Pending