Aripiprazole lauroxil - CAS 1259305-29-7
Catalog number: 1259305-29-7
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
5-HT Receptor | Dopamine Receptor
Aripiprazole lauroxil is a Dopamine D2 receptor agonist, Serotonin 1A receptor agonist and ISerotonin 2A receptor antagonist under the development of Alkermes plc. Aripiprazole lauroxil is applicated as long-acting injectable atypical antipsychotic for the treatment of schizophrenia. It is an N-acyloxymethyl prodrug of aripiprazole
Aristada; RDC-3317; RDC 3317; RDC3317; UNII-B786J7A343; ALKS 9070; ALKS9070; ALKS-9070; ALKS 9072; ALKS-9072; ALKS9072; [7-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy]-2-oxo-3,4-dihydroquinolin-1-yl]methyl dodecanoate
Soluble in DMSO
-20°C Freezer
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Canonical SMILES:
Current Developer:
Alkermes plc
1.Aripiprazole Lauroxil: A Review in Schizophrenia.
Frampton JE Drugs. 2017 Dec;77(18):2049-2056. doi: 10.1007/s40265-017-0848-4.
Aripiprazole lauroxil long-acting injectable (LAI) [Aristada;®;] is an intramuscularly administered, extended-release prodrug of aripiprazole, an established atypical antipsychotic agent that, in terms of its relative position within the class, is at the low end of the risk spectrum for metabolic side effects. In the USA, aripiprazole lauroxil LAI is indicated for the treatment of schizophrenia; approved doses of the drug can be injected once-monthly (q4w), every 6 weeks (q6w) or every 2 months (q8w). The efficacy of the 441 and 882 mg q4w dosages in the treatment of acute exacerbations of schizophrenia and as long-term maintenance therapy in stable schizophrenia has been directly demonstrated in a phase III clinical trial and extension, while the efficacy of the 662 mg q4w, 882 mg q6w and 1064 mg q8w dosing regimens has been established on the basis of pharmacokinetic bridging studies. Aripiprazole lauroxil LAI therapy was generally well tolerated, with an adverse event profile consistent with that of oral aripiprazole (with the exception of injection-site reactions), including a low propensity to cause metabolic disturbances. Thus, aripiprazole lauroxil LAI extends the treatment regimen options for patients with schizophrenia; as with other LAI formulations of antipsychotic agents, it can be particularly recommended for patients with recurrent relapses related to nonadherence to oral preparations and for those who prefer this mode of administration.
2.Relative bioavailability and safety of aripiprazole lauroxil, a novel once-monthly, long-acting injectable atypical antipsychotic, following deltoid and gluteal administration in adult subjects with schizophrenia.
Turncliff R;Hard M;Du Y;Risinger R;Ehrich EW Schizophr Res. 2014 Nov;159(2-3):404-10. doi: 10.1016/j.schres.2014.09.021. Epub 2014 Sep 27.
Aripiprazole lauroxil is a linker lipid ester of aripiprazole for extended-release intramuscular (IM) injection. This multicenter, randomized, open-label study evaluated the pharmacokinetics (PK), relative bioavailability, and tolerability of a single IM deltoid or gluteal injection of aripiprazole lauroxil in adult subjects with chronic stable schizophrenia or schizoaffective disorder. Forty-six subjects were randomized 1:1 to aripiprazole lauroxil 441 mg IM in the deltoid or gluteal muscle. Samples were collected through 89 days post-dose to measure levels of aripiprazole lauroxil, N-hydroxymethyl aripiprazole, aripiprazole, and dehydro-aripiprazole. Forty-three (93.5%) subjects completed all study assessments; most were CYP2D6 extensive or immediate metabolizers (96%); two (4%) were poor metabolizers. The PK of aripiprazole following aripiprazole lauroxil was characterized by a steady rise in plasma concentrations (Tmax 44-50 days), a broad peak, and prolonged exposure attributable to the dissolution of aripiprazole lauroxil and formation rate-limited elimination of aripiprazole (t1/2=15.4-19.2 days). Deltoid vs. gluteal administration resulted in slightly higher Cmax aripiprazole concentrations [1.
3.Aripiprazole Lauroxil Compared with Paliperidone Palmitate in Patients with Schizophrenia: An Indirect Treatment Comparison.
Cameron C;Zummo J;Desai DN;Drake C;Hutton B;Kotb A;Weiden PJ Value Health. 2017 Jul - Aug;20(7):876-885. doi: 10.1016/j.jval.2017.03.010. Epub 2017 May 9.
BACKGROUND: ;Aripiprazole lauroxil (AL) is a long-acting injectable atypical antipsychotic recently approved for treatment of schizophrenia on the basis of a large-scale trial of two doses of AL versus placebo. There are no direct-comparison studies with paliperidone palmitate (PP; long-acting antipsychotic used most often in acute settings) for the acute psychotic episode.;OBJECTIVES: ;To indirectly compare efficacy and safety of the pivotal AL study with all PP studies meeting indirect comparison criteria.;METHODS: ;Systematic searches of MEDLINE, Embase, Cochrane CENTRAL, PsycINFO,, International Clinical Trials Registry Platform, and gray literature were performed to identify randomized controlled trials of PP with similar designs to the AL trial. Bayesian network meta-analysis compared treatments with respect to symptom response and tolerability issues including weight gain, akathisia, parkinsonism, and likelihood of treatment-emergent adverse events.;RESULTS: ;Three appropriate PP studies were identified for indirect comparison. Both doses of AL (441 mg and 882 mg monthly) were used and compared with two efficacious doses of PP (156 mg and 234 mg monthly). All four active-treatment conditions were associated with comparable reductions in acute symptoms (Positive and Negative Syndrome Scale) versus placebo and were of similar magnitude (range of mean difference -8.
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