Aripiprazole lauroxil

Modify Date: 2024-01-06 23:05:30

Aripiprazole lauroxil Structure
Aripiprazole lauroxil structure
Common Name Aripiprazole lauroxil
CAS Number 1259305-29-7 Molecular Weight 660.71400
Density N/A Boiling Point N/A
Molecular Formula C36H51Cl2N3O4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Aripiprazole lauroxil


Aripiprazole lauroxil, an N-acyloxymethyl prodrug of aripiprazole, is a Long-acting injectable (LAI) typical antipsychotic for schizophrenia. Aripiprazole lauroxil is cleaved by body’s enzyme esterase to N-hydroxymethyl aripiprazole (plus lauric acid) and then to aripiprazole (plus formaldehyde), no toxicity[1].

 Names

Name [7-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy]-2-oxo-3,4-dihydroquinolin-1-yl]methyl dodecanoate
Synonym More Synonyms

 Aripiprazole lauroxil Biological Activity

Description Aripiprazole lauroxil, an N-acyloxymethyl prodrug of aripiprazole, is a Long-acting injectable (LAI) typical antipsychotic for schizophrenia. Aripiprazole lauroxil is cleaved by body’s enzyme esterase to N-hydroxymethyl aripiprazole (plus lauric acid) and then to aripiprazole (plus formaldehyde), no toxicity[1].
Related Catalog
In Vivo Aripiprazole lauroxil (intravenous administration; 1.87 mg/ml) bioconversion in vivo involves the formation of an intermediate, N-hydroxymethyl aripiprazole, the in vitro data indicates a high bioconversion of aripiprazole lauroxil, thus, the concentration of N-hydroxymethyl aripiprazole observed in the animals dosed with aripiprazole lauroxil is surprisingly high[1]. Animal Model: Female Sprague Dawley rats[1] Dosage: 1.87 mg/ml  Administration: Blood samples is taken at 5, 15, 30 min and 1, 2, 4, 6, 8 and 24 h after administration Result: Exhibits an clearance: 0.32 ± 0.11 L/h/kg. 
References

[1]. Jann MW, et al. Long-Acting Injectable Second-Generation Antipsychotics: An Update and Comparison Between Agents.CNS Drugs. 2018 Mar;32(3):241-257.

[2]. Rohde M, et al. Biological conversion of aripiprazole lauroxil - An N-acyloxymethyl aripiprazole prodrug.Results Pharma Sci. 2014 May 2;4:19-25.

 Chemical & Physical Properties

Molecular Formula C36H51Cl2N3O4
Molecular Weight 660.71400
Exact Mass 659.32600
PSA 62.32000
LogP 8.74330
Storage condition 2~8°C

 Safety Information

Hazard Codes Xi

 Synonyms

Aripiprazole lauroxil (USAN)
Aripiprazole lauroxil
UNII-B786J7A343
(7-(4-(4-(2,3-Dichlorophenyl)piperazin-1-yl)butoxy)-2-oxo-3,4-dihydroquinolin-1(2H)-yl)methyl dodecanoate
RDC-3317
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