Comparative Pharmacology
Head-to-head clinical analysis: ARISTADA versus REXULTI.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ARISTADA versus REXULTI.
ARISTADA vs REXULTI
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Aripiprazole lauroxil is a prodrug of aripiprazole, a partial agonist at dopamine D2 and serotonin 5-HT1A receptors and an antagonist at 5-HT2A receptors. The mechanism of action in schizophrenia and bipolar I disorder is thought to be mediated through these receptor interactions.
Partial agonist at D2 and 5-HT1A receptors; antagonist at 5-HT2A and α1B/α2C adrenergic receptors.
Initial dose: 675 mg intramuscularly every 4 weeks for the first 2 doses, then maintenance dose of 882 mg intramuscularly every 4 weeks. Alternatively, 1064 mg intramuscularly every 6 weeks after appropriate initiation.
2 mg orally once daily initially; increase to 4 mg once daily no sooner than week 2; target dose 4 mg once daily; range 2-4 mg once daily.
None Documented
None Documented
Terminal elimination half-life of aripiprazole lauroxil (the prodrug in ARISTADA) is approximately 54 days (range 29-74 days) after IM injection, allowing monthly dosing.
Terminal elimination half-life is approximately 19–23 days for brexpiprazole and its major metabolite DM-3411, requiring up to 2–3 months to reach steady state.
Primarily renally excreted (approximately 60% as metabolites, <1% unchanged). Fecal elimination accounts for about 20%.
Approximately 25% of the dose is excreted in urine as unchanged drug and metabolites; about 54% is excreted in feces. Renal excretion of unchanged drug is minor (<1%).
Category C
Category C
Atypical Antipsychotic
Atypical Antipsychotic