Comparative Pharmacology
Head-to-head clinical analysis: LUMATEPERONE TOSYLATE versus NUPLAZID.
Peer-Reviewed Evidence
Head-to-head clinical analysis: LUMATEPERONE TOSYLATE versus NUPLAZID.
LUMATEPERONE TOSYLATE vs NUPLAZID
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Lumateperone tosylate is an atypical antipsychotic with a unique mechanism of action involving antagonism of serotonin 5-HT2A receptors, partial agonism of serotonin 5-HT1A receptors, and antagonism of dopamine D2 receptors; it also modulates glutamate via phosphorylation of GluN2B subunits and inhibits serotonin reuptake.
Selective serotonin 5-HT2A receptor inverse agonist and antagonist; also has moderate affinity for 5-HT2C and 5-HT1A receptors.
42 mg orally once daily
34 mg orally once daily.
None Documented
None Documented
Terminal elimination half-life is approximately 24-29 hours, allowing once-daily dosing. Steady-state reached in about 5 days.
Terminal elimination half-life is approximately 50 hours (range 40-70 hours), allowing once-daily dosing.
Approximately 60% excreted in urine as metabolites (unchanged drug negligible) and 30% in feces via biliary elimination.
Fecal (approximately 60%) as unchanged drug and metabolites; renal (approximately 13%) as unchanged drug and metabolites.
Category C
Category C
Atypical Antipsychotic
Atypical Antipsychotic