Comparative Pharmacology
Head-to-head clinical analysis: LURASIDONE HYDROCHLORIDE versus SAPHRIS.
Head-to-head clinical analysis: LURASIDONE HYDROCHLORIDE versus SAPHRIS.
LURASIDONE HYDROCHLORIDE vs SAPHRIS
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Lurasidone is an atypical antipsychotic that acts as a full antagonist at D2 and 5-HT2A receptors, with high affinity for 5-HT7 and 5-HT1A receptors, moderate affinity for alpha2C and alpha2A adrenergic receptors, and no appreciable affinity for H1, M1, or alpha1 receptors.
Asenapine is an atypical antipsychotic with high affinity for serotonin 5-HT2A, 5-HT2C, 5-HT6, and 5-HT7 receptors; dopamine D2, D3, and D4 receptors; and alpha2-adrenergic receptors. It also has moderate affinity for histamine H1 and alpha1-adrenergic receptors, and low affinity for muscarinic M1 receptors.
40 mg orally once daily initially, titrated to 80 mg once daily; maximum 80 mg per day.
5 mg sublingually twice daily, may increase to 10 mg twice daily based on tolerability and efficacy.
None Documented
None Documented
Terminal elimination half-life is approximately 18 hours (range 14–24 hours), supporting once-daily dosing.
Terminal elimination half-life is 30-40 hours, supporting once-daily dosing.
Approximately 80% of total radioactivity recovered in feces (67% as metabolites, 9% as unchanged drug) and 19% in urine (mostly metabolites); less than 1% excreted as unchanged parent in urine.
After oral administration, approximately 50% of the dose is excreted in urine (mostly as metabolites, <1% unchanged) and 40% in feces (mostly as metabolites).
Category A/B
Category C
Atypical Antipsychotic
Atypical Antipsychotic