Drug intelligence / Profile preview

olanzapine + samidorphan l-malate

Development stage
Approved
Lead developer
Alkermes
Modality
Small Molecules
Administration
Oral
01

Overview

Olanzapine + samidorphan l-malate is an oral fixed-dose combination antipsychotic marketed as **LYBALVI** that combines olanzapine, a multi-receptor atypical antipsychotic whose therapeutic activity in schizophrenia and bipolar I disorder is primarily attributed to dopamine and serotonin receptor antagonism, with samidorphan as samidorphan l-malate, an opioid receptor antagonist added to mitigate olanzapine-associated weight gain. The product was developed for adults with schizophrenia and bipolar I disorder, including acute manic or mixed episodes and maintenance treatment in bipolar I disorder. It is supplied as once-daily film-coated bilayer tablets in multiple strengths containing olanzapine with a fixed 10 mg samidorphan component.

Brand names
LYBALVI
Other names
olanzapine + samidorphan l-malateolanzapine and samidorphanolanzapine + samidorphan
02

Targets

HTR2A (Serotonin receptor 5-HT2A)HTR2C (5-hydroxytryptamine 2C receptor)HTR3A (5-hydroxytryptamine receptor 3A)ADRA1A (α1A)DOR (Opioid Receptor Delta 1)DRD1 (Dopamine D1 Receptor)DRD2 (Dopamine D2 Receptor)DRD4 (Dopamine D4 Receptor)HRH1 (Histamine H1 Receptor)KOR (Kappa opioid receptor)MOR (Mu opioid receptor)M1 (Muscarinic acetylcholine receptor M1)CHRM2 (M2)CHRM3 (M3)CHRM4 (M4)CHRM5 (M5)

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