Drug intelligence / Profile preview

olanzapine + samidorphan

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

Overview

**Olanzapine + samidorphan** is an oral fixed-dose combination of olanzapine, an atypical antipsychotic, and samidorphan, an opioid receptor modulator. Marketed in the United States as **Lybalvi**, it is approved for adults with schizophrenia and for adults with bipolar I disorder, including acute manic or mixed episodes as monotherapy or adjunctive therapy with lithium or valproate, and maintenance monotherapy. Olanzapine provides antipsychotic activity principally through dopamine and serotonin receptor antagonism, while samidorphan was added to mitigate olanzapine-associated weight gain without materially altering olanzapine exposure. The product is supplied as once-daily bilayer film-coated tablets containing 5 mg, 10 mg, 15 mg, or 20 mg olanzapine with 10 mg samidorphan. ([dailymed.nlm.nih.gov](https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=32ffddd1-4e2b-45d9-9b36-bb730167ec80))

Brand names
Lybalvi
Other names
OLZ/SAMolanzapine + samidorphanolanzapine + samidorphan L-malateolanzapine and samidorphanolanzapine and samidorphan L-malateolanzapine/samidorphan
02

Targets

HTR2A (Serotonin receptor 5-HT2A)HRH1 (Histamine H1 Receptor)mAChR (Muscarinic acetylcholine receptors)ADRA1A (α1A)DRD2 (Dopamine D2 Receptor)MOR (Mu opioid receptor)DOR (Opioid Receptor Delta 1)KOR (Kappa opioid receptor)

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