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    Overview

    Samidorphan L-malate is the L-malate salt of samidorphan, a potent µ-opioid receptor antagonist (with partial agonist activity at κ- and δ-opioid receptors). It is used in a fixed-dose combination with the antipsychotic olanzapine (e.g., the brand Lybalvi / ALKS 3831).

    Therapeutic class

    Opioid receptor antagonist; used in combination with olanzapine

    Chemical name

    (1R,9R,10S)-17-(cyclopropylmethyl)-3,10-dihydroxy-13-oxo-17-azatetracyclo[7.5.3.0^{1,10}.0^{2,7}]heptadeca-2,4,6-triene-4-carboxamide; (2S)-2-hydroxybutanedioic acid

    Molecular formula

    C25H32N2O9 | Molecular weight: 504.5 g/mol

    Appearance & solubility

    White to almost white powder. Soluble in dimethylformamide and in water.

    Clinical applications

    Samidorphan is combined with olanzapine to mitigate olanzapine-associated weight gain while olanzapine provides treatment for schizophrenia and bipolar I disorder. Samidorphan is not itself an antipsychotic; it is co-administered to improve the tolerability of olanzapine therapy.

    Mode of administration

    Oral (administered as a fixed-dose combination tablet with olanzapine).

    Pharmacological effects

    Samidorphan acts as a µ-opioid receptor antagonist. In combination with olanzapine it is intended to reduce the weight gain associated with olanzapine, an effect attributed to modulation of opioid-mediated pathways involved in appetite and energy regulation.

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