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Anticonvulsant
Zuranolone
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    Zuranolone

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    Zuranolone
    SAGE-217.svg
    Clinical data
    Other names SAGE-217; S-812217; SGE-797; BIIB-125; 3α-Hydroxy-3β-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5β-pregnan-20-one; 3β-Methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-norpregnanolone; 3α-Hydroxy-3β-methyl-5β-dihydro-21-(4-cyano-1H-pyrazol-1'-yl)-19-norprogesterone
    Routes of
    administration    		 By mouth
    Drug class Neurosteroid; GABAA receptor positive allosteric modulator
    Pharmacokinetic data
    Elimination half-life 16–23 hours
    Identifiers
    • 1-(2-((3R,5R,8R,9R,10S,13S,14S,17S)-3-Hydroxy-3,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2-oxoethyl)-1H-pyrazole-4-carbonitrile
    CAS Number
    PubChem CID
    ChemSpider
    UNII
    KEGG
    Chemical and physical data
    Formula C25H35N3O2
    Molar mass 409.574 g·mol−1
    3D model (JSmol)
    • O=C(CN1N=CC(C#N)=C1)[C@H]2CC[C@@]3([H])[C@]4([H])CC[C@]5([H])C[C@](C)(O)CC[C@]5([H])[C@@]4([H])CC[C@@]32C
    • InChI=1S/C25H35N3O2/c1-24(30)9-7-18-17(11-24)3-4-20-19(18)8-10-25(2)21(20)5-6-22(25)23(29)15-28-14-16(12-26)13-27-28/h13-14,17-22,30H,3-11,15H2,1-2H3/t17-,18+,19-,20-,21+,22-,24-,25+/m1/s1
    • Key:HARRKNSQXBRBGZ-GVKWWOCJSA-N

    Zuranolone (INN; developmental code names SAGE-217, S-812217) is an investigational medication which is under development by SAGE Therapeutics for the treatment of depressive disorders and a variety of other indications. It is a synthetic, orally active, inhibitory pregnane neurosteroid, and acts as a positive allosteric modulator of the GABAA receptor. The drug was developed as an improvement on the intravenously-administered neurosteroid brexanolone (allopregnanolone), with high oral bioavailability and a biological half-life suitable for once-daily administration. Its half-life is around 16 to 23 hours, compared to approximately 9 hours for brexanolone. As of December 2022, zuranolone is in preregistration for major depressive disorder and postpartum depression,phase III clinical trials for insomnia, and phase II clinical studies for bipolar depression, essential tremor, and Parkinson's disease. Zuranolone has also been investigated for treatment of dyskinesias and seizures, but no further development has been reported for these indications.

    See also

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