Chemistry:SAGE-217
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| Clinical data | |
|---|---|
| Other names | 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 |
| Identifiers | |
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| Chemical and physical data | |
| Formula | C25H35N3O2 |
| Molar mass | 409.273 g/mol g·mol−1 |
| 3D model (JSmol) | |
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SAGE-217 is an investigational medication which is under development by SAGE Therapeutics for the treatment of major depressive disorder, postpartum depression, essential tremor, Parkinson's disease, insomnia, and seizures.[1][2] It is a synthetic, orally active, inhibitory pregnane neurosteroid, and acts as a positive allosteric modulator of the GABAA receptor.[1][2][3] The drug was developed as an improvement of allopregnanolone (brexanolone) with high oral bioavailability and a biological half-life suitable for once-daily administration.[2] As of February 2018, SAGE-217 is in phase II clinical trials for major depressive disorder, postpartum depression, essential tremor, and Parkinson's disease and is in phase I clinical studies for insomnia and seizures.[1] It is also in the preclinical stage of development for dyskinesias.[1]
See also
References
- ↑ 1.0 1.1 1.2 1.3 "SAGE 217". http://adisinsight.springer.com/drugs/800043382. Retrieved 2018-02-10.
- ↑ 2.0 2.1 2.2 "Breakthroughs in neuroactive steroid drug discovery". Bioorg. Med. Chem. Lett. 28 (2): 61–70. 2018. doi:10.1016/j.bmcl.2017.11.043. PMID 29223589.
- ↑ "Neuroactive Steroids. 2. 3α-Hydroxy-3β-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5β-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (γ-Aminobutyric Acid)A Receptor". J. Med. Chem. 60 (18): 7810–7819. 2017. doi:10.1021/acs.jmedchem.7b00846. PMID 28753313.
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