Dimdazenil
Dimdazenil (trade name Junoenil) is a pharmaceutical drug for insomnia.[1] It is a benzodiazepine derivative and a partial positive allosteric modulator of the GABAA receptor[2] with two- to four-fold higher functional affinity for the α1 subunit relative to the α2, α3, and α5 subunits.
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| Trade names | Junoenil |
| Other names | EVT-201 |
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| Formula | C17H17ClN6O2 |
| Molar mass | 372.81 g·mol−1 |
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Medical use
Dimdezenil shows effectiveness in the treatment of insomnia, but has less intrinsic activity in comparison to currently-marketed benzodiazepines and the Z-drugs;[3] however, it is thought that the lower efficacy may result in fewer side effects, such as motor incoordination.[3] In China, dimdezenil is approved for short-term treatment of insomnia.[4]
History
Dimdezenil was originally developed by Roche, based on preclinical data, as a non-sedating anxiolytic, but was found to produce sedation in humans in phase I clinical trials. For this reason, it was subsequently licensed to Evotec, which is now developing it for the treatment of insomnia.[3] By 2007, dimdezenil completed phase II clinical trials for this indication, with positive findings reported.[5] In China, the drug was developed by Zhejiang Jingxin Pharmaceutical.
References
- Huang Z, Zhan S, Chen C, Zhang R, Zhou Y, He J, et al. (February 2024). "Efficacy and safety of Dimdazenil in adults with insomnia disorder: results from a multicenter, randomized, double-blind, placebo-controlled phase III trials". Sleep. 47 (2). doi:10.1093/sleep/zsad272. PMC 10851846. PMID 37875349.
{{cite journal}}: CS1 maint: overridden setting (link) - Guilleminault C (2010). Sleep Medicine. Elsevier Health Sciences. pp. 574–. ISBN 978-1-4377-1836-2.
- Monti JM, Pandi-Perumal SR, Möhler H (28 September 2010). GABA and Sleep: Molecular, Functional and Clinical Aspects. Springer Science & Business Media. pp. 50–51. ISBN 978-3-0346-0226-6.
- Syed YY (March 2024). "Dimdazenil: First Approval". Drugs. doi:10.1007/s40265-024-02020-9. PMID 38546956.
- Plunkett JW (September 2007). Plunkett's Biotech & Genetics Industry Almanac 2008: Biotech & Genetics Industry Market Research, Statistics, Trends & Leading Companies. Plunkett Research, Ltd. pp. 311–. ISBN 978-1-59392-087-6.