Share to: share facebook share twitter share wa share telegram print page

Dimdazenil

Dimdazenil
200px
Clinical data
Trade namesJunoenil
Other namesEVT-201
Legal status
Legal status
  • Rx in China
Identifiers
  • 7-Chloro-3-[5-[(dimethylamino)methyl]-1,2,4-oxadiazol-3-yl]-5-methyl-4H-imidazo[1,5-a][1,4]benzodiazepin-6-one
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC17H17ClN6O2
Molar mass372.81 g·mol−1
3D model (JSmol)
  • Clc4cccc3n2cnc(c1nc(on1)CN(C)C)c2CN(C(=O)c34)C
  • InChI=1S/C17H17ClN6O2/c1-22(2)8-13-20-16(21-26-13)15-12-7-23(3)17(25)14-10(18)5-4-6-11(14)24(12)9-19-15/h4-6,9H,7-8H2,1-3H3
  • Key:JCYLWUVDHLVGER-UHFFFAOYSA-N

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.

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

  1. ^ 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.
  2. ^ Guilleminault C (2010). Sleep Medicine. Elsevier Health Sciences. pp. 574–. ISBN 978-1-4377-1836-2.
  3. ^ a b c 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.
  4. ^ Syed YY (March 2024). "Dimdazenil: First Approval". Drugs. doi:10.1007/s40265-024-02020-9. PMID 38546956.
  5. ^ 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.
Kembali kehalaman sebelumnya