EVT-201

EVT-201 is a benzodiazepine derivative drug and partial positive allosteric modulator of the benzodiazepine site of the GABAA receptor.[1] It has 2–4-fold higher functional affinity for the α1 subunit relative to the α2, α3, and α5 subunits and significantly less intrinsic activity in comparison to currently-marketed benzodiazepines and the Z-drugs.[2] Despite the lower efficacy, EVT-201 still shows effectiveness in the treatment of insomnia, and it is thought that the lower efficacy may result in fewer side effects, such as motor incoordination.[2] The drug 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.[2] As of 2007, EVT-201 has completed phase II clinical trials for this indication, with positive findings reported.[3] As of August 2015, Phase II development is ongoing in China.[4]

EVT-201
Clinical data
ATC code
  • None
Identifiers
  • 7-Chloro-3-{5-[(dimethylamino)methyl]-1,2,4-oxadiazol-3-yl}-5-methyl-4,5-dihydro-6H-imidazo[1,5-a][1,4]benzodiazepin-6-one
CAS Number
PubChem CID
ChemSpider
UNII
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

See also

References
  1. Guilleminault C (2010). Sleep Medicine. Elsevier Health Sciences. pp. 574–. ISBN 978-1-4377-1836-2.
  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.
  3. 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.
  4. "Drug Profile: EVT 201". AdisInsight. Adis International Ltd, part of Springer Science+Business Media. Retrieved 30 November 2015.


This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.