Chemistry:EVT-201
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| Formula | C17H17ClN6O2 |
| Molar mass | 372.81 g·mol−1 |
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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]
See also
References
- ↑ Sleep Medicine. Elsevier Health Sciences. 2010. pp. 574–. ISBN 978-1-4377-1836-2. https://books.google.com/books?id=np1NaFTF_CQC&pg=PA574.
- ↑ 2.0 2.1 2.2 GABA and Sleep: Molecular, Functional and Clinical Aspects. Springer Science & Business Media. 28 September 2010. pp. 50–51. ISBN 978-3-0346-0226-6. https://books.google.com/books?id=u54tqIOP8RUC&pg=PA50.
- ↑ Plunkett's Biotech & Genetics Industry Almanac 2008: Biotech & Genetics Industry Market Research, Statistics, Trends & Leading Companies. Plunkett Research, Ltd.. September 2007. pp. 311–. ISBN 978-1-59392-087-6. https://books.google.com/books?id=3BGBibHJ1FYC&pg=PT311.
- ↑ "Drug Profile: EVT 201". Adis International Ltd, part of Springer Science+Business Media. http://adisinsight.springer.com/drugs/800023883.
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