Vortioxetine
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Vortioxetine
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| Systematic (IUPAC) name | |
| 1-(2-((2,4-dimethylphenyl)thio)phenyl)piperazine | |
| Clinical data | |
| Pregnancy cat. | ? |
| Legal status | Investigational New Drug |
| Routes | Oral |
| Identifiers | |
| CAS number | 508233-74-7  |
| ATC code | None |
| PubChem | CID 9966051 |
| ChemSpider | 26286009 |
| Synonyms | Lu AA21004 |
| Chemical data | |
| Formula | C18H22N2S |
| Mol. mass | 298.45 g/mol |
| SMILES | eMolecules & PubChem |
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Vortioxetine (code name Lu AA21004) is an experimental drug currently under development by Lundbeck and Takeda for the treatment of major depressive disorder (MDD) and generalized anxiety disorder (GAD).[1]
Phase III clinical development is nearly finished and submission of marketing authorization for the treatment of MDD is planned during the second half of 2012, both in the United States and Canada and in Europe.[2]
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Contents
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Efficacy
In May 2011, Lundbeck presented the results of four phase III trials on vortioxetine at the 2011 Annual Meeting of the American Psychiatric Association. A significant effect was shown in two of the studies (one for active treatment using the Hamilton Depression Rating Scale (HAM-D), the second as a maintenance treatment), vortioxetine failed to prove superiority over placebo in a third (again using the HAM-D) and the fourth was nullified by an exceptionally high placebo response (according to the Montgomery-Åsberg Depression Rating Scale (MADRS)).[3]
In July 2011, Lundbeck published the results of a double-blind, randomized, placebo-controlled clinical trial with venlafaxine as an active reference. It was found to be superior to placebo in treating MDD while having fewer side effects than venlafaxine.[4] Similarly, in May 2012, Lundbeck published the results of a double-blind, randomized, placebo-controlled clinical trial with duloxetine evaluating vortioxetine in elderly depressed patients, and it was found superior to placebo, with fewer side effects than duloxetine.[5]
In May 2012, Lundbeck disclosed the results of three phase III clinical trials, showing Vortioxetine's superiority over placebo according to the MADRS.[2]
Side effects
The most common side effects reported with vortioxetine are nausea, vomiting, diarrhea, headache, and dizziness.[2][3][5]
Incidence of sexual dysfunction is reportedly lower than with venlafaxine.[4]
Pharmacology
Vortioxetine is a so-called "serotonin modulator and stimulator".[6] It has been shown to possess the following pharmacological actions:[7][8]
- Serotonin transporter (SERT) blocker (Ki = 1.6 nM) (or serotonin reuptake inhibitor (SRI))
- 5-HT1A receptor high-efficacy partial agonist/near-full agonist (Ki = 15 nM; IA = 80%)
- 5-HT1B receptor partial agonist (Ki = 33 nM)
- 5-HT3A receptor antagonist (Ki = 3.7 nM)
- 5-HT7 receptor antagonist (Ki = 19 nM)
Vortioxetine also has affinity for the β1-adrenergic receptor (Ki = 46 nM), though any actions at this site are unlikely to contribute to its therapeutic effects and likely only to contribute to side effects.[7]
See also
References
- ^ Jancin B (December 2009). "Lu AA21004 Looks Promising for Depression". Clinical Psychiatry News 37 (12): 24–25. doi:10.1016/S0270-6644(09)70441-2. http://www.clinicalpsychiatrynews.com/article/S0270-6644(09)70441-2/preview.
- ^ a b c http://www.fiercebiotech.com/press-releases/statistically-significant-clinical-phase-iii-results-lu-aa21004-provide-bas
- ^ a b http://investor.lundbeck.com/releasedetail.cfm?ReleaseID=608559
- ^ a b Alvarez E, Perez V, Dragheim M, Loft H, Artigas F (July 2011). "A double-blind, randomized, placebo-controlled, active reference study of Lu AA21004 in patients with major depressive disorder". The International Journal of Neuropsychopharmacology / Official Scientific Journal of the Collegium Internationale Neuropsychopharmacologicum (CINP): 1–12. doi:10.1017/S1461145711001027. PMID 21767441. http://journals.cambridge.org/abstract_S1461145711001027.
- ^ a b Katona C, Hansen T, Olsen Ck (May (epub) 2012). "A randomized, double-blind, placebo-controlled, duloxetine-referenced, fixed-dose study comparing the efficacy and safety of Lu AA21004 in elderly patients with major depressive disorder". International clinical psychopharmacology. PMID 22572889.
- ^ "Lundbeck's "Serotonin Modulator and Stimulator" Lu AA21004: How Novel? How Good? - GLG News". http://www.glgroup.com/News/Lundbecks-Serotonin-Modulator-and-Stimulator-Lu-AA21004--How-Novel--How-Good--17944.html.
- ^ a b Bang-Andersen B, Ruhland T, Jørgensen M, et al. (May 2011). "Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenylpiperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder"]. Journal of Medicinal Chemistry 54 (9): 3206–21. doi:10.1021/jm101459g. PMID 21486038. http://dx.doi.org/10.1021/jm101459g.
- ^ N. Moore; B. Bang-Andersen; L. Brennum; K. Fredriksen; S. Hogg; A. Mork; T. Stensbol; H. Zhong; C. Sanchez; D. Smith (August 2008). "Lu AA21004: a novel potential treatment for mood disorders". European Neuropsychopharmacology 18 (Supplement 4): S321. doi:10.1016/S0924-977X(08)70440-1. http://linkinghub.elsevier.com/retrieve/pii/S0924977X08704401.
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