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Vortioxetine

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Vortioxetine
Systematic (IUPAC) name
1-(2-((2,4-dimethylphenyl)thio)phenyl)piperazine
Clinical data
Pregnancy cat.  ?
Legal status Investigational
Identifiers
CAS number 508233-74-7 YesY
ATC code None
ChemSpider 26286009 YesY
Synonyms Lu AA21004; Lu-AA-21004
Chemical data
Formula C18H22N2S
Mol. mass 298.45 g/mol
SMILES eMolecules & PubChem
 YesY(what is this?)  (verify)

Vortioxetine (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] It is a so-called "serotonin modulator and stimulator",[2] and acts as a serotonin transporter blocker (Ki = 1.6 nM), 5-HT1A receptor near-full agonist (Ki = 15 nM; IA = 80%), 5-HT1B receptor partial agonist (Ki = 33 nM), 5-HT3A receptor antagonist (Ki = 3.7 nM), and 5-HT7 receptor antagonist (Ki = 19 nM).[3][4] It also has affinity for the β1-adrenergic receptor (Ki = 46 nM), though its intrinsic activity at this site is not yet known.[3] In 2009, vortioxetine began phase III clinical trials.[1] In a double-blind, randomized, placebo-controlled clinical trial with venlafaxine as an active reference, it was found to be efficacious in treating MDD, while having fewer side effects than its comparator.[5] A New Drug Application (NDA) is not expected to be submitted to the Food and Drug Administration (FDA) until 2012.[6]

[edit] See also

[edit] References

  1. ^ a b 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. 
  2. ^ "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. 
  3. ^ 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. 
  4. ^ 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. 
  5. ^ 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. 
  6. ^ K. Haddley (2011). "LU-AA-21004". Drugs of the Future 36 (8): 577–584. doi:10.1358/dof.2011.36.8.1655803. 



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