|Trade names||Trintellix, Brintellix|
|By mouth (film-coated tablets)|
|Bioavailability||75% (peak at 7–11 hours)|
|Metabolism||Extensive hepatic, primarily CYP2D6-mediated oxidation|
|Elimination half-life||66 hours|
|Excretion||59% in urine, 26% in feces|
|Chemical and physical data|
|Molar mass||298.45 g/mol (379.36 as hydrobromide)|
|3D model (JSmol)|
Vortioxetine is an antidepressant medication that is prescribed to treat depression. It purportedly relieves depression symptoms by increasing serotonin concentrations in the brain, by inhibiting its reuptake in the synapse and by modulating (activating certain receptors while blocking, or antagonizing, others) certain serotonin receptors. This puts it in the class of atypical antidepressants known as serotonin modulators and stimulators. It is made by the pharmaceutical companies Lundbeck and Takeda.
Vortioxetine is used as a treatment for major depressive disorder.
The most common side effects reported with vortioxetine are nausea, diarrhea, dry mouth, constipation, vomiting, flatulence, dizziness, and sexual dysfunction. Vortioxetine used alone in high dose or in combination with other medications, such as other antidepressants, can produce a potentially life-threatening drug reaction known as serotonin syndrome.
Incidence of sexual dysfunction is higher in patients taking vortioxetine than in people taking placebos but appears to be lower than in people taking most other antidepressants.
Vortioxetine's pKa values are determined to be 9.1 (± 0.1) and 3.0 (± 0.2) according to Australian Public Assessment Report for vortioxetine hydrobromide.
|Ki (nM)||IC50 / EC50 (nM)||IA (%)|
* Human isoforms
Vortioxetine reaches peak plasma concentration (Cmax) within 7 to 11 hours post-administration (Tmax), and its mean terminal half-life (T⁄1/2) is ≈ 66 hours. Steady-state plasma concentrations are typically reached within two weeks. It has no active metabolites (i.e., it is not a prodrug).
Vortioxetine was discovered by scientists at Lundbeck who reported the rationale and synthesis for the drug (then called Lu AA21004) in a 2011 paper.
In 2007, the compound was in Phase II clinical trials, and Lundbeck and Takeda entered into a partnership in which Takeda paid Lundbeck $40 million upfront, with promises of up to $345 million in milestone payments, and Takeda agreed to pay most of the remaining cost of developing the drug. The companies agreed to co-promote the drug in the US and Japan, and that Lundbeck would receive a royalty on all such sales. The deal included another drug candidate, tedatioxetine (Lu AA24530), and could be expanded to include two other Lundbeck compounds.
Vortioxetine was previously trademarked as Brintellix in the United States, but on May 2, 2016, the US FDA approved a name change to Trintellix in order to avoid confusion with the blood-thinning medication Brilinta (ticagrelor).
Vortioxetine has been studied in several clinical trials as a potential treatment for generalized anxiety disorder; however, it has not been shown to be clinically beneficial for this application.
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- US Label Archived 2016-01-31 at the Wayback Machine. Last updated July 2014 after review in September, 2014. Versions of label are available at FDA index page Page accessed January 19, 2016
- Connolly, KR; Thase, ME (2016). "Vortioxetine: a New Treatment for Major Depressive Disorder". Expert opinion on pharmacotherapy. 17 (3): 421–31. doi:10.1517/14656566.2016.1133588. PMID 26679430.
The authors suggest that vortioxetine is currently a good second-line antidepressant option and shows promise, pending additional long-term data, to become a first-line antidepressant option.
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- Stahl, Stephen M. Stahl's Essential Psychopharmacology: Neuroscientific Basis and Practical Applications (4th ed.). Cambridge University Press. ISBN 978-1107686465.
- Sanchez, C; Asin, KE; Artigas, F (2015). "Vortioxetine, a novel antidepressant with multimodal activity: review of preclinical and clinical data". Pharmacol. Ther. 145: 43–57. doi:10.1016/j.pharmthera.2014.07.001. PMID 25016186.
- Daniel Beaulieu for First Word Pharma. September 5th, 2007 Lundbeck, Takeda enter strategic alliance for mood disorder, anxiety drugs Archived 2016-10-10 at the Wayback Machine.
- FDA approves new drug to treat major depressive disorder Archived 2013-10-03 at the Wayback Machine., U.S. Food and Drug Administration Press Announcement.
- EMA Brintellix page at EMA site Archived 2016-01-26 at the Wayback Machine. Page accessed January 19, 2016
- Commissioner, Office of the. "Safety Alerts for Human Medical Products - Brintellix (vortioxetine): Drug Safety Communication - Brand Name Change to Trintellix, to Avoid Confusion With Antiplatelet Drug Brilinta (ticagrelor)". www.fda.gov. Archived from the original on 2016-05-05. Retrieved 2016-05-02.
- Fu, Jie; Peng, Lilei; Li, Xiaogang (2016-04-19). "The efficacy and safety of multiple doses of vortioxetine for generalized anxiety disorder: a meta-analysis". Neuropsychiatric Disease and Treatment. 12: 951–959. doi:10.2147/NDT.S104050. ISSN 1176-6328. PMC 4844447
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