Vilazodone

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Vilazodone
Systematic (IUPAC) name
5-(4-[4-(5-cyano-1H-indol-3-yl)butyl]piperazin-1-yl)benzofuran-2-carboxamide
Clinical data
Trade namesViibryd
AHFS/Drugs.comConsumer Drug Information
MedlinePlusa611020
Licence dataUS FDA:link
Pregnancy cat.C (US)
Legal status-only (US)
RoutesOral
Pharmacokinetic data
Half-life20-24 hours
Identifiers
CAS number163521-12-8 N
ATC codeN06AX24
PubChemCID 6918313
ChemSpider5293518 YesY
UNIIS239O2OOV3 YesY
KEGGD09698 YesY
ChEMBLCHEMBL439849 YesY
Chemical data
FormulaC26H27N5O2 
Mol. mass441.524 g/mol
 N (what is this?)  (verify)
 
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Vilazodone
Systematic (IUPAC) name
5-(4-[4-(5-cyano-1H-indol-3-yl)butyl]piperazin-1-yl)benzofuran-2-carboxamide
Clinical data
Trade namesViibryd
AHFS/Drugs.comConsumer Drug Information
MedlinePlusa611020
Licence dataUS FDA:link
Pregnancy cat.C (US)
Legal status-only (US)
RoutesOral
Pharmacokinetic data
Half-life20-24 hours
Identifiers
CAS number163521-12-8 N
ATC codeN06AX24
PubChemCID 6918313
ChemSpider5293518 YesY
UNIIS239O2OOV3 YesY
KEGGD09698 YesY
ChEMBLCHEMBL439849 YesY
Chemical data
FormulaC26H27N5O2 
Mol. mass441.524 g/mol
 N (what is this?)  (verify)

Vilazodone (United States trade name Viibryd) is a serotonergic antidepressant developed by Clinical Data for the treatment of major depressive disorder. The chemical compound was originally developed by Merck KGaA (Germany).[1] By 2009 two phase III clinical trials with positive results had been completed.[2] Vilazodone was approved by the FDA for use in the United States to treat major depressive disorder in January 21, 2011.[3][4][5]

Contents

Pharmacology

Vilazodone acts as a serotonin reuptake inhibitor (IC50 = 0.5 nM) and 5-HT1A receptor partial agonist (IC50 = 0.2 nM; IA = ~60-70%).[6][7] It has negligible affinity for other serotonin receptors such as 5-HT1D, 5-HT2A, and 5-HT2C.[6][7]

Partial agonism of the 5-HT1A receptor is a relatively novel mechanism of action and is also shared by the anxiolytic buspirone (Buspar), and the atypical antipsychotic / antidepressant aripiprazole (Abilify).

Efficacy and tolerability

Vilazodone is approved in 10 mg, 20 mg, and 40 mg doses.

According to an eight-week, randomized, double-blind, placebo-controlled trial, vilazodone was reported to elicit an antidepressant response after one week of treatment. After eight weeks, subjects assigned to vilazodone experienced a significantly higher response rate than the group given placebo. At a dose of 40 mg per day, it is considered to be well tolerated and reported adverse effects ranged from mild to moderate in intensity; side effects included diarrhea, nausea, and somnolence.[8] In contrast to other SSRIs currently on the market, initial clinical trials showed that vilazodone did not cause significant weight gain or decreased sexual desire/function as with many other antidepressants, which often cause people to abandon their use.[3]

However, FDA staff called these claims into question in a September 2011 article that concluded "it is unknown whether [vilazodone] has any advantages compared to other drugs in the antidepressant class." [9]

See also

References

  1. ^ Clinical Data's Vilazodone Patient Enrollment Over One Third Complete. August 17th, 2006[dead link]
  2. ^ de Paulis T (March 2007). "Drug evaluation: Vilazodone--a combined SSRI and 5-HT1A partial agonist for the treatment of depression". IDrugs : the Investigational Drugs Journal 10 (3): 193–201. PMID 17351874. 
  3. ^ a b "FDA approves Clinical Data Inc's antidepressant". Reuters. January 22, 2011. http://www.reuters.com/article/idUSN2111362920110122. 
  4. ^ "FDA approves Clinical Data Inc's antidepressant". Reuters. January 22, 2011. http://www.reuters.com/article/idUSN2111362920110122. 
  5. ^ "Clinical Data, Inc. - Clinical Data, Inc. Submits New Drug Application for Vilazodone for the Treatment of Major Depressive Disorder". http://investor.clda.com/releasedetail.cfm?ReleaseID=453924. 
  6. ^ a b Page ME, Cryan JF, Sullivan A, et al. (September 2002). "Behavioral and neurochemical effects of 5-(4-[4-(5-Cyano-3-indolyl)-butyl)-butyl-1-piperazinyl)-benzofuran-2-carboxamide (EMD 68843): a combined selective inhibitor of serotonin reuptake and 5-hydroxytryptamine(1A) receptor partial agonist"]. The Journal of Pharmacology and Experimental Therapeutics 302 (3): 1220–7. doi:10.1124/jpet.102.034280. PMID 12183683. http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=12183683. 
  7. ^ a b Hughes ZA, Starr KR, Langmead CJ, et al. (March 2005). "Neurochemical evaluation of the novel 5-HT1A receptor partial agonist/serotonin reuptake inhibitor, vilazodone". European Journal of Pharmacology 510 (1–2): 49–57. doi:10.1016/j.ejphar.2005.01.018. PMID 15740724. http://linkinghub.elsevier.com/retrieve/pii/S0014-2999(05)00041-5. 
  8. ^ Rickels K, Athanasiou M, Robinson DS, Gibertini M, Whalen H, Reed CR (March 2009). "Evidence for efficacy and tolerability of vilazodone in the treatment of major depressive disorder: a randomized, double-blind, placebo-controlled trial". The Journal of Clinical Psychiatry 70 (3): 326–33. PMID 19284933. http://article.psychiatrist.com/?ContentType=START&ID=10003992. 
  9. ^ Laughren TP, Gobburu J, Temple RJ, Unger EF, Bhattaram A, Dinh PV, Fossom L, Hung HM, Klimek V, Lee JE, Levin RL, Lindberg CY, Mathis M, Rosloff BN, Wang SJ, Wang Y, Yang P, Yu B, Zhang H, Zhang L, Zineh I (September 2011). "Vilazodone: clinical basis for the US Food and Drug Administration's approval of a new antidepressant". The Journal of Clinical Psychiatry 72 (9): 1166–73. PMID 21951984. http://www.ncbi.nlm.nih.gov/pubmed/21951984.