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Drug Discovery Case History

The Preclinical and Clinical Effects of Vilazodone for the Treatment of Major Depressive Disorder

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Pages 515-523 | Received 20 Oct 2015, Accepted 26 Feb 2016, Published online: 16 Mar 2016

References

  • World Health Organization. Depression Fact sheet No. 369 [updated 2012 October]. Available from: http://www.who.int/mediacentre/factsheets/fs369/en/
  • Kessler RC, Chiu WT, Demler O, et al. Prevalence, severity, and comorbidity of 12-month DSM-IV disorders in the National Comorbidity Survey Replication. Arch Gen Psychiatry. 2005;62(6):617–627.
  • American Psychiatric Association. Diagnostic and statistical manual of mental disorders: DSM 5. Arlington, VA: American Psychiatric Association; 2013.
  • Sullivan PF, Neale MC, Kendler KS. Genetic epidemiology of major depression: review and meta-analysis. Am J Psychiatry. 2000;157(10):1552–1562.
  • Hasler G. Pathophysiology of depression: do we have any solid evidence of interest to clinicians? World Psychiatry. 2010;9(3):155–161.
  • Richelson E. Serotonin: and what about its side effects? Depress Anxiety. 1998;7(Suppl 1):18–20.
  • Blier P. Norepinephrine and selective norepinephrine reuptake inhibitors in depression and mood disorders: their pivotal roles. J Psychiatry Neurosci. 2001;26(Suppl):S1–2.
  • Goldstein DJ, Mallinckrodt C, Lu Y, et al. Duloxetine in the treatment of major depressive disorder: a double-blind clinical trial. J Clin Psychiatry. 2002;63(3):225–231.
  • Hirschfeld RM. The epidemiology of depression and the evolution of treatment. J Clin Psychiatry. 2012;73(Suppl 1):5–9.
  • Berger M, Gray JA, Roth BL. The expanded biology of serotonin. Annu Rev Med. 2009;60:355–366.
  • Stahl SM. Stahl’s essential psychopharmacology: neuroscientific basis and practical applications. New York (NY): Cambridge University Press; 2013.
  • Mann JJ. The serotonergic system in mood disorders and suicidal behaviour. Philos Trans R Soc London B Biol Sci. 2013;368(1615):20120537.
  • Owens MJ, Nemeroff CB. Role of serotonin in the pathophysiology of depression: focus on the serotonin transporter. Clin Chem. 1994;40(2):288–295.
  • Van Praag HM. Depression, suicide and the metabolism of serotonin in the brain. J Affect Disord. 1982;4(4):275–290.
  • Delgado PL, Charney DS, Price LH, et al. Serotonin function and the mechanism of antidepressant action: reversal of antidepressant-induced remission by rapid depletion of plasma tryptophan. Arch Gen Psychiatry. 1990;47(5):411–418.
  • Shopsin B, Friedman E, Gershon S. Parachlorophenylalanine reversal of tranylcypromine effects in depressed patients. Arch Gen Psychiatry. 1976;33(7):811–819.
  • Charney DS. Monamine dysfunction and the pathophysiology and treatment of depression. J Clin Psychiatry. 1998;59(Suppl 14):11–14.
  • Hirschfeld R. History and evolution of the monoamine hypothesis of depression. J Clin Psychiatry. 2000;61(Suppl 6):4–6.
  • Glazer WM. A new antidepressant. Behav Healthc. 2011;31(6):39–40.
  • Maes M, Meltzer HY. The serotonin hypothesis of major depression. In: Bloom FE, Kupfer DJ, editors. Psychopharmacology: the fourth generation of progress. New York, NY: Raven Press; 1995. p. 933–944.
  • Singh M, Schwartz TL. Clinical utility of vilazodone for the treatment of adults with major depressive disorder and theoretical implications for future clinical use. Neuropsychiatr Dis Treat. 2012;8:123.
  • Sprouse JS, Aghajanian GK. Electrophysiological responses of serotoninergic dorsal raphe neurons to 5-HT1A and 5-HT1B agonists. Synapse. 1987;1(1):3–9.
  • Blier P, De Montigny C. Modification of 5-HT neuron properties by sustained administration of the 5-HT1A agonist gepirone: electrophysiological studies in the rat brain. Synapse. 1987;1(5):470–480.
  • Invernizzi R, Belli S, Samanin R. Citalopram’s ability to increase the extracellular concentrations of serotonin in the dorsal raphe prevents the drug’s effect in the frontal cortex. Brain Res. 1992;584(1):322–324.
  • Bel N, Artigas F. Fluvoxamine preferentially increases extracellular 5-hydroxytryptamine in the raphe nuclei: an in vivo microdialysis study. Eur J Pharmacol. 1992;229(1):101–103.
  • Quinaux N, Scuvée-Moreau J, Dresse A. Inhibition of in vitro and ex vivo uptake of noradrenaline and 5-hydroxytryptamine by five antidepressants; correlation with reduction of spontaneous firing rate of central monoaminergic neurones. Naunyn Schmiedebergs Arch Pharmacol. 1982;319(1):66–70.
  • Rollema H, Clarke T, Sprouse JS, et al. Combined administration of a 5-hydroxytryptamine (5-HT) 1D antagonist and a 5-HT reuptake inhibitor synergistically increases 5-HT release in guinea pig hypothalamus in vivo. J Neurochem. 1996;67(5):2204–2207.
  • Hervás I, Queiroz CM, Adell A, et al. Role of uptake inhibition and autoreceptor activation in the control of 5-HT release in the frontal cortex and dorsal hippocampus of the rat. Br J Pharmacol. 2000;130(1):160–166.
  • Bel N, Artigas F. Chronic treatment with fluvoxamine increases extracellular serotonin in frontal cortex but not in raphe nuclei. Synapse. 1993;15(3):243–245.
  • Blier P, De Montigny C. Current advances and trends in the treatment of depression. Trends Pharmacol Sci. 1994;15(7):220–226.
  • Kostowski W, Plaznik A, Stefanski R. Intra-hippocampal buspirone in animal models of anxiety. Eur J Pharmacol. 1989;168(3):393–396.
  • Kusserow H, Davies B, Hortnagl H, et al. Reduced anxiety-related behaviour in transgenic mice overexpressing serotonin 1A receptors. Brain Res Mol Brain Res. 2004;129(1–2):104–116.
  • Ramboz S, Oosting R, Amara DA, et al. Serotonin receptor 1A knockout: an animal model of anxiety-related disorder. Proc Natl Acad Sci U S A. 1998;95(24):14476–14481.
  • Nash JR, Sargent PA, Rabiner EA, et al. Serotonin 5-HT1A receptor binding in people with panic disorder: positron emission tomography study. Br J Psychiatry. 2008;193(3):229–234.
  • Nierenberg AA, Petersen TJ, Alpert JE. Prevention of relapse and recurrence in depression: the role of long-term pharmacotherapy and psychotherapy. J Clin Psychiatry. 2003;64(15):13–17.
  • Khan A. Vilazodone, a novel dual-acting serotonergic antidepressant for managing major depression. Expert Opin Investig Drugs. 2009;18(11):1753–1764.
  • Corruble E, de Bodinat C, Belaidi C, et al. Efficacy of agomelatine and escitalopram on depression, subjective sleep and emotional experiences in patients with major depressive disorder: a 24-wk randomized, controlled, double-blind trial. Int J Neuropsychopharmacol. 2013;16(10):2219–2234.
  • Nierenberg A, Wright E. Evolution of remission as the new standard in the treatment of depression. J Clin Psychiatry. 1998;60:7–11.
  • Thase ME, Entsuah AR, Rudolph RL. Remission rates during treatment with venlafaxine or selective serotonin reuptake inhibitors. Br J Psychiatry. 2001;178(3):234–241.
  • Keller MB, McCullough JP, Klein DN, et al. A comparison of nefazodone, the cognitive behavioral-analysis system of psychotherapy, and their combination for the treatment of chronic depression. N Engl J Med. 2000;342(20):1462–1470.
  • Lindsey WT. Vilazodone for the treatment of depression. Ann Pharmacother. 2011;45(7–8):946–953.
  • Blier P, Bergeron R. Effectiveness of pindolol with selected antidepressant drugs in the treatment of major depression. J Clin Psychopharmacol. 1995;15(3):217–222.
  • Araneda R, Andrade R. 5-Hydroxytryptamine 2 and 5-hydroxytryptamine 1A receptors mediate opposing responses on membrane excitability in rat association cortex. Neuroscience. 1991;40(2):399–412.
  • Kreiss DS, Lucki I. Effects of acute and repeated administration of antidepressant drugs on extracellular levels of 5-hydroxytryptamine measured in vivo. J Pharmacol Exp Ther. 1995;274(2):866–876.
  • Invernizzi R, Bramante M, Samanin R. Role of 5-HT 1A receptors in the effects of acute and chronic fluoxetine on extracellular serotonin in the frontal cortex. Pharmacol Biochem Behav. 1996;54(1):143–147.
  • Romero L, Bel N, Artigas F, et al. Effect of pindolol on the function of pre-and postsynaptic 5-HT 1A receptors: in vivo microdialysis and electrophysiological studies in the rat brain. Neuropsychopharmacol. 1996;15(4):349–360.
  • Hjorth S, Bengtsson H, Kullberg A, et al. Serotonin autoreceptor function and antidepressant drug action. J Psychopharmacol. 2000;14(2):177–185.
  • Artigas F, Romero L, de Montigny C, et al. Acceleration of the effect of selected antidepressant drugs in major depression by 5-HT 1A antagonists. Trends Neurosci. 1996;19(9):378–383.
  • Blier P, Bergeron R. Early onset of therapeutic action in depression and greater efficacy of antidepressant treatments: are they related? Int Clin Psychopharmacol. 1997;12:S21–8.
  • Pérez V, Gilaberte I, Faries D, et al. Randomised, double-blind, placebo-controlled trial of pindolol in combination with fluoxetine antidepressant treatment. Lancet. 1997;349(9065):1594–1597.
  • Rush AJ, Trivedi MH, Wisniewski SR, et al. Acute and longer-term outcomes in depressed outpatients requiring one or several treatment steps: a STAR* D report. Am J Psychiatry. 2006;163(11):1905–1917.
  • Hopkins CR. ACS chemical neuroscience molecule spotlight on viibryd (vilazodone). ACS Chem Neurosci. 2011;2(10):554.
  • Page ME, Detke MJ, Dalvi A, et al. Serotonergic mediation of the effects of fluoxetine, but not desipramine, in the rat forced swimming test. Psychopharmacology. 1999;147(2):162–167.
  • Ashby CR Jr., Kehne JH, Bartoszyk GD, et al. Electrophysiological evidence for rapid 5-HT(1)A autoreceptor inhibition by vilazodone, a 5-HT(1)A receptor partial agonist and 5-HT reuptake inhibitor. Eur J Pharmacol. 2013;714(1–3):359–365.
  • Done C, Sharp T. Biochemical evidence for the regulation of central noradrenergic activity by 5-HT 1A and 5-HT 2 receptors: microdialysis studies in the awake and anaesthetized rat. Neuropharmacology. 1994;33(3):411–421.
  • Suzuki M, Matsuda T, Asano S, et al. Increase of noradrenaline release in the hypothalamus of freely moving rat by postsynaptic 5-hydroxytryptamine1A receptor activation. Br J Pharmacol. 1995;115(4):703–711.
  • Chen NH, Reith ME. Monoamine interactions measured by microdialysis in the ventral tegmental area of rats treated systemically with (±)-8-Hydroxy-2-(Di-n-Propylamino) tetralin. J Neurochem. 1995;64(4):1585–1597.
  • Gobert A, Rivet J-M, Audinot V, et al. Simultaneous quantification of serotonin, dopamine and noradrenaline levels in single frontal cortex dialysates of freely-moving rats reveals a complex pattern of reciprocal auto-and heteroreceptor-mediated control of release. Neuroscience. 1998;84(2):413–429.
  • Hughes ZA, Starr KR, Langmead CJ, et al. Neurochemical evaluation of the novel 5-HT1A receptor partial agonist/serotonin reuptake inhibitor, vilazodone. Eur J Pharmacol. 2005;510(1–2):49–57.
  • Kehne JH, Bartoszyk GD, Greiner HE, editors. In vitro characterization of vilazodone as a dual-acting serotonin reuptake receptor and 5-HT1A receptor partial agonist. Poster presented at: 65th Annual Meeting of the Society of Biological Psychiatry Meeting; 2010.
  • Page ME, Cryan JF, Sullivan A, et al. 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-hydroxytryptamine1A receptor partial agonist. J Pharmacol Exp Ther. 2002;302(3):1220–1227.
  • Adamec R, Bartoszyk GD, Burton P. Effects of systemic injections of vilazodone, a selective serotonin reuptake inhibitor and serotonin 1 A receptor agonist, on anxiety induced by predator stress in rats. Eur J Pharmacol. 2004;504(1):65–77.
  • Treit D, Degroot A, Bartoszyk GD, et al. 68843 injections reduce anxiety in the shock-probe, but not the plus-maze test. Eur J Pharmacol. 2001;414(2):245–248.
  • de Paulis T. Drug evaluation: vilazodone–a combined SSRI and 5-HT1A partial agonist for the treatment of depression. IDrugs. 2007;10(3):193–201.
  • Bartoszyk GD, Hegenbart R, Ziegler H. EMD 68843, a serotonin reuptake inhibitor with selective presynaptic 5-HT 1A receptor agonistic properties. Eur J Pharmacol. 1997;322(2):147–153.
  • Garcia-Garcia A, Banerjee P, Leonardo ED, editors. Acute vilazodone administration induces hypothermia in mice through a 5-HT1A mechanism. Neuropsychopharmacology. 4 Crinan St, London N1 9xw, England: Nature Publishing Group Macmillan Building; 2013.
  • Choi E, Zmarlicka M, Ehret MJ. Vilazodone: A novel antidepressant. Am J Hosp Pharm. 2012;69(18):1551–1557.
  • Edwards J, Sperry V, Adams MH, et al. Vilazodone lacks proarrhythmogenic potential in healthy participants: a thorough ECG study. Int J Clin Pharmacol Ther. 2013;51(6):456–465.
  • Viibryd [prescribing information]. St. Louis, MO: Forest Pharmaceuticals, LLC; 2015.
  • Spina E, Pisani F, Perucca E. Clinically significant pharmacokinetic drug interactions with carbamazepine. Clin Pharmacokinet. 1996;31(3):198–214.
  • Boinpally R, Alcorn H, Adams MH, et al. Pharmacokinetics of vilazodone in patients with mild or moderate renal impairment. Clin Drug Investig. 2013;33(3):199–206.
  • Frampton JE. Vilazodone: in major depressive disorder. CNS Drugs. 2011;25(7):615–627.
  • Owen R. Vilazodone: a new treatment option for major depressive disorder. Drugs Today (Barc). 2011;47(7):531–537.
  • Boinpally R, Gad N, Gupta S, et al. Influence of CYP3A4 induction/inhibition on the pharmacokinetics of vilazodone in healthy subjects. Clin Ther. 2014;36(11):1638–1649.
  • Brown PC. Center for drug evaluation and research: tertiary pharmacology/toxicology review. Washington (DC): U.S. Food and Drug Administration; 2010. Reference ID 2891807 [Viibryd].
  • Rickels K, Athanasiou M, Robinson DS, et al. Evidence for efficacy and tolerability of vilazodone in the treatment of major depressive disorder: a randomized, double-blind, placebo-controlled trial. J Clin Psychiatry. 2009;70(3):326–333.
  • Khan A, Cutler AJ, Kajdasz DK, et al. A randomized, double-blind, placebo-controlled, 8-week study of vilazodone, a serotonergic agent for the treatment of major depressive disorder. J Clin Psychiatry. 2011;72(4):441–447.
  • Rickels K, Athanasiou M, Reed C. Vilazodone, a novel, dual-acting antidepressant: current status, future promise, and potential for individualized treatment of depression. Personalized Med. 2009;6:216–224.
  • Mathews M, Gommoll C, Chen D, et al. Efficacy and safety of vilazodone 20 and 40 mg in major depressive disorder: a randomized, double-blind, placebo-controlled trial. Int Clin Psychopharmacol. 2015;30(2):67–74.
  • Croft HA, Pomara N, Gommoll C, et al. Efficacy and safety of vilazodone in major depressive disorder: a randomized, double-blind, placebo-controlled trial. J Clin Psychiatry. 2014;75(11):e1291–8.
  • Robinson DS, Kajdasz DK, Gallipoli S, et al. A 1-year, open-label study assessing the safety and tolerability of vilazodone in patients with major depressive disorder. J Clin Psychopharmacol. 2011;31(5):643–646.
  • Gommoll C, Durgam S, Mathews M, et al. A double-blind, randomized, placebo-controlled, fixed-dose phase III study of vilazodone in patients with generalized anxiety disorder. Depress Anxiety. 2015;32(6):451–459.
  • Gommoll C, Forero G, Mathews M, et al. Vilazodone in patients with generalized anxiety disorder: a double-blind, randomized, placebo-controlled, flexible-dose study. Int Clin Psychopharmacol. 2015;30(6):297–306.
  • Durgam S, Gommoll C, Forero G, et al. Efficacy and safety of vilazodone in patients with generalized anxiety disorder: a randomized, double-blind, placebo-controlled, flexible-dose trial. J Clin Psychiatry. Forthcoming 2015.
  • Huang SM, Bhattaram A, Mehrotra N, et al. Is this the dose for you?: the role of modeling. Clin Pharmacol Ther. 2013;93(2):159–162.
  • Dopheide JA. Vilazodone’s comparative merits yet to be demonstrated. Am J Hosp Pharm. 2012;69(18):1549.
  • Morganroth J, Thorn M, Gallipoli S, et al. editors. An evaluation of the effect of vilazodone on cardiac safety. Anaheim, CA: American Society of Health-System Pharmacy Midyear Clinical Meeting and Exihibition; 2010.
  • Sachdeva P, Patel B, Patel B. Drug use in pregnancy; a point to ponder! Indian J Pharm Sci. 2009;71(1):1.
  • Chambers CD, Hernandez-Diaz S, Van Marter LJ, et al. Selective serotonin-reuptake inhibitors and risk of persistent pulmonary hypertension of the newborn. N Engl J Med. 2006;354(6):579–587.
  • Chen KC, Yeh TL, Lee IH, et al. Age, gender, depression, and sexual dysfunction in Taiwan. J Sex Med. 2009;6(11):3056–3062.
  • Kennedy SH, Dickens SE, Eisfeld BS, et al. Sexual dysfunction before antidepressant therapy in major depression. J Affect Disord. 1999;56(2–3):201–208.
  • Hull EM, Muschamp JW, Sato S. Dopamine and serotonin: influences on male sexual behavior. Physiol Behav. 2004;83(2):291–307.
  • Clayton AH. The pathophysiology of hypoactive sexual desire disorder in women. Int J Gynaecol Obstet. 2010;110(1):7–11.
  • Pfaus JG. Reviews: Pathways of sexual desire. J Sex Med. 2009;6(6):1506–1533.
  • Sukoff Rizzo SJ, Pulicicchio C, Malberg JE, et al. 5-HT(1A) receptor antagonism reverses and prevents fluoxetine-induced sexual dysfunction in rats. Int J Neuropsychopharmacol. 2009;12(8):1045–1053.
  • Oosting RS, Chan JS, Olivier B, et al. Differential effects of vilazodone versus citalopram and paroxetine on sexual dysfunction and serotonin transporter and receptors in male rats. Psychopharmacol. 2016;233(6):1025–1034.
  • Clayton AH, Kennedy SH, Edwards JB, et al. The effect of vilazodone on sexual function during the treatment of major depressive disorder. J Sex Med. 2013;10(10):2465–2476.
  • Clayton AH, Gommoll C, Chen D, et al. Sexual dysfunction during treatment of major depressive disorder with vilazodone, citalopram, or placebo: results from a phase IV clinical trial. Int Clin Psychopharmacol. 2015;30(4):216–223.
  • Clayton AH, McGarvey EL, Clavet GJ, et al. Comparison of sexual functioning in clinical and nonclinical populations using the Changes in Sexual Functioning Questionnaire (CSFQ). Psychopharmacol Bull. 1997;33(4):747–753.
  • Thase ME, Chen D, Edwards J, et al. Efficacy of vilazodone on anxiety symptoms in patients with major depressive disorder. Int Clin Psychopharmacol. 2014;29(6):351–356.