Experimental Serotonergic Agents for the Treatment of Schizophrenia

References

• Picchioni MM, Murray RM. Schizophrenia. BMJ. 2007;335(7610):91–95. doi:10.1136/bmj.39227.616447.BE
   PubMed Web of Science ®Google Scholar
• Levine SZ, Lurie I, Kohn R, Levav I. Trajectories of the course of schizophrenia: from progressive deterioration to amelioration over three decades. Schizophr Res. 2011;126:184–191. doi:10.1016/j.schres.2010.10.026
   Web of Science ®Google Scholar
• Silberstein J, Harvey PD. Cognition, social cognition, and Self-assessment in schizophrenia: prediction of different elements of everyday functional outcomes. CNS Spectr. 2019;24(1):88–93. doi:10.1017/S1092852918001414
   PubMed Web of Science ®Google Scholar
• Kasckow JW, Zisook S. Co-occurring depressive symptoms in the older patient with schizophrenia. Drugs Aging. 2008;25(8):631–647. doi:10.2165/00002512-200825080-00002
   Web of Science ®Google Scholar
• Pani L, Pira L, Marchese G. Antipsychotic efficacy: relationship to optimal D2-receptor occupancy. Eur Psychiatry. 2007;22(5):267–275. doi:10.1016/j.eurpsy.2007.02.005
   PubMed Web of Science ®Google Scholar
• Uhl I, Kulik A, Roser P, et al. Central serotonergic function in patients with predominantly negative symptoms of schizophrenia. Schizophr Res. 2018;193:443–444. doi:10.1016/j.schres.2017.05.041
   Web of Science ®Google Scholar
• Krause M, Zhu Y, Huhn M, et al. Antipsychotic drugs for patients with schizophrenia and predominant or prominent negative symptoms: a systematic review and meta-analysis. Eur Arch Psychiatry Clin Neurosci. 2018;268(7):625–639. doi:10.1007/s00406-018-0869-3
   PubMed Web of Science ®Google Scholar
• Buoli M, Kahn RS, Serati M, Altamura AC, Cahn W. Haloperidol versus second-generation antipsychotics in the long-term treatment of schizophrenia. Hum Psychopharmacol. 2016;31(4):325–331. doi:10.1002/hup.2542
   Web of Science ®Google Scholar
• Solmi M, Murru A, Pacchiarotti I, et al. Safety, tolerability, and risks associated with first- and second-generation antipsychotics: a state-of-the-art clinical review. Ther Clin Risk Manag. 2017;13:757–777. doi:10.2147/TCRM.S117321
   PubMed Web of Science ®Google Scholar
• Sullivan LC, Clarke WP, Berg KA. Atypical antipsychotics and inverse agonism at 5-HT2 receptors. Curr Pharm Des. 2015;21(26):3732–3738. doi:10.2174/1381612821666150605111236
   PubMed Web of Science ®Google Scholar
• Leucht S, Corves C, Arbter D, Engel RR, Li C, Davis JM. Second-generation versus first-generation antipsychotic drugs for schizophrenia: a meta-analysis. Lancet. 2009;373(9657):31–41. doi:10.1016/S0140-6736(08)61764-X
   PubMed Web of Science ®Google Scholar
• Nielsen RE, Levander S, Kjaersdam Telléus G, Jensen SO, Østergaard Christensen T, Leucht S. Second-generation antipsychotic effect on cognition in patients with schizophrenia–a meta-analysis of randomized clinical trials. Acta Psychiatr Scand. 2015;131(3):185–196. doi:10.1111/acps.12374
   PubMed Web of Science ®Google Scholar
• Galling B, Vernon JA, Pagsberg AK, et al. Efficacy and safety of antidepressant augmentation of continued antipsychotic treatment in patients with schizophrenia. Acta Psychiatr Scand. 2018;137(3):187–205. doi:10.1111/acps.12854
   PubMed Web of Science ®Google Scholar
• Gregory A, Mallikarjun P, Upthegrove R. Treatment of depression in schizophrenia: systematic review and meta-analysis. BJP. 2017;211(4):198–204. doi:10.1192/bjp.bp.116.190520
   Web of Science ®Google Scholar
• Sepehry AA, Potvin S, Elie R, Stip E. Selective serotonin reuptake inhibitor (SSRI) add-on therapy for the negative symptoms of schizophrenia: a meta-analysis. J Clin Psychiatry. 2007;68(4):604–610. doi:10.4088/jcp.v68n0417
   PubMed Web of Science ®Google Scholar
• Mao YM, Zhang MD. Augmentation with antidepressants in schizophrenia treatment: benefit or risk. Neuropsychiatr Dis Treat. 2015;11:701–713. doi:10.2147/NDT.S62266
   Web of Science ®Google Scholar
• Jones CA, McCreary AC. Serotonergic approaches in the development of novel antipsychotics. Neuropharmacology. 2008;55(6):1056–1065. doi:10.1016/j.neuropharm.2008.05.025
   Web of Science ®Google Scholar
• Davis RE, Correll CU. ITI-007 in the treatment of schizophrenia: from novel pharmacology to clinical outcomes. Expert Rev Neurother. 2016;16(6):601–614. doi:10.1080/14737175.2016.1174577
   PubMed Web of Science ®Google Scholar
• Vanover K, Dmitrienko A, Glass S, et al. S44. Lumateperone (ITI-007) for the treatment of schizophrenia: placebo-controlled clinical trials and an open-label safety switching study. Schizophr Bull. 2018;44(Suppl1):S341. doi:10.1093/schbul/sby018.831
   Web of Science ®Google Scholar
• Blair HA. Lumateperone: first Approval. Drugs. 2020;80(4):417–423. doi:10.1007/s40265-020-01271-6
   PubMed Web of Science ®Google Scholar
• Bruins Slot LA, Kleven MS, Newman-Tancredi A. Effects of novel antipsychotics with mixed D(2) antagonist/5-HT(1A) agonist properties on PCP-induced social interaction deficits in the rat. Neuropharmacology. 2005;49(7):996–1006. doi:10.1016/j.neuropharm.2005.05.013
   PubMed Web of Science ®Google Scholar
• Tadori Y, Kitagawa H, Forbes RA, McQuade RD, Stark A, Kikuchi T. Differences in agonist/antagonist properties at human dopamine D(2) receptors between aripiprazole, bifeprunox and SDZ 208-912. Eur J Pharmacol. 2007;574(2–3):103–111. doi:10.1016/j.ejphar.2007.07.031
   Web of Science ®Google Scholar
• Stahl SM. Essential Psychopharmacology of Antipsychotics and Mood Stabilizers. Cambridge: Cambridge University Press; 2002.
   Google Scholar
• A 6 months double-blind, risperidone-referenced, flexible dose, parallel-group extension study of bifeprunox in patients with schizophrenia. EudraCT number: 2004-002185-38. Available from: https://www.clinicaltrialsregister.eu/ctr-search/trial/2004-002185-38/results. Accessed January 19, 2020.
   Google Scholar
• Lundbeck. A one-year multi-national, multi-centre, randomised, double-blind, parallel-group, fixed-dose bifeprunox study combining a 12-week placebo-controlled, quetiapine-referenced phase with a 12-month quetiapine-controlled phase in patients with schizophrenia. EudraCT number: 2007-001097-90. Available from: https://www.clinicaltrialsregister.eu/ctr-search/trial/2007-001097-90/GR. Accessed January 19, 2020.
   Google Scholar
• A 40-Week Open, Flexible-Dose, Expansion Study of Bifeprunox in Patients with Schizophrenia. EudraCT number: 2004-000707-18. Available from: https://www.cliicaltrialsregister.eu/ctr-search/trial/2004-000707-18/IT. Accessed January 19, 2020.
   Google Scholar
• Lundbeck. An Open-Label Safety Study of Bifeprunox Investigating Flexible Doses of 20, 30, or 40mg/Day in Patients with Schizophrenia Who Have Completed Studies 10206 or 10265. EudraCT Number: 2005-000497-50. Available from: https://www.clinicaltrialsregister.eu/ctr-search/trial/2005-000497-50/IT. Accessed January 19, 2020.
   Google Scholar
• Ye N, Song Z, Zhang A. Dual ligands targeting dopamine D2 and serotonin 5-HT1A receptors as new antipsychotical or anti-Parkinsonian agents. Curr Med Chem. 2014;21(4):437–457. doi:10.2174/09298673113206660300
   Web of Science ®Google Scholar
• Assié MB, Koek W. [(3)H]-8-OH-DPAT binding in the rat brain raphe area: involvement of 5-HT(1A) and non-5-HT(1A) receptors. Br J Pharmacol. 2000;130(6):1348–1352. doi:10.1038/sj.bjp.0703426
   Web of Science ®Google Scholar
• Cassaday HJ, Hodges H, Gray JA. The effects of ritanserin, RU 24969 and 8-OH-DPAT on latent inhibition in the rat. J Psychopharmacol. 1993;7(1Suppl):63–71. doi:10.1177/026988119300700110
   Web of Science ®Google Scholar
• Winstanley CA, Chudasama Y, Dalley JW, Theobald DE, Glennon JC, Robbins TW. Intra-prefrontal 8-OH-DPAT and M100907 improve visuospatial attention and decrease impulsivity on the five-choice serial reaction time task in rats. Psychopharmacology. 2003;167(3):304–314. doi:10.1007/s00213-003-1398-x
   Web of Science ®Google Scholar
• Gogos A, Kusljic S, van den Buuse M. 8-OH-DPAT-induced effects on prepulse inhibition: pre- vs. post-synaptic 5-HT1A receptor activation. Pharmacol Biochem Behav. 2005;81(3):664–672. doi:10.1016/j.pbb.2005.05.007
   Web of Science ®Google Scholar
• Pompeu TE, Alves FR, Figueiredo CD, et al. Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579. Eur J Med Chem. 2013;66:122–134. doi:10.1016/j.ejmech.2013.05.027
   PubMed Web of Science ®Google Scholar
• Neves G, Antonio CB, Betti AH, et al. New insights into pharmacological profile of LASSBio-579, a multi-target N-phenylpiperazine derivative active on animal models of schizophrenia. Behav Brain Res. 2013;237:86–95. doi:10.1016/j.bbr.2012.09.016
   Web of Science ®Google Scholar
• Catafau AM, Bullich S, Nucci G, Burgess C, Gray F, Merlo-Pich E, Barcelona Clinical Imaging in Psychiatry Group. Contribution of SPECT measurements of D2 and 5-HT2A occupancy to the clinical development of the antipsychotic SB-773812. J Nucl Med. 2011;52(4):526–534. doi:10.2967/jnumed.110.081885
   Web of Science ®Google Scholar
• Gsk. A Multi Centre, Double-Blind, Double-Dummy, Placebo-Controlled, Randomised, Adaptive, Dose-Range Study to Evaluate the Safety and Efficacy of SB-773812 Administered Once Daily for 12 Weeks in Adults with Schizophrenia. EudraCT number: 2005-002883-27. Available from: https://www.clinicaltrialsregister.eu/ctr-search/trial/2005-002883-27/results. Accessed January 19, 2020.
   Google Scholar
• ACADIA Pharmaceuticals Advances AM-831 to Phase I Clinical Development in Collaboration with Meiji Seika Pharma. 2011. Available from: http://phxcorporate-irnet. Accessed January 19, 2020.
   Google Scholar
• ACADIA Pharmaceuticals. AM 831. Available from: https://adisinsight.springer.com/drugs/800016551. Accessed January 19, 2020.
   Google Scholar
• Citrome L. A review of the pharmacology, efficacy and tolerability of recently approved and upcoming oral antipsychotics: an evidence-based medicine approach. CNS Drugs. 2013;27(11):879–911. doi:10.1007/s40263-013-0105-7
   PubMed Web of Science ®Google Scholar
• Lundbeck. A 6-Month, Randomised, Double-Blind, Parallel-Group, Risperidone-Controlled, Fixed-Dose Study Evaluating the Safety and Efficacy of Zicronapine in Patients with Schizophrenia. EudraCT Number: 2010-022181-28. Available from: https://www.clinicaltrialsregister.eu/ctr-search/trial/2010-022181-28/EE. Accessed January 19, 2020.
   Google Scholar
• Liu J, Ogden A, Comery TA, Spiros A, Roberts P, Geerts H. Prediction of Efficacy of Vabicaserin, a 5-HT2C agonist, for the treatment of schizophrenia using a quantitative systems pharmacology model. CPT Pharmacometrics Syst Pharmacol. 2014;3(4):e111. doi:10.1038/psp.2014.7
   Google Scholar
• Pfizer. Study Evaluating Vabicaserin in Subjects with Schizophrenia. NLM identifier: NCT00563706. Available from: https://clinicaltrials.gov/ct2/show/NCT00563706. Accessed January 19, 2020.
   Google Scholar
• Yamazaki M, Okabe M, Yamamoto N, Yarimizu J, Harada K. Novel 5-HT5A receptor antagonists ameliorate scopolamine-induced working memory deficit in mice and reference memory impairment in aged rats. J Pharmacol Sci. 2015;127(3):362–369. doi:10.1016/j.jphs.2015.02.006
   Web of Science ®Google Scholar
• Yamazaki M, Harada K, Yamamoto N, et al. ASP5736, a novel 5-HT5A receptor antagonist, ameliorates positive symptoms and cognitive impairment in animal models of schizophrenia. Eur Neuropsychopharmacol. 2014;24(10):1698–1708. doi:10.1016/j.euroneuro.2014.07.009
   Web of Science ®Google Scholar
• Popik P, Krawczyk M, Kuziak A, et al. Serotonin type 5A receptor antagonists inhibit D-lysergic acid diethylamide discriminatory cue in rats. J Psychopharmacol. 2019;33(11):1447–1455. doi:10.1177/0269881119867603
   Web of Science ®Google Scholar
• Thomas DR, Soffin EM, Roberts C, et al. SB-699551-A (3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[(4ʹ-{[(2-phenylethyl)amino]methyl}-4-biphenylyl)methyl]propanamide dihydrochloride), a novel 5-ht5A receptor-selective antagonist, enhances 5-HT neuronal function: evidence for an autoreceptor role for the 5-ht5A receptor in guinea pig brain. Neuropharmacology. 2006;51(3):566–577. doi:10.1016/j.neuropharm.2006.04.019
   Web of Science ®Google Scholar
• Ivachtchenko AV, Lavrovsky Y, Ivanenkov YA. AVN-211, novel and highly selective 5-HT6 receptor small molecule antagonist, for the treatment of alzheimer’s disease. Mol Pharm. 2016;13(3):945–963. doi:10.1021/acs.molpharmaceut.5b00830
   Web of Science ®Google Scholar
• Morozova MA, Lepilkina TA, Rupchev GE, et al. Add-on clinical effects of selective antagonist of 5HT6 receptors AVN-211 (CD-008-0173) in patients with schizophrenia stabilized on antipsychotic treatment: pilot study. CNS Spectr. 2014;19(4):316–323. doi:10.1017/S1092852913000394
   Web of Science ®Google Scholar
• Avineuro, pharmaceuticals. Available from: www.avineuro.com. Accessed January 19, 2020.
   Google Scholar
• Arnt J, Bang-Andersen B, Grayson B, et al. Lu AE58054, a 5-HT6 antagonist, reverses cognitive impairment induced by subchronic phencyclidine in a novel object recognition test in rats. Int J Neuropsychopharmacol. 2010;13(8):1021–1033. doi:10.1017/S1461145710000659
   PubMed Web of Science ®Google Scholar
• Lundbeck. A Randomised, Double-Blind, Parallel-Group, Fixed-Dose Study Exploring the Efficacy and Safety of Lu AE58054 as Augmentation Therapy to Risperidone in Patients with Schizophrenia. EudraCT Number: 2008-001441-26. Available from: https://www.clinicaltrialsregister.eu/ctr-search/trial/2008-001441-26/IT. Accessed January 19, 2020.
   Google Scholar
• Idalopirdine. https://www.alzforum.org/therapeutics/idalopirdine. Accessed January 19, 2020.
   Google Scholar
• Leysen JE, Gommeren W, Van Gompel P, Wynants J, Janssen PF, Laduron PM. Receptor-binding properties in vitro and in vivo of ritanserin: A very potent and long acting serotonin-S2 antagonist. Mol Pharm. 1985;27(6):600–611.
   Web of Science ®Google Scholar
• Lundbeck updates on clinical phase III study for Lu AF35700 in Treatment-Resistant Schizophrenia. Available from:https://investor.lundbeck.com/news-releases/news-release-details/lundbeck-updates-clinical-phase-iii-study-lu-af35700-treatment. ( Valby, Oct. 25, 2018)
   Google Scholar
• Lundbeck. Efficacy of Lu AF35700 in Patients with Early-In-Disease or Late-In-Disease Treatment-Resistant Schizophrenia (Anew). NLM identifier: NCT03230864. Available from: https://clinicaltrials.gov/ct2/show/NCT03230864. Accessed January 19, 2020.
   Google Scholar
• Cantillon M, Prakash A, Alexander A, Ings R, Sweitzer D, Bhat L. Dopamine serotonin stabilizer RP5063: a randomized, double-blind, placebo-controlled multicenter trial of safety and efficacy in exacerbation of schizophrenia or schizoaffective disorder. Schizophr Res. 2017;189:126–133. doi:10.1016/j.schres.2017.01.043
   Web of Science ®Google Scholar
• Cantillon M, Ings R, Bhat L. Initial Clinical Experience of RP5063 following single doses in normal healthy volunteers and multiple doses in patients with stable schizophrenia. Clin Transl Sci. 2018;11(4):387–396. doi:10.1111/cts.12545
   Web of Science ®Google Scholar
• Reviva pharmaceuticals. RP5063 in Subjects with Schizophrenia or Schizoaffective Disorder (REFRESH). NLM identifier: NCT01490086. Available from: https://clinicaltrials.gov/ct2/show/NCT01490086. Accessed January 19, 2020.
   Google Scholar
• Reviva pharmaceuticals clinical trials. Available from: http://revivapharma.com/clinical-trails. Accessed January 19, 2020.
   Google Scholar
• Frankle WG, Lombardo I, Kegeles LS, et al. Serotonin 1A receptor availability in patients with schizophrenia and schizo-affective disorder: a positron emission tomography imaging study with [11C]WAY 100635. Psychopharmacology. 2006;189(2):155–164. doi:10.1007/s00213-006-0543-8
   Web of Science ®Google Scholar
• Meltzer HY, Li Z, Kaneda Y, Ichikawa J. Serotonin receptors: their key role in drugs to treat schizophrenia. Prog Neuropsychopharmacol Biol Psychiatry. 2003;27(7):1159–1172. doi:10.1016/j.pnpbp.2003.09.010
   PubMed Web of Science ®Google Scholar
• Burnet PW, Eastwood SL, Harrison PJ. 5-HT1A and 5-HT2A receptor mRNAs and binding site densities are differentially altered in schizophrenia. Neuropsychopharmacology. 1996;15(5):442–455. doi:10.1016/S0893-133X(96)00053-X
   PubMed Web of Science ®Google Scholar
• Pogorelov VM, Rodriguiz RM, Cheng J, et al. 5-HT2C agonists modulate schizophrenia-like behaviors in mice. Neuropsychopharmacology. 2017;42(11):2163–2177. doi:10.1038/npp.2017.52
   PubMed Web of Science ®Google Scholar
• Gonzalez R, Chávez-Pascacio K, Meneses A. Role of 5-HT5A receptors in the consolidation of memory. Behav Brain Res. 2013;252:246–251. doi:10.1016/j.bbr.2013.05.051
   Web of Science ®Google Scholar
• de Bruin NM, Kruse CG. 5-HT6 receptor antagonists: potential efficacy for the treatment of cognitive impairment in schizophrenia. Curr Pharm Des. 2015;21(26):3739–3759. doi:10.2174/1381612821666150605112105
   PubMed Web of Science ®Google Scholar
• Woods S, Clarke NN, Layfield R, Fone KC. 5-HT(6) receptor agonists and antagonists enhance learning and memory in a conditioned emotion response paradigm by modulation of cholinergic and glutamatergic mechanisms. Br J Pharmacol. 2012;167(2):436–449. doi:10.1111/j.1476-5381.2012.02022.x
   Web of Science ®Google Scholar
• Mauri MC, Paletta S, Maffini M, et al. Clinical pharmacology of atypical antipsychotics: an update. EXCLI J. 2014;13:1163–1191.
   PubMed Web of Science ®Google Scholar
• Korcsmáros T, Szalay MS, Böde C, Kovács IA, Csermely P. How to design multi-target drugs. Expert Opin Drug Discov. 2007;2(6):799–808. doi:10.1517/17460441.2.6.799
   PubMed Web of Science ®Google Scholar
• Correll CU, Kishimoto T, Kane JM. Randomized controlled trials in schizophrenia: opportunities, limitations, and trial design alternatives. Dialogues Clin Neurosci. 2011;13(2):155–172.
   PubMedGoogle Scholar
• Liberati A, Altman D, Tetzlaff J, et al. The PRISMA statement for reporting systematic reviews and meta-analyses of studies that evaluate health care interventions: explanation and elaboration. Journal of clinical epidemiology. 2009;62(10).
   Google Scholar