Iloperidone: chemistry, pharmacodynamics, pharmacokinetics and metabolism, clinical efficacy, safety and tolerability, regulatory affairs, and an opinion

Bibliography

• American Psychiatric Association. Diagnostic and statistical manual of mental disorders DSM-IV-TR, Fourth edition (Text Revision). American Psychiatric Publishing, Inc., Arlington, Virginia; 2000
   Google Scholar
• Volavka J, Citrome L. Oral antipsychotics for the treatment of schizophrenia: heterogeneity in efficacy and tolerability should drive decision-making. Expert Opin Pharmacother 2009;10:1917-28
   PubMed Web of Science ®Google Scholar
• Citrome L. Iloperidone for schizophrenia: a review of the efficacy and safety profile for this newly commercialised second-generation antipsychotic. Int J Clin Pract 2009;63:1237-48
   PubMed Web of Science ®Google Scholar
• Citrome L. Iloperidone redux: a dissection of the drug approval package for this newly commercialised second-generation antipsychotic. Int J Clin Pract 2010;64:707-18
   PubMed Web of Science ®Google Scholar
• Leucht S, Corves C, Arbter D, Second-generation versus first-generation antipsychotic drugs for schizophrenia: a meta-analysis. Lancet 2009;373:31-41
   PubMed Web of Science ®Google Scholar
• Citrome L. Asenapine for schizophrenia and bipolar disorder: a review of the efficacy and safety profile for this newly approved sublingually absorbed second-generation antipsychotic. Int J Clin Pract 2009;63:1762-84
   PubMed Web of Science ®Google Scholar
• Citrome L. Paliperidone palmitate – review of the efficacy, safety and cost of a new second-generation depot antipsychotic medication. Int J Clin Pract 2010;64:216-39
   PubMed Web of Science ®Google Scholar
• Citrome L. Patient perspectives in the development and use of long-acting antipsychotics in schizophrenia: focus on olanzapine long-acting injection. Patient Prefer Adherence 2009;3:345-55
   PubMed Web of Science ®Google Scholar
• Citrome L. Olanzapine pamoate: a stick in time? A review of the efficacy and safety profile of a new depot formulation of a second-generation antipsychotic. Int J Clin Pract 2009;63:140-50
   PubMed Web of Science ®Google Scholar
• Meyer JM, Loebel AD, Schweizer E. Lurasidone: a new drug in development for schizophrenia. Expert Opin Investig Drugs 2009;18:1715-26
   PubMed Web of Science ®Google Scholar
• Otsuka Pharmaceutical Development & Commercialization, Inc., 2008. Intramuscular Depot Formulation of Aripiprazole as Maintenance Treatment in Patients with Schizophrenia (ASPIRE). Available from: http://clinicaltrials.gov/ct2/show/NCT00731549 [Last accessed 7 August 2010]
   Google Scholar
• Patil ST, Zhang L, Martenyi F, Activation of mGlu2/3 receptors as a new approach to treat schizophrenia: a randomized Phase 2 clinical trial. Nat Med 2007;13:1102-7
   PubMed Web of Science ®Google Scholar
• Labrie V, Roder JC. The involvement of the NMDA receptor D-serine/glycine site in the pathophysiology and treatment of schizophrenia. Neurosci Biobehav Rev 2010;34:351-72
   PubMed Web of Science ®Google Scholar
• Vanda Pharmaceuticals. FDA Approves Vanda Pharmaceuticals' Fanapt for the Treatment of Schizophrenia. Press release, 6 May 2009. Available from: http://phx.corporate-ir.net/phoenix.zhtml?c=196233&p=irol-newsArticle&ID=1285454&highlight= [Last accessed 7 August 2010]
   Google Scholar
• Vanda Pharmaceuticals. Vanda Pharmaceuticals Announces Receipt of not Approvable Letter from FDA for Iloperidone. Press release, 28 July 2008. Available from: http://phx.corporate-ir.net/phoenix.zhtml?c=196233&p=irol-newsArticle&ID=1179851&highlight= [Last accessed 7 August 2010]
   Google Scholar
• Vanda Pharmaceuticals. Fanapt (iloperidone) Tablets. Available from: http://www.pharma.us.novartis.com/product/pi/pdf/fanapt.pdf [Last accessed 7 August 2010]
   Google Scholar
• Strupczewski JT, Bordeau KJ, Chiang Y, 3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873). J Med Chem 1995;38:1119-31
   PubMed Web of Science ®Google Scholar
• Novartis. Novartis Enters Into Agreement for Exclusive US and Canadian Rights to Fanapt(TM), an FDA-Approved Oral Therapy for Schizophrenia. Press release, 12 October 2009. Available from: http://www.novartis.com/newsroom/media-releases/en/2009/1346595.shtml [Last accessed 7 August 2010]
   Google Scholar
• Corbett R, Griffiths L, Shipley JE, Iloperidone: preclinical profile and early clinical evaluation. CNS Drug Rev 1997;3:120-47
   Google Scholar
• FDA. Drug Approval Package. Fanapt (Iloperidone) Tablets. 12 June 2009. Available from: http://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022192s000TOC.cfm [Last accessed 7 August 2010]
   Google Scholar
• Stahl SM. Stahl's essential psychopharmacology, Third edition. Cambridge University Press, Cambride; 2008
   Google Scholar
• Shayegan DK, Stahl SM. Atypical antipsychotics: matching receptor profile to individual patient's clinical profile. CNS Spectr 2004;9(Suppl 11):6-14
   PubMed Web of Science ®Google Scholar
• Szewczak MR, Corbett R, Rush DK, The pharmacological profile of iloperidone, a novel atypical antipsychotic agent. J Pharmacol Exp Ther 1995;274:1404-13
   PubMed Web of Science ®Google Scholar
• Kongsamut S, Roehr JE, Cai J, Iloperidone binding to human and rat dopamine and 5-HT receptors. Eur J Pharmacol 1996;317:417-23
   PubMed Web of Science ®Google Scholar
• Kalkman HO, Subramanian N, Hoyer D. Extended radioligand binding profile of iloperidone: a broad spectrum dopamine/serotonin/norepinephrine receptor antagonist for the management of psychotic disorders. Neuropsychopharmacology 2001;25:904-14
   PubMed Web of Science ®Google Scholar
• Kalkman HO, Feuerbach D, Lotscher E, Schoeffter P. Functional characterization of the novel antipsychotic iloperidone at human D2, D3, alpha 2C, 5-HT6, and 5-HT1A receptors. Life Sci 2003;73:1151-9
   PubMed Web of Science ®Google Scholar
• Subramanian N, Kalkman HO. Receptor profile of P88-8991 and P95-12113, metabolites of the novel antipsychotic iloperidone. Prog Neuropsychopharmacol Biol Psychiatry 2002;26:553-60
   PubMed Web of Science ®Google Scholar
• Szczepanik AM, Brougham LR, Roehr JE, Ex vivo studies with iloperidone (HP 873), a potential atypical antipsychotic with dopamine D2/5-hydroxytryptamine2 receptor antagonist activity. J Pharmacol Exp Ther 1996;278:913-20
   PubMed Web of Science ®Google Scholar
• Mack K, Volpi S, Licamele L, Effect of polymorphisms in the dopamine receptor 2 gene on iloperidone efficacy for the treatment of patients with schizophrenia. Poster presentation NR1-058. 162nd Annual Meeting of the American Psychiatric Association; 16 – 21 May 2009; San Francisco, CA
   Google Scholar
• Sainati SM, Hubbard JW, Chi E, Safety, tolerability, and effect of food on the pharmacokinetics of iloperidone (HP 873), a potential atypical antipsychotic. J Clin Pharmacol 1995;35:713-20
   PubMed Web of Science ®Google Scholar
• Wolfgang C. Genotyping facilitates individualized prediction of pharmacokinetic exposure of iloperidone in extensive and poor metabolizers. Poster presentation NR-508. 160th Annual Meeting of the American Psychiatric Association; 19 – 24 May 2007; San Diego, CA, USA
   Google Scholar
• Sedek G, Wolfgang C. Iloperidone is well tolerated by subjects with renal or hepatic impairment in single-dose clinical pharmacokinetic studies. Poster presentation NR-476. 160th Annual Meeting of the American Psychiatric Association; 19 – 24 May 2007; San Diego, CA, USA
   Google Scholar
• Baroldi P, Wolfgang C, Fisher D. A pharmacokinetic (PK)–pharmacodynamic (PD) relationship exists for efficacy of iloperidone, a novel investigational atypical antipsychotic agent. Poster presentation NR-507. 160th Annual Meeting of the American Psychiatric Association; 19 – 24 May 2007; San Diego, CA, USA
   Google Scholar
• Albers LJ, Musenga A, Raggi MA. Iloperidone: a new benzisoxazole atypical antipsychotic drug. Is it novel enough to impact the crowded atypical antipsychotic market? Expert Opin Investig Drugs 2008;17:61-75
   PubMed Web of Science ®Google Scholar
• Potkin SG, Litman RE, Torres R, Wolfgang CD. Efficacy of iloperidone in the treatment of schizophrenia: initial phase 3 studies. J Clin Psychopharmacol 2008;28(2 Suppl 1):S4-11
   PubMed Web of Science ®Google Scholar
• Cutler AJ, Kalali AH, Weiden PJ, Four-week, double-blind, placebo- and ziprasidone-controlled trial of iloperidone in patients with acute exacerbations of schizophrenia. J Clin Psychopharmacol 2008;28(2 Suppl 1):S20-8
   PubMed Web of Science ®Google Scholar
• Kane JM, Lauriello J, Laska E, Long-term efficacy and safety of iloperidone: results from 3 clinical trials for the treatment of schizophrenia. J Clin Psychopharmacol 2008;28(2 Suppl 1):S29-35
   PubMed Web of Science ®Google Scholar
• Weiden PJ, Cutler AJ, Polymeropoulos MH, Wolfgang CD. Safety profile of iloperidone: a pooled analysis of 6-week acute-phase pivotal trials. J Clin Psychopharmacol 2008;28(2 Suppl 1):S12-19
   PubMed Web of Science ®Google Scholar
• Pfizer. Geodon: US Package Insert for Geodon (ziprasidone HCl) and Geodon (ziprasidone mesylate) for Injection. LAB-0273-16.0; revised November 2009. Available from: http://www.pfizer.com/files/products/uspi_geodon.pdf [Last accessed 7 August 2010]
   Google Scholar
• Greenberg WM, Citrome L. Ziprasidone for schizophrenia and bipolar disorder: a review of the clinical trials. CNS Drug Rev 2007;13:137-77
   PubMedGoogle Scholar
• Streiner DL, Cairney J. What's under the ROC? An introduction to receiver operating characteristics curves. Can J Psychiatry 2007;52:121-8
   PubMed Web of Science ®Google Scholar
• Citrome L. Adjunctive lithium and anticonvulsants for the treatment of schizophrenia: what is the evidence? Expert Rev Neurother 2009;9:55-71
   PubMed Web of Science ®Google Scholar
• Hill CL, Phadke D, Boyce KM. Four-week iloperidone depot injectable: safety and pharmacokinetic profile in patients with schizophrenia and schizoaffective disorder. Poster presentation NR4-022. 161st Annual Meeting of the American Psychiatric Association; 3 – 8 May 2008; Washington, DC
   Google Scholar
• Naber D, Moritz S, Lambert M, Improvement of schizophrenic patients' subjective well-being under atypical antipsychotic drugs. Schizophr Res 2001;50:79-88
   PubMed Web of Science ®Google Scholar
• Voruganti LN, Heslegrave RJ, Awad AG. Quality of life measurement during antipsychotic drug therapy of schizophrenia. J Psychiatry Neurosci 1997;22:267-74
   PubMed Web of Science ®Google Scholar
• Morosini PL, Magliano L, Brambilla L, Development, reliability and acceptability of a new version of the DSM-IV Social and Occupational Functioning Assessment Scale (SOFAS) to assess routine social functioning. Acta Psychiatr Scand 2000;101:323-9
   PubMed Web of Science ®Google Scholar