Iloperidone (Fanapt ®), a novel atypical antipsychotic, is a potent HERG blocker and delays cardiac ventricular repolarization at clinically relevant concentration

Pharmacological Research

Volumn 66, Issue 1, 2012, Pages 60-65

  Vigneault, Patrick ^a,b   Pilote, Sylvie ^b   Patoine, Dany ^b   Simard, Chantale ^a,b   Drolet, Benoit ^a,b  

^a UNIVERSITÉ LAVAL   (Canada)

^b LAVAL UNIVERSITY   (Canada)

Author keywords

Antipsychotic; Cardiac ventricular repolarization; HERG blocker; Iloperidone

Indexed keywords

ILOPERIDONE; POTASSIUM CHANNEL HERG;

ACTION POTENTIAL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CELL STRAIN HEK293; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG EXPOSURE; EX VIVO STUDY; GENETIC TRANSFECTION; GUINEA PIG; HEART PACING; HEART REPOLARIZATION; HEART VENTRICLE REPOLARIZATION; IN VITRO STUDY; IN VIVO STUDY; ISOLATED HEART; MALE; NONHUMAN; PATCH CLAMP; POTASSIUM CURRENT; PRIORITY JOURNAL; QT PROLONGATION; SINUS RHYTHM; TELEMETRY;

ACTION POTENTIALS; ANIMALS; ANTIPSYCHOTIC AGENTS; ARRHYTHMIAS, CARDIAC; DOSE-RESPONSE RELATIONSHIP, DRUG; ELECTROCARDIOGRAPHY, AMBULATORY; ETHER-A-GO-GO POTASSIUM CHANNELS; GUINEA PIGS; HEART CONDUCTION SYSTEM; HEK293 CELLS; HUMANS; ISOXAZOLES; MALE; PATCH-CLAMP TECHNIQUES; PERFUSION; PIPERIDINES; POTASSIUM CHANNEL BLOCKERS; RISK ASSESSMENT; TELEMETRY; TIME FACTORS; TRANSFECTION;

EID: 84860460685     PISSN: 10436618     EISSN: 10961186     Source Type: Journal    
DOI: 10.1016/j.phrs.2012.03.008     Document Type: Article

References (20)

1. K. Kleinhaus, S. Harlap, M. Perrin, O. Manor, M. Weiser, and P. Lichtenberg Age, sex and first treatment of schizophrenia in a population cohort Journal of Psychiatric Research 45 1 2011 136 141
2. S.A. Arif, and M.M. Mitchell Iloperidone: a new drug for the treatment of schizophrenia American Journal of Health-System Pharmacy 68 4 2011 301 308
3. L. Citrome Iloperidone for schizophrenia: a review of the efficacy and safety profile for this newly commercialised second-generation antipsychotic International Journal of Clinical Practice 63 8 2009 1237 1248
4. L. Citrome Iloperidone: chemistry, pharmacodynamics, pharmacokinetics and metabolism, clinical efficacy, safety and tolerability, regulatory affairs, and an opinion Expert Opinion on Drug Metabolism & Toxicology 6 12 2010 1551 1564
5. J. Bishop, and D. Bishop Iloperidone for the treatment of schizophrenia Drugs Today (Barcelona) 46 8 2010 567 579
6. J. Marino, and J. Caballero Iloperidone for the treatment of schizophrenia Annals of Pharmacotherapy 44 5 2010 863 870
7. S. Caccia, L. Pasina, and A. Nobili New atypical antipsychotics for schizophrenia: iloperidone Drug Design, Development and Therapy 4 2010 33 48
8. S. Volpi, C. Heaton, K. Mack, J. Hamilton, R. Lannan, and C. Wolfgang Whole genome association study identifies polymorphisms associated with QT prolongation during iloperidone treatment of schizophrenia Molecular Psychiatry 14 11 2009 1024 1031
9. J. Kane, J. Lauriello, E. Laska, M. Di Marino, and C. Wolfgang Long-term efficacy and safety of iloperidone: results from 3 clinical trials for the treatment of schizophrenia Journal of Clinical Psychopharmacology 28 2 Suppl 1 2008 S29 S35
10. A. Cutler, A. Kalali, P. Weiden, J. Hamilton, and C. Wolfgang Four-week, double-blind, placebo- and ziprasidone-controlled trial of iloperidone in patients with acute exacerbations of schizophrenia Journal of Clinical Psychopharmacology 28 2 Suppl 1 2008 S20 S28
11. P. Weiden, A. Cutler, M. Polymeropoulos, and C. Wolfgang Safety profile of iloperidone: a pooled analysis of 6-week acute-phase pivotal trials Journal of Clinical Psychopharmacology 28 2 Suppl 1 2008 S12 S19
12. R.L. Hamlin, A. Kijtawornrat, B.W. Keene, and D.M. Hamlin QT and RR intervals in conscious and anesthetized guinea pigs with highly varying RR intervals and given QTc-lengthening test articles Toxicological Sciences 76 2 2003 437 442 (Pubitemid 38035437)
13. J. Silvestre, and J. Prous Comparative evaluation of hERG potassium channel blockade by antipsychotics Methods and Findings in Experimental and Clinical Pharmacology 29 7 2007 457 465 (Pubitemid 350157134)
14. N. Subramanian, and H. Kalkman Receptor profile of P 88-8991 and P 95-12113, metabolites of the novel antipsychotic iloperidone Progress in Neuro-Psychopharmacology and Biological Psychiatry 26 2002 553 560 (Pubitemid 34252950)
15. S. Potkin, R. Litman, R. Torres, and C. Wolfgang Efficacy of iloperidone in the treatment of schizophrenia: initial phase 3 studies Journal of Clinical Psychopharmacology 28 2 Suppl 1 2008 S4 S11
16. W.S. Redfern, L. Carlsson, A.S. Davis, W.G. Lynch, I. MacKenzie, and S. Palethorpe Relationships between preclinical cardiac electrophysiology, clinical QT interval prolongation and torsade de pointes for a broad range of drugs: evidence for a provisional safety margin in drug development Cardiovascular Research 58 2003 32 45 (Pubitemid 36351620)
17. A. Paulussen, R. Gilissen, M. Armstrong, P. Doevendans, P. Verhasselt, and H. Smeets Genetic variations of KCNQ1, KCNH2, SCN5A, KCNE1, and KCNE2 in drug-induced long QT syndrome patients Journal of Molecular Medicine (Berlin) 82 3 2004 182 188 (Pubitemid 38392168)
18. P. Yang, H. Kanki, B. Drolet, T. Yang, J. Wei, and P.C. Viswanathan Allelic variants in long-QT disease genes in patients with drug-associated torsades de pointes Circulation 105 16 2002 1943 1948 (Pubitemid 34437622)
19. D.M. Roden Acquired long QT syndromes and the risk of proarrhythmia Journal of Cardiovascular Electrophysiology 11 8 2000 938 940 (Pubitemid 30663004)
20. M. Malik, and A.J. Camm Evaluation of drug-induced QT interval prolongation: implications for drug approval and labelling Drug Safety 24 5 2001 323 351 (Pubitemid 32417533)