The preclinical discovery and development of ezogabine for the treatment of epilepsy

Bibliography

• Anand IS, Shah JS, Patel SK, Patel CN. Retigabine: a novel anticonvulsant drug. Indian J Pharmacol 2005;37:340-1
   Google Scholar
• Gunthorpe MJ, Large CH, Sankar R. The mechanism of action of retigabine (ezogabine), a first-in-class K+ channel opener for the treatment of epilepsy. Epilepsia 2012;53:412-24
   PubMed Web of Science ®Google Scholar
• Singh NA, Charlier C, Stauffer D, et al. A novel potassium channel gene, KCNQ2, is mutated in an inherited epilepsy of newborns. Nat Genet 1998;18:25-9
   PubMed Web of Science ®Google Scholar
• Charlier C, Singh NA, Ryan SG, et al. A pore mutation in a novel KQT-like potassium channel gene in an idiopathic epilepsy family. Nat Genet 1998;18:53-5
   PubMed Web of Science ®Google Scholar
• Wang HS, Pan Z, Shi W, et al. KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel. Science 1998;282(5395):1890-3
   PubMed Web of Science ®Google Scholar
• Zhou P, Yu H, Gu M, et al. Phosphatidylinositol 4,5-bisphosphate alters pharmacological selectivity for epilepsy-causing KCNQ potassium channels. Proc Natl Acad Sci USA 2013;110:8726-31
   PubMed Web of Science ®Google Scholar
• Kaiboriboon K, Bakaki PM, Lhatoo SD, Koroukian S. Incidence and prevalence of treated epilepsy among poor health and low-income Americans. Neurology 2013;80:1942-9
   PubMed Web of Science ®Google Scholar
• Lhatoo SD, Sander JW. Cause-specific mortality in epilepsy. Epilepsia 2005;46(Suppl 11):36-9
   PubMed Web of Science ®Google Scholar
• La Vecchia C, Negri E. A review of epidemiological data on epilepsy, phenobarbital, and risk of liver cancer. Eur J Cancer Prev 2013; published online 12 March 2013; doi: 10.1097/CEJ.0b013e32836014c8
   Web of Science ®Google Scholar
• Nordentoft M. Prevention of suicide and attempted suicide in Denmark. Epidemiological studies of suicide and intervention studies in selected risk groups. Dan Med Bull 2007;54:306-69
   PubMed Web of Science ®Google Scholar
• Téllez-Zenteno JF, Nguyen R, Hernádez-Ronquillo L. Injuries, accidents and mortality in epilepsy: a review of its prevalence risk factors and prevention. Rev Invest Clin 2010;62:466-79
   PubMed Web of Science ®Google Scholar
• Pohlmann-Eden B, Weaver DF. The puzzle(s) of pharmacoresistant epilepsy. Epilepsia 2013;54(Suppl 2):1-4
   PubMed Web of Science ®Google Scholar
• Kwan P, Arzimanoglou A, Berg AT, et al. Definition of drug resistant epilepsy: consensus proposal by the ad hoc Task Force of the ILAE Commission on Therapeutic Strategies. Epilepsia 2010;51:1069-77
   PubMed Web of Science ®Google Scholar
• Maehara T, Inaji M, Matsuura M. Surgical effects of focus resection for patients with intractable epilepsy. Neurol Med Chir (Tokyo) 2013;53:281-6
   PubMed Web of Science ®Google Scholar
• Privitera M. Current challenges in the management of epilepsy. Am J Manag Care 2011;17(Suppl 7):S195-203
   PubMedGoogle Scholar
• French JA, Gazzola DM. Antiepileptic drug treatment: new drugs and new strategies. Continuum (Minneap Minn) 2013;19(3 Epilepsy):643-55
   PubMedGoogle Scholar
• Gerlach AC, Krajewski JL. Antiepileptic drug discovery and development: what have we learned and where are we going? Pharmaceuticals 2010;3:2884-99
   Google Scholar
• Barrese V, Miceli F, Soldovieri MV, et al. Neuronal potassium channel openers in the management of epilepsy: role and potential of retigabine. Clin Pharmacol 2010;2:225-36
   PubMedGoogle Scholar
• Wang X, Zhou H, Zheng J, et al. Identification and characterization of four process-related impurities in retigabine. J Pharm Biomed Anal 2012;71:148-51
   PubMed Web of Science ®Google Scholar
• Lakshmi B, Saraswathi K, Reddy TV. Rp-hplc method development and validation for the analyisis of ezogabine in pharmaceutical dosage forms. Int J A Ps BMS 2012;1:7-14
   Google Scholar
• Ermer J. Validation in pharmaceutical analysis. Part I: an integrated approach. J Pharm Biomed Anal 2001;24:755-67
   PubMed Web of Science ®Google Scholar
• Tatulian L, Delmas P, Abogadie FC, Brown DA. Activation of expressed KCNQ potassium currents and native neuronal M-type potassium currents by the anti-convulsant drug retigabine. J Neurosci 2001;21(15):5535-45
   PubMed Web of Science ®Google Scholar
• Dupuis DS, Schrøder RL, Jespersen T, et al. Activation of KCNQ5 channels stably expressed in HEK293 cells by BMS-204352. Eur J Pharmacol 2002;437:129-37
   PubMed Web of Science ®Google Scholar
• Wuttke TV, Seebohm G, Bail S, et al. The new anticonvulsant retigabine favors voltage-dependent opening of the Kv7.2 (KCNQ2) channel by binding to its activation gate. Mol Pharmacol 2005;67:1009-17
   PubMed Web of Science ®Google Scholar
• Li P, Chen Z, Xu H, et al. The gating charge pathway of an epilepsy-associated potassium channel accommodates chemical ligands. Cell Res 2013; published online 25 June 2013; doi: 10.1038/cr.2013.82
   Web of Science ®Google Scholar
• Rundfeldt C, Netzer R. Modulatory binding site in potassium channels for screening and finding new active ingredients. US6472165; 2002
   Google Scholar
• Asta Medica Aktiengesellschaft. Pharmaceutically active 1,2,4-triamino-benzene derivatives, processes for their preparation and pharmaceutical compositions containing them. US5384330; 1995
   Google Scholar
• Asta Medica Aktiengesellschaft. 1,2,4-triaminobenzene derivatives and processes for their preparation. EP0554543A2; 1993
   Google Scholar
• Fitzgerald RN, Millar A, Fell Toczko J. Process for the preparation of retigabine. W02012098075A1; 2012
   Google Scholar
• Szelenyi I, Brune K, Hermann R, Locher M. Combinations of Retigabine and Sodium Channel Inhibitors or Sodium Channel-Influencing Active Compounds for Treating Pains. US7799832; 2010
   Google Scholar
• Asta Medica Aktiengesellschaft. Modifications of 2-amino-4-(4-fluorobenzylamino)-1-ethoxycarbonylaminobenzene, and process for their preparation. US5638151; 2003
   Google Scholar
• Biljana Nadjsombati. Modified release formulation and methods of use. US20100323016; 2010
   Google Scholar
• Rostock A, Tober C, Rundfeldt C, et al. D-23129: a new anticonvulsant with a broad spectrum activity in animal models of epileptic seizures. Epilepsy Res 1996;23:211-23
   PubMed Web of Science ®Google Scholar
• Dailey JW, Cheong JH, Ko KH, et al. Anticonvulsant properties of D-20443 in genetically epilepsy-prone rats: prediction of clinical response. Neurosci Lett 1995;195:77-80
   PubMed Web of Science ®Google Scholar
• Marescaux C, Micheletti G, Vergnes M, et al. A model of chronic spontaneous petit mal-like seizures in the rat: comparison with pentylenetetrazol-induced seizures. Epilepsia 1984;25:326-31
   PubMed Web of Science ®Google Scholar
• Marescaux C, Vergnes M, Depaulis A. Genetic absence epilepsy in rats from Strasbourg – a review. J Neural Transm Suppl 1992;35:37-69
   PubMedGoogle Scholar
• Large CH, Sokal DM, Nehlig A, et al. The spectrum of anticonvulsant efficacy of retigabine (ezogabine) in animal models: implications for clinical use. Epilepsia 2012;53:425-36
   PubMed Web of Science ®Google Scholar
• de Sarro G, di Paola ED, Conte G, et al. Influence of retigabine on the anticonvulsant activity of some antiepileptic drugs against audiogenic seizures in DBA/2 mice. Naunyn Schmiedebergs Arch Pharmacol 2001;363:330-6
   PubMed Web of Science ®Google Scholar
• Tober C, Rostock A, Rundfeldt C, Bartsch R. D-23129: a potent anticonvulsant in the amygdala kindling model of complex partial seizures. Eur J Pharmacol 1996;303:163-9
   PubMed Web of Science ®Google Scholar
• Mazarati A, Wu J, Shin D, et al. Antiepileptogenic and antiictogenic effects of retigabine under conditions of rapid kindling: an ontogenic study. Epilepsia 2008;49:1777-86
   PubMed Web of Science ®Google Scholar
• Smith MD, Adams AC, Saunders GW, et al. Phenytoin- and carbamazepine-resistant spontaneous bursting in rat entorhinal cortex is blocked by retigabine in vitro. Epilepsy Res 2007;74:97-106
   PubMed Web of Science ®Google Scholar
• Straub H, Köhling R, Höhling J, et al. Effects of retigabine on rhythmic synchronous activity of human neocortical slices. Epilepsy Res 2001;44:155-65
   PubMed Web of Science ®Google Scholar
• Bialer M, Johannessen SI, Levy RH, et al. Progress report on new antiepileptic drugs: a summary of the Ninth Eilat Conference (EILAT IX). Epilepsy Res 2009;83:1-43
   PubMed Web of Science ®Google Scholar
• McCallum LA, Pierce SL, England SK, et al. The contribution of Kv7 channels to pregnant mouse and human myometrial contractility. J Cell Mol Med 2011;15:577-86
   PubMed Web of Science ®Google Scholar
• Löscher W, Nolting B. The role of technical, biological and pharmacological factors in the laboratory evaluation of anticonvulsant drugs. IV. Protective indices. Epilepsy Res 1991;9:1-10
   PubMed Web of Science ®Google Scholar
• Summary Basis of Decision. Potiga®, Health Canada. 2012. Available from: http://www.hc-sc.gc.ca [Last accessed 13 July 2013]
   Google Scholar
• Trobalt® (retigabine). Summary of Product Characteristics. Glaxo Group Ltd, at European Medicines Agency. Available from: http://www.ema.europa.eu/docs/en [Last accessed 13 July 2013]
   Google Scholar
• Luszczki JJ, Wu JZ, Raszewski G, Czuczwar SJ. Isobolographic characterization of interactions of retigabine with carbamazepine, lamotrigine, and valproate in the mouse maximal electroshock-induced seizure model. Naunyn Schmiedebergs Arch Pharmacol 2009;379:163-79
   PubMed Web of Science ®Google Scholar
• Deeks ED. Retigabine (ezogabine): in partial-onset seizures in adults with epilepsy. CNS Drugs 2011;25:887-900
   PubMed Web of Science ®Google Scholar
• French JA, Abou-Khalil BW, Leroy RF, et al. RESTORE 1/Study 301 Investigators. Randomized, double-blind, placebo-controlled trial of ezogabine (retigabine) in partial epilepsy. Neurology 2011;76:1555-63
   PubMed Web of Science ®Google Scholar
• Brodie MJ, Lerche H, Gil-Nagel A, et al. RESTORE 2 Study Group. Efficacy and safety of adjunctive ezogabine (retigabine) in refractory partial epilepsy. Neurology 2010;75:1817-24
   PubMed Web of Science ®Google Scholar
• Porter RJ, Partiot A, Sachdeo R, et al. 205 Study Group. Randomized, multicenter, dose-ranging trial of retigabine for partial-onset seizures. Neurology 2007;68:1197-204
   PubMed Web of Science ®Google Scholar
• Porter RJ, Burdette DE, Gil-Nagel A, et al. Retigabine as adjunctive therapy in adults with partial-onset seizures: integrated analysis of three pivotal controlled trials. Epilepsy Res 2012;101:103-12
   PubMed Web of Science ®Google Scholar
• Gil-Nagel A, Brodie MJ, Leroy R, et al. Safety and efficacy of ezogabine (retigabine) in adults with refractory partial-onset seizures: interim results from two ongoing open-label studies. Epilepsy Res 2012;102:117-21
   PubMed Web of Science ®Google Scholar
• Harris JA, Murphy JA. Retigabine (ezogabine) as add-on therapy for partial-onset seizures: an update for clinicians. Ther Adv Chronic Dis 2011;2:371-6
   Google Scholar
• Yamada M, Welty TE. Ezogabine: an evaluation of its efficacy and safety as adjunctive therapy for partial-onset seizures in adults. Ann Pharmacother 2012;46:1358-67
   PubMed Web of Science ®Google Scholar
• Ciliberto MA, Weisenberg JL, Wong M. Clinical utility, safety, and tolerability of ezogabine (retigabine) in the treatment of epilepsy. Drug Healthc Patient Saf 2012;4:81-6
   Google Scholar
• Martyn-St James M, Glanville J, McCool R, et al. The efficacy and safety of retigabine and other adjunctive treatments for refractory partial epilepsy: a systematic review and indirect comparison. Seizure 2012;21:665-78
   PubMed Web of Science ®Google Scholar
• Orhan G, Wuttke TV, Nies AT, et al. Retigabine/Ezogabine, a KCNQ/K(V)7 channel opener: pharmacological and clinical data. Expert Opin Pharmacother 2012;13:1807-16
   PubMed Web of Science ®Google Scholar
• Retigabine (Trobalt): indication restricted to last-line use, and new monitoring requirements after reports of pigment changes in ocular tissue, skin, lips or nails. 2013;6(12):A2
   Google Scholar
• GlaxoSmithKline. Open-label, multiple dose study to evaluate the pharmacokinetics, safety, and tolerability of ezogabine/retigabine as adjunctive treatment in subjects aged from 12 years to less than 18 years with partial onset seizures or Lennox-Gastaut syndrome. ClinicalTrials.gov Web site. Bethesda, MD: National Library of Medicine. 2011. NLM identifier: NCT01494584 Available from: http://clinicaltrials.gov/ct2/show/NCT01494584?term=NCT01494584 [Last accessed 22 July 2013]
   Google Scholar
• GlaxoSmithKline. RTG113388, a long-term, open-label safety extension study of retigabine/ezogabine in pediatric subjects with partial onset seizures (≥12 years old) and subjects with Lennox-Gastaut syndrome (≥12 years old). ClinicalTrials.gov Web site. Bethesda, MD: National Library of Medicine. 2012. NLM identifier: NCT01668654 Available from: http://clinicaltrials.gov/ct2/show/NCT01668654?term=01668654&rank=1 [Last accessed 22 July 2013]
   Google Scholar
• Chhim RF, Shelton CM, Christensen ML. Recent new drug approvals, part 2: drugs undergoing active clinical studies in children. J Pediatr Pharmacol Ther 2013;18:14-38
   PubMedGoogle Scholar
• GlaxoSmithKline. An Open Label, Randomised, Repeat Dose Study to Assess the Pharmacokinetic Performance of FiveEzogabine/Retigabine Modified Release (MR) Formulations at Steady State Compared to the Immediate Release (IR) Formulation. ClinicalTrials.gov Web site. Bethesda, MD: National Library of Medicine. 2012. NLM identifier: NCT01332513 Available from: http://clinicaltrials.gov/ct2/show/NCT01332513?term=ezogabine&rank=7 [Last accessed 22 July 2013]
   Google Scholar
• GlaxoSmithKline. Risk of Urinary Retention with Ezogabine. ClinicalTrials.gov Web site. Bethesda, MD: National Library of Medicine. 2012. NLM identifier: NCT01462656 Available from: http://clinicaltrials.gov/ct2/show/NCT01462656?term=ezogabine&rank=21 [Last time accessed 22 July 2013]
   Google Scholar
• López-Muñoz F, Alamo C. Monoaminergic neurotransmission: the history of the discovery of antidepressants from 1950s until today. Curr Pharm Des 2009;15:1563-86
   PubMed Web of Science ®Google Scholar
• López-Muñoz F, Alamo C, García-García P. The discovery of chlordiazepoxide and the clinical introduction of benzodiazepines: half a century of anxiolytic drugs. J Anxiety Disord 2011;25:554-62
   PubMed Web of Science ®Google Scholar
• Pattnaik BR, Hughes BA. Effects of KCNQ channel modulators on the M-type potassium current in primate retinal pigment epithelium. Am J Physiol Cell Physiol 2012;302:C821-33
   PubMed Web of Science ®Google Scholar