1,450
Views
27
CrossRef citations to date
0
Altmetric
Drug Evaluation

Siponimod for the treatment of secondary progressive multiple sclerosis

, &
Pages 143-150 | Received 02 Sep 2018, Accepted 19 Nov 2018, Published online: 05 Dec 2018

References

  • Tullman MJ. Overview of the epidemiology, diagnosis, and disease progression associated with multiple sclerosis. Am J Manag Care. 2013 Feb;19(2 Suppl):S15–S20.
  • Luchetti S, Fransen NL, van Eden CG, et al. Progressive multiple sclerosis patients show substantial lesion activity that correlates with clinical disease severity and sex: a retrospective autopsy cohort analysis. Acta Neuropathol. 2018 Apr;135(4):511–528.
  • Lublin FD, Reingold SC. Defining the clinical course of multiple sclerosis: results of an international survey. National multiple sclerosis society (USA) advisory committee on clinical trials of new agents in multiple sclerosis. Neurology. 1996 Apr;46(4):907–911.
  • Lublin FD, Reingold SC, Cohen JA, et al. Defining the clinical course of multiple sclerosis: the 2013 revisions. Neurology. 2014 Jul 15;83(3):278–286.
  • Wingerchuk DM, Carter JL. Multiple sclerosis: current and emerging disease-modifying therapies and treatment strategies. Mayo Clin Proc. 2014 Feb;89(2):225–240.
  • Lassmann H. Targets of therapy in progressive MS. Mult Scler. 2017 Oct;23(12):1593–1599.
  • Smith AL, Cohen JA, Hua LH. Therapeutic targets for multiple sclerosis: current treatment goals and future directions. Neurotherapeutics. 2017 Jun 26.
  • Scolding N, Barnes D, Cader S, et al. Association of British Neurologists: revised (2015) guidelines for prescribing disease-modifying treatments in multiple sclerosis. Pract Neurol. 2015 Aug;15(4):273–279.
  • Montalban X, Gold R, Thompson AJ, et al. ECTRIMS/EAN guideline on the pharmacological treatment of people with multiple sclerosis. Eur J Neurol. 2018 Feb;25(2):215–237.
  • Rae-Grant A, Day GS, Marrie RA, et al. Practice guideline recommendations summary: disease-modifying therapies for adults with multiple sclerosis: report of the guideline development, dissemination, and implementation subcommittee of the American Academy of Neurology. Neurology. 2018 Apr 24;90(17):777–788.
  • Kappos L, Bar-Or A, Cree BAC, et al. Siponimod versus placebo in secondary progressive multiple sclerosis (EXPAND): a double-blind, randomised, phase 3 study. Lancet. 2018 Mar 31;391(10127):1263–1273.
  • Montalban X, Hauser SL, Kappos L, et al. Ocrelizumab versus placebo in primary progressive multiple sclerosis. N Engl J Med. 2017 Jan 19;376(3):209–220.
  • Hla T. Physiological and pathological actions of sphingosine 1-phosphate. Semin Cell Dev Biol. 2004 Oct;15(5):513–520.
  • Brinkmann V. Sphingosine 1-phosphate receptors in health and disease: mechanistic insights from gene deletion studies and reverse pharmacology. Pharmacol Ther. 2007 Jul;115(1):84–105.
  • Hla T, Brinkmann V. Sphingosine 1-phosphate (S1P): physiology and the effects of S1P receptor modulation. Neurology. 2011 Feb 22;76(8 Suppl 3):S3–S8.
  • Pan S, Gray NS, Gao W, et al. Discovery of BAF312 (Siponimod), a potent and selective S1P receptor modulator. ACS Med Chem Lett. 2013 Mar 14;4(3):333–337.
  • Okajima F. Plasma lipoproteins behave as carriers of extracellular sphingosine 1-phosphate: is this an atherogenic mediator or an anti-atherogenic mediator? Biochim Biophys Acta. 2002 May 23;1582(1–3):132–137.
  • Brinkmann V, Billich A, Baumruker T, et al. Fingolimod (FTY720): discovery and development of an oral drug to treat multiple sclerosis. Nat Rev Drug Discov. 2010 Nov;9(11):883–897.
  • Kim YM, Sachs T, Asavaroengchai W, et al. Graft-versus-host disease can be separated from graft-versus-lymphoma effects by control of lymphocyte trafficking with FTY720. J Clin Invest. 2003 Mar;111(5):659–669.
  • Comi G, Hartung HP, Bakshi R, et al. Benefit-risk profile of sphingosine-1-phosphate receptor modulators in relapsing and secondary progressive multiple sclerosis. Drugs. 2017 Oct;77(16):1755–1768.
  • Kappos L, Radue EW, O’Connor P, et al. A placebo-controlled trial of oral fingolimod in relapsing multiple sclerosis. N Engl J Med. 2010 Feb 4;362(5):387–401.
  • Lublin F, Miller DH, Freedman MS, et al. Oral fingolimod in primary progressive multiple sclerosis (INFORMS): a phase 3, randomised, double-blind, placebo-controlled trial. Lancet. 2016 Mar 12;387(10023):1075–1084.
  • Park SJ, Im DS. Sphingosine 1-phosphate receptor modulators and drug discovery. Biomol Ther (Seoul). 2017 Jan 1;25(1):80–90.
  • Gergely P, Nuesslein-Hildesheim B, Guerini D, et al. The selective sphingosine 1-phosphate receptor modulator BAF312 redirects lymphocyte distribution and has species-specific effects on heart rate. Br J Pharmacol. 2012 Nov;167(5):1035–1047.
  • Legangneux E, Gardin A, Johns D. Dose titration of BAF312 attenuates the initial heart rate reducing effect in healthy subjects. Br J Clin Pharmacol. 2013 Mar;75(3):831–841.
  • Glaenzel U, Jin Y, Nufer R, et al. Metabolism and disposition of siponimod, a novel selective S1P1/S1P5 agonist, in healthy volunteers and in vitro identification of human cytochrome p450 enzymes involved in its oxidative metabolism. Drug Metab Dispos. 2018 Jul;46(7):1001–1013.
  • Jin Y, Borell H, Gardin A, et al. In vitro studies and in silico predictions of fluconazole and CYP2C9 genetic polymorphism impact on siponimod metabolism and pharmacokinetics. Eur J Clin Pharmacol. 2018 Apr;74(4):455–464.
  • Selmaj K, Li DK, Hartung HP, et al. Siponimod for patients with relapsing-remitting multiple sclerosis (BOLD): an adaptive, dose-ranging, randomised, phase 2 study. Lancet Neurol. 2013 Aug;12(8):756–767.
  • Kappos L, Li DK, Stuve O, et al. Safety and efficacy of siponimod (BAF312) in patients with relapsing-remitting multiple sclerosis: dose-blinded, randomized extension of the phase 2 bold study. JAMA Neurol. 2016 Sep 1;73(9):1089–1098.
  • Legangneux E, Shakeri-Nejad K, Aslanis V, et al. Cardiac effects of siponimod (BAF312) re-initiation after variable periods of drug discontinuation in healthy subjects. Clin Ther. 2016 Mar;38(3):631–45 e1.
  • Ufer M, Shakeri-Nejad K, Gardin A, et al. Impact of siponimod on vaccination response in a randomized, placebo-controlled study. Neurol Neuroimmunol Neuroinflamm. 2017 Nov;4(6):e398.
  • Hellmann MA, Lev N, Lotan I, et al. Tumefactive demyelination and a malignant course in an MS patient during and following fingolimod therapy. J Neurol Sci. 2014 Sep 15;344(1–2):193–197.
  • Hussain R, O’Leary S, Pacheco FM, et al. Acute relapse after initiation of siponimod in a patient with secondary progressive MS. J Neurol. 2016 Mar;263(3):606–610.
  • Fujii C, Kondo T, Ochi H, et al. Altered T cell phenotypes associated with clinical relapse of multiple sclerosis patients receiving fingolimod therapy. Sci Rep. 2016 Oct 18;6:35314.
  • Giordana MT, Cavalla P, Uccelli A, et al. Overexpression of sphingosine-1-phosphate receptors on reactive astrocytes drives neuropathology of multiple sclerosis rebound after fingolimod discontinuation. Mult Scler. 2018 Jul;24(8):1133–1137.
  • Centonze D, Rossi S, Rinaldi F, et al. Severe relapses under fingolimod treatment prescribed after natalizumab. Neurology. 2012 Nov 6;79(19):2004–2005.
  • Faissner S, Hoepner R, Lukas C, et al. Tumefactive multiple sclerosis lesions in two patients after cessation of fingolimod treatment. Ther Adv Neurol Disord. 2015 Sep;8(5):233–238.
  • Gyang TV, Hamel J, Goodman AD, et al. Fingolimod-associated PML in a patient with prior immunosuppression. Neurology. 2016 May 10;86(19):1843–1845.
  • Berger JR. Classifying PML risk with disease modifying therapies. Mult Scler Relat Disord. 2017 Feb;12:59–63.
  • Min JH, Kim BJ, Lee KH. Development of extensive brain lesions following fingolimod (FTY720) treatment in a patient with neuromyelitis optica spectrum disorder. Mult Scler. 2012 Jan;18(1):113–115.
  • Yoshii F, Moriya Y, Ohnuki T, et al. Fingolimod-induced leukoencephalopathy in a patient with neuromyelitis optica spectrum disorder. Mult Scler Relat Disord. 2016 May;7:53–57.
  • Fisniku LK, Brex PA, Altmann DR, et al. Disability and T2 MRI lesions: a 20-year follow-up of patients with relapse onset of multiple sclerosis. Brain. 2008 Mar;131(Pt 3):808–817.
  • Leray E, Yaouanq J, Le Page E, et al. Evidence for a two-stage disability progression in multiple sclerosis. Brain. 2010 Jul;133(Pt 7):1900–1913.
  • Fogarty E, Schmitz S, Tubridy N, et al. Comparative efficacy of disease-modifying therapies for patients with relapsing remitting multiple sclerosis: systematic review and network meta-analysis. Mult Scler Relat Disord. 2016 Sep;9:23–30.
  • Panitch H, Miller A, Paty D, et al. Interferon beta-1b in secondary progressive MS: results from a 3-year controlled study. Neurology. 2004 Nov 23; 63(10):1788–1795.
  • Kuhle J, Hardmeier M, Disanto G, et al. A 10-year follow-up of the European multicenter trial of interferon beta-1b in secondary-progressive multiple sclerosis. Mult Scler. 2016 Apr;22(4):533–543.
  • Kappos L, Weinshenker B, Pozzilli C, et al. Interferon beta-1b in secondary progressive MS: a combined analysis of the two trials. Neurology. 2004 Nov 23;63(10):1779–1787.
  • Hartung HP, Gonsette R, Konig N, et al. Mitoxantrone in progressive multiple sclerosis: a placebo-controlled, double-blind, randomised, multicentre trial. Lancet. 2002 Dec 21-28;360(9350):2018–2025.
  • Filippini G, Del Giovane C, Vacchi L, et al. Immunomodulators and immunosuppressants for multiple sclerosis: a network meta-analysis. Cochrane Database Syst Rev. 2013 Jun;06(6):CD008933.
  • Kulakowska A, Zendzian-Piotrowska M, Baranowski M, et al. Intrathecal increase of sphingosine 1-phosphate at early stage multiple sclerosis. Neurosci Lett. 2010 Jun 25;477(3):149–152.
  • Novgorodov AS, El-Alwani M, Bielawski J, et al. Activation of sphingosine-1-phosphate receptor S1P5 inhibits oligodendrocyte progenitor migration. FASEB J. 2007 May;21(7):1503–1514.
  • Pebay A, Toutant M, Premont J, et al. Sphingosine-1-phosphate induces proliferation of astrocytes: regulation by intracellular signalling cascades. Eur J Neurosci. 2001 Jun;13(12):2067–2076.
  • Sim-Selley LJ, Goforth PB, Mba MU, et al. Sphingosine-1-phosphate receptors mediate neuromodulatory functions in the CNS. J Neurochem. 2009 Aug;110(4):1191–1202.
  • Soliven B, Miron V, Chun J. The neurobiology of sphingosine 1-phosphate signaling and sphingosine 1-phosphate receptor modulators. Neurology. 2011 Feb 22;76(8 Suppl 3):S9–S14.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.