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The emergence of oral-administered small molecules in multiple sclerosis (MS) therapeutics affords patients potential benefits of improved adherence, convenience, and increased effectiveness within a therapeutic area, which has otherwise benefited predominantly from injectable disease-modifying medicines for several decades. Switching from injectable to oral MS treatment may also improve treatment persistence.1 Siponimod (BAF312) is an oral investigational drug, a selective sphingosine 1-phosphate (S1P1,5) receptor modulator,2,3 currently in phase 3 clinical trials for secondary progressive MS (ClinicalTrials.gov Identifier: NCT01665144). Siponimod bears similarities with fingolimod, an S1P1,3,4,5 receptor modulator and first-in-class oral medication approved in the United States in 2010 for relapsing remitting MS (RRMS).4 Because of more selective modulation of S1P receptors, it is important to understand whether the pharmacokinetic profile of siponimod offers improved efficacy and safety.
Hammond ER. Perspectives on Safety and Efficacy—The BOLD Phase 2 Extension Study of Siponimod in Relapsing-Remitting Multiple Sclerosis. JAMA Neurol. 2016;73(9):1052-1054. doi:10.1001/jamaneurol.2016.2284