Table 2.

Main features of the currently approved oral disease-modifying treatments for relapsing multiple sclerosis (only data relative to currently approved dose presented)

Molecule Trials	Efficacy		Safety	Tolerability
	Relapsea	Disabilitya
Fingolimod Fingolimod Research Evaluating Effects of Daily Oral therapy in Multiple Sclerosis (FREEDOMS)24	−55%	−26.6%b	Herpes virus and other opportunistic infections,d bradyarrhythmias, macular edema, skin neoplasms	High burden for first-dose administration
TRial Assessing injectable interferoN vs. FTY720 Oral in RRMS (TRANSFORMS)25	−51.5%b	−25.3%c
Teriflunomide Teriflunomide Multiple Sclerosis Oral (TEMSO)26	−31.5%	−29.8%	Liver-enzyme increase, neutropenia, pregnancy issues	Hair thinning, gastrointestinal events
Oral teriflunomide for patients with relapsing multiple sclerosis (TOWER)27	−36.3%	−31.5%
Dimethyl fumarate Determination of the Efficacy and Safety of Oral Fumarate in Relapsing–Remitting MS (DEFINE)28	−41.3%	−38%	Leukopenia, lymphopeniae	Flushing, gastrointestinal events
Comparator and an Oral Fumarate in Relapsing-Remitting Multiple Sclerosis (CONFIRM)29	−44.0%	−21%c

Notes:

^aRelative reduction in relapse rate (primary end point) and disability worsening (secondary end point) versus placebo;

^bversus IFNβ_1a 30 μg once weekly (12-month follow-up);

^cnot significant;

^dincluding progressive multifocal encephalopathy and cryptococcosis;

^efour patients older than 50 years developed progressive multifocal encephalopathy following a prolonged grade 2 or 3 lymphopenia.