Multiple sclerosis (MS) is a chronic inflammatory disease of the central nervous system. The seven therapies currently approved by regulatory agencies are administered by subcutaneous or intramuscular injection or intravenous infusion. Many phase 2 trials involving oral MS therapeutics were recently completed, as were two phase 3 trials of fingolimod and one phase 3 trial of cladribine. Numerous other oral treatments are being investigated in ongoing phase 3 trials. Although an oral route of administration is attractive, these medications also present new challenges in balancing convenience, efficacy, and safety. In this review, we examine the safety and efficacy data from emerging oral therapies in an attempt to clarify their potential future role in the treatment of MS patients.