Cladribine, a synthetic deoxyadenosine analog, is an oral immunomodulatory agent that produces targeted, sustained reduction of T and B lymphocytes. This mechanism of action provides the rationale for use in relapsing-remitting multiple sclerosis (MS) in a short-course annual dosing regimen. Based on the results of a pivotal Phase III study, therapy with cladribine tablets has the potential to become a licensed oral disease-modifying medication for relapsing forms of MS. This article will review the key points regarding MS and its pathogenesis, and discuss current unmet treatment needs. In particular the review provides an overview of emerging potential new oral MS therapies with a focus on the mechanism of action, chemistry, pharmacokinetics, pharmacodynamics, clinical efficacy and safety of cladribine tablets. Assessments and conclusions will include a speculative 5-year outlook.