Oral therapies for multiple sclerosis: a review of agents in phase III development or recently approved

CNS Drugs. 2011 Jan;25(1):37-52. doi: 10.2165/11539820-000000000-00000.


Several disease-modifying therapies are approved for the management of multiple sclerosis (MS). While reasonably effective, these therapies require long-term parenteral self-injection, which is inconvenient for some patients and can be associated with injection-related adverse effects. Consequently, there is a need in MS for an oral therapy option. Currently, five oral therapies are in phase III development or have recently been approved for the treatment of relapsing-remitting MS: cladribine (approved in Russia and Australia), fingolimod (approved in the US and Russia), BG-12 (phase III), laquinimod (phase III) and teriflunomide (phase III). While the availability of oral therapies has been much anticipated by physicians and patients, neurologists will need to be cautious in selecting such therapy, which may appear to have efficacy and convenience advantages versus current therapies, but may also carry novel safety and tolerability concerns. The decision to use these new therapies will most likely be based on an overall assessment of efficacy, safety, tolerability and adherence, the potential need for monitoring and cost effectiveness. The objective of this article is to review the currently available data for each of these new oral therapies, which addresses the mechanism of action, efficacy and safety, and to provide a perspective on the potential future role of these therapies within clinical practice. Although better patient compliance is expected with the oral agents compared with the injectables, the safety profiles of these new oral drugs will have to be watched carefully.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Administration, Oral
  • Cladribine / administration & dosage
  • Clinical Trials, Phase III as Topic
  • Crotonates / administration & dosage
  • Dimethyl Fumarate
  • Fingolimod Hydrochloride
  • Fumarates / administration & dosage
  • Humans
  • Hydroxybutyrates
  • Multiple Sclerosis / drug therapy*
  • Nitriles
  • Propylene Glycols / administration & dosage
  • Quinolones / administration & dosage
  • Sphingosine / administration & dosage
  • Sphingosine / analogs & derivatives
  • Toluidines / administration & dosage


  • Crotonates
  • Fumarates
  • Hydroxybutyrates
  • Nitriles
  • Propylene Glycols
  • Quinolones
  • Toluidines
  • teriflunomide
  • Cladribine
  • laquinimod
  • Dimethyl Fumarate
  • Fingolimod Hydrochloride
  • Sphingosine