Fingolimod: a review of its mode of action in the context of its efficacy and safety profile in relapsing forms of multiple sclerosis

Expert Rev Neurother. 2016;16(1):31-44. doi: 10.1586/14737175.2016.1123094. Epub 2016 Jan 13.

Abstract

Fingolimod is an orally administered, first-in-class therapy for the treatment of relapsing forms of multiple sclerosis. Data from pivotal clinical trials show that fingolimod has a robust, significant effect on annualized relapse rates and MRI outcomes. Fingolimod has a novel, well-characterized mechanism of action. It acts through a specific set of receptors, sphingosine 1-phosphate receptors, present on the surface of a wide range of human cells and tissues, including neural cells, neurons and lymphocytes. Here we review the current literature to describe the mechanism of action of fingolimod in the context of its well-established clinical efficacy and safety profile. Understanding of the mechanisms behind any non-therapeutic effects of fingolimod facilitates their prediction and management in the clinical setting.

Keywords: Fingolimod; efficacy; mechanism of action; multiple sclerosis; non-therapeutic effects; safety.

Publication types

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

MeSH terms

  • Fingolimod Hydrochloride / standards
  • Fingolimod Hydrochloride / therapeutic use*
  • Humans
  • Immunosuppressive Agents / standards
  • Immunosuppressive Agents / therapeutic use
  • Multiple Sclerosis, Relapsing-Remitting / drug therapy*
  • Propylene Glycols

Substances

  • Immunosuppressive Agents
  • Propylene Glycols
  • Fingolimod Hydrochloride