A Review on Fingolimod; the First Oral Medication for Multiple Sclerosis

Multiple sclerosis (MS) is a progressive neurological autoimmune disease that usually starts in the late third and early forth decades of life. Demyelination of neurons in the central nervous system (CNS) and, subsequently, loss of nerve cells is the known disease pathogenesis. The disease is controlled by a class of medicines which are mainly immunomodulators. Fingolimod (FIN) is the first approved oral medication for controlling relapsing-remitting type of MS. It is chemically modified form of a fungus metabolite with long history of use in traditional Chinese medicine. Its mechanism of action is through functional antagonism of sphingosine-1 phosphate receptors which leads to lymphocyte entrapment in lymphoid tissues and reduction of their circulating number in the CNS. FIN efficacy comparing with placebo and first line therapies for MS (e.g. Interferon) has been proved through several clinical trials. Common side effects of FIN are usually mild and are well tolerated. FIN can pass through placenta and has been assigned to pregnancy category C according to the observed effects in animal studies. Since the drug molecule is secreted into milk, lactation during consumption is not recommended.
Considering oral administration and mild side effects of FIN, it can be useful in management of MS. However, due to the incidence of some rare but serious adverse effects such as systemic viral infections, macular edema, and cardiovascular complications, physicians should investigate patient’s clinical status and underlying comorbidities carefully.