Fingolimod is an immunosuppressant that has been derived from the fungus Isaria sinclairii. In 2010, it was approved by the United States Food and Drug Administration (FDA), becoming the first disease-modifying oral drug to be approved. The drug was approved to minimize relapses of multiple sclerosis and was noted to delay the progression of disability in patients.
This drug was synthesized for the first time in 1992 from myriocin through a type of chemical modification. The benefits related to both organ transplants and multiple sclerosis were then studied. Fingolimod was proved to be useful during a phase III kidney transplant clinical trial, but it was shown to be no better or worse than the common method of care used during an organ transplant.
The phase III clinical trials relating to multiple sclerosis were where a majority of the positive results were seen. In two separate phase III clinical trials, it was shown that fingolimod could reduce the relapse rate in multiple sclerosis by more than 50 percent when compared with both a placebo as well as an active comparator, interferon beta-1a. Seventy percent of multiple sclerosis patients who were taking FTY720, the specific drug, were relapse-free after three years of treatment.
There are several common side effects to taking fingolimod. During testing, two patients died from a herpes infection, although there was no conclusive evidence that it was because of fingolimod. The fingolimod also was being taken at much higher dosage levels than are recommended. Additional side effects include shortness of breath, headaches, bronchitis, increased liver enzymes and hypertension.
Fingolimod has been shown to be an effective way to prevent multiple sclerosis relapses, but how it works is unclear. It has been classified as a sphingosine 1-phosphate receptor modulator. This means that it binds to receptors in the body and prevents lymphocytes from exiting lymph nodes, which decreases their count in the bloodstream.
The FDA approval of fingolimod was based on the largest clinical trial program that had ever been submitted for a multiple sclerosis drug. It included data that was combined from a wide variety of clinical studies. From this data, it was concluded that fingolimod is effective at reducing relapses, minimizing the risk of symptom progression and decreasing the number of brain lesions detected by magnetic resonance imaging (MRI).
