Fingolimod hydrochloride

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Fingolimod Hydrochloride is a medication primarily used in the treatment of multiple sclerosis (MS). It is a sphingosine 1-phosphate receptor modulator, which works by sequestering lymphocytes in lymph nodes, preventing them from contributing to an autoimmune reaction.

Pharmacology[edit | edit source]

Fingolimod is a prodrug, which means it is metabolized into its active form in the body. It is converted by sphingosine kinase into fingolimod-phosphate, which acts as a functional antagonist of the sphingosine-1-phosphate receptor. This receptor is found on the surface of lymphocytes, a type of white blood cell involved in the immune response. By binding to this receptor, fingolimod-phosphate prevents the lymphocytes from leaving the lymph nodes and entering the central nervous system, where they would contribute to the inflammation and nerve damage seen in MS.

Clinical Use[edit | edit source]

Fingolimod Hydrochloride is used in the treatment of relapsing forms of multiple sclerosis. It has been shown to reduce the frequency of clinical exacerbations and to delay the accumulation of physical disability. However, it is generally reserved for patients who have not responded adequately to, or cannot tolerate, other treatments for MS due to its potential side effects.

Side Effects[edit | edit source]

The most common side effects of Fingolimod Hydrochloride include headache, flu-like symptoms, diarrhea, and back pain. It can also cause more serious side effects, such as a slow heart rate, infections, and macular edema. Therefore, patients taking this medication require regular monitoring.

History[edit | edit source]

Fingolimod was first synthesized in 1992, and its potential use in MS was identified in the early 2000s. It was approved by the Food and Drug Administration (FDA) in 2010, making it the first oral medication approved for MS.

See Also[edit | edit source]


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Contributors: Prab R. Tumpati, MD