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Siponimod is available as a 0.25 mg, 1 mg, and 2 mg oral tablet.

Siponimod is a sphingosine 1-phosphate receptor modulator and is used to treat relapsing forms of multiple sclerosis (MS).

Siponimod is a sphingosine 1-phosphate (S1P) receptor modulator. It attaches to the S1P receptor protein found on your white blood cells. This blocks white blood cells from leaving your lymph nodes and releasing into the body. The exact way Siponimod works to treat MS is unknown. But it’s thought to lower the number of white blood cells that reaches your nervous system where they can cause nerve damage.

Your dose of Siponimod will depend on your genetic makeup, which can affect how well your body can break down the medication. For this reason, you’ll need to do genetic testing before starting Siponimod so your provider can choose the appropriate dose for you. In general, the typical starting dose is 0.25 mg by mouth once daily. Then, your provider will slowly raise your dose over 4 or 5 days to reach the target maintenance dose of 1 mg or 2 mg once daily.

Siponimod is a safe and effective treatment when used for FDA licensed indications. However, like all medications, they may give you unwanted side effects. You should always discuss potential side effects with your physician to ensure the medication is suitable and right for you. You should not use this medication in the following:

• Patients with a CYP2C9*3/*3 genotype
• In the last 6 months, experienced myocardial infarction, unstable angina, stroke, TIA, decompensated heart failure requiring hospitalization, or Class
  III/IV heart failure
• Presence of Mobitz type II second-degree, third-degree AV block, or sick sinus syndrome, unless patient has a functioning pacemaker

Common side effects of Siponimod:

• Headache
• High blood pressure
• Higher liver enzyme levels in the blood
• Falls
• Swelling of the arms and legs
• Nausea
• Dizziness
• Diarrhea
• Low heart rate
• Pain in arms or legs

Serious side effects are rare with Siponimod. Contact your healthcare provider immediately if you experience any of the following.

• Infection: fever, difficulty breathing, diarrhea, weakness, cough, stomach pain, sweating, chills
• Dangerously slow heart rate: dizziness, tiredness, weakness, confusion, feeling faint, trouble breathing, chest pain
• Liver problems: nausea, vomiting, stomach pain, swelling of your stomach, yellowing of your skin or the whites of your eyes, clay-colored stool
• Skin cancer: skin changes, swollen lymph nodes
• Brain problems: severe headaches, visual changes, difficulty staying awake, weakness on one side of the body, dizziness, trouble speaking, seizure

The following medications may interact with Siponimod:

• Vaccination: Avoid live-attenuated vaccines during and for up to 4 weeks after treatment with Siponimod
• CYP2C9 and CYP3A4 Inhibitors: Increase in Siponimod exposure; concomitant use of Siponimod with moderate CYP2C9 and moderate or strong CYP3A4 inhibitors is not recommended.
• CYP2C9 and CYP3A4 Inducers: Decrease in Siponimod exposure; concomitant use of Siponimod with moderate CYP2C9 and strong
• CYP3A4 inducers is not recommended

Various FDA-approved generic manufacturers

Siponimod may harm your unborn baby. Talk to your healthcare provider right away if you become pregnant while taking Siponimod or if you become pregnant within 10 days after you stop taking Siponimod. If you are a woman who can become pregnant, you should use effective birth control during your treatment with Siponimod and for at least 10 days after you stop taking Siponimod. There is a registry for women who become pregnant during treatment with Siponimod. If you become pregnant while taking Siponimod, talk to your healthcare provider about registering with the MotherToBaby Pregnancy Study in Multiple Sclerosis. The purpose of this registry is to collect information about your health and your baby’s health. For more information or to register, contact MotherToBaby by calling 1-877-311-8972, by sending an email to MotherToBaby@health.ucsd.edu, or go to Mother to baby

• Mayzent