Siponimod

What is Siponimod?

US FDA approved under the brandname Mayzent, Siponimod is a sphingosine 1-phosphate (s1p) receptor modulator indicated for the treatment of relapsing forms of multiple sclerosis (ms)

Siponimod structure

What are the uses of Siponimod?

Mayzent is a sphingosine 1-phosphate (s1p) receptor modulator indicated for the treatment of relapsing forms of multiple sclerosis (ms), to include clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease, in adults.

How does Siponimod work?

• Siponimod is an S1P receptor modulator.
• Siponimod binds with high affinity to S1P receptors 1 and 5.
• Siponimod blocks the capacity of lymphocytes to egress from lymph nodes, reducing the number of lymphocytes in peripheral blood.
• The exact mechanism by which siponimod exerts therapeutic effects in multiple sclerosis is unknown, but may involve reduction of lymphocyte migration into the central nervous system.

Who Should Not Use Siponimod?

• Patients with a CYP2C93/3 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.
• Warnings and precautions
• Infections: mayzent may increase the risk. Obtain a complete blood count (cbc) before initiating treatment. Monitor for infection during treatment. Do not start in patients with active infection.
• Macular edema: an ophthalmic evaluation is recommended before starting treatment and if there is any change in vision while taking mayzent. Diabetes mellitus and uveitis increase the risk.
• Bradyarrhythmia and atrioventricular conduction delays: mayzent may result in a transient decrease in heart rate; titration is required for treatment initiation. Consider resting heart rate with concomitant beta-blocker use; obtain cardiologist consultation before concomitant use with other drugs that decrease heart rate.
• Respiratory effects: may cause a decline in pulmonary function. Assess pulmonary function (e.G., spirometry) if clinically indicated.
• Liver injury: obtain liver enzyme results before initiation. Closely monitor patients with severe hepatic impairment. Discontinue if significant liver injury occurs.
• Cutaneous malignancies: periodic skin examination is recommended.
• Increased blood pressure: monitor blood pressure (bp) during treatment.
• Fetal risk: women of childbearing potential should use effective contraception during and for 10 days after stopping mayzent.

Is Siponimod FDA approved?

Yes. It is US FDA approved under the brandname Mayzent in March of 2019.

How should Siponimod be used?

• Assessments are required prior to initiating mayzent.
• Titration is required for treatment initiation.
• The recommended maintenance dosage is 2 mg.
• The recommended maintenance dosage in patients with a cyp2c9*1/*3 or *2/*3 genotype is 1 mg.
• Administer tablets whole; do not split, crush, or chew.
• First-dose monitoring is recommended for patients with sinus bradycardia, first- or second-degree [mobitz type I] atrioventricular (av) block, or a history of myocardial infarction or heart failure.

What are the dosage forms and brand names of Siponimod?

It comes as tablets of 0.25 mg and 2 mg

What side effects can Siponimod cause?

Most common adverse reactions (incidence greater than 10%) are headache, hypertension, and transaminase increases.

What special precautions should I follow?

• Vaccination: avoid live attenuated vaccines during and for up to 4 weeks after treatment with mayzent.
• Cyp2c9 and cyp3a4 inhibitors: increase in siponimod exposure; concomitant use of mayzent with moderate cyp2c9 and moderate or strong cyp3a4 inhibitors is not recommended.
• Cyp2c9 and cyp3a4 inducers: decrease in siponimod exposure; concomitant use of mayzent with moderate cyp2c9 and strong cyp3a4 inducers is not recommended

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can Siponimod be used in pregnancy?

No

Can Siponimod be used in children?

Not studied in children

What are the active and inactive ingredients in Siponimod?

Active ingredients

• Siponimod

Inactive ingredients

• Lactose monohydrate
• Cellulose, microcrystalline
• Crospovidone, unspecified
• Glyceryl dibehenate
• Silicon dioxide
• Talc
• Titanium dioxide
• Ferric oxide red
• Ferric oxide yellow

What should I know about storage and disposal of Siponimod?

Unopened Containers

• MAYZENT 0.25 mg and 2 mg tablets may be stored at room temperature between 68°F to 77°F (20°C to 25°C) for up to 3 months. If you need to store MAYZENT tablets for more than 3 months, containers should remain unopened and stored in a refrigerator between 36°F to 46°F (2°C to 8°C) until use.

Opened Containers

Bottles

• MAYZENT 0.25 mg and 2 mg tablets may be stored at room temperature between 68°F to 77°F (20°C to 25°C) for up to 3 months.
• Do not refrigerate after opening.

Starter Pack/Blister Card

• MAYZENT 0.25 mg tablets may be stored at room temperature between 68°F to 77°F (20°C to 25°C) for up to 3 months.
• Do not refrigerate after opening.
• Store in original calendarized blister wallet container.
• Keep MAYZENT and all medicines out of the reach of children.

Who manufactures and distributes Siponimod?

• Novartis

• Dailymed label info on Siponimod
• FDA Siponimod

Siponimod Resources
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