Mayzent: 7 things you should know

Medically reviewed by Carmen Pope, BPharm. Last updated on July 3, 2023.

1. How it works

• Mayzent is a brand (trade) name for siponimod that may be used to treat various forms of multiple sclerosis.
• Mayzent (siponimod) works by binding with high affinity to two receptors on the surface of lymphocytes (a type of white blood cell) called S1P receptors 1 and 5. This prevents them from leaving the lymph nodes and getting into the bloodstream. The exact way Mayzent works in Multiple Sclerosis is unknown, but it may be due to this reduction in the migration of lymphocytes from the lymph nodes into the central nervous system which may lower inflammation.
• Mayzent belongs to the class of medicines known as sphingosine-1-phosphate (S1P) receptor modulators. It may also be called a small molecule drug or a selective immunosuppressant.

2. Upsides

• May be used to treat relapsing forms of multiple sclerosis, including clinically isolated syndrome, relapsing-remitting disease (RRMS), and active secondary progressive disease (SPMS with relapses).
• Taken orally once a day. There is a 5-day titration period, which starts with 0.25mg once a day and slowly builds up to a 2mg/day dose. If one titration dose is missed for more than 24 hours, treatment needs to be started back at day 1.
• Helps to decrease the frequency of relapse symptoms. Significantly slows down disability progression in people with active secondary progressive disease (SPMS with relapses), but does not cure MS.
• Some people with commercial insurance may be eligible for a $0 copay card. The annual maximum you can towards your copay card is $18,000. Most Medicare plans cover Mayzent, but you may be responsible for an out-of-pocket copay. Savings may also be available for other types of insurance or if you have no insurance.
• Novartis offers the Alongside MS Support Program for patients prescribed Mayzent. Call 1-877-MAYZENT (1-877-629-9368) for more information. This program pairs the patient with a coordinator who will help them start treatment, get the needed lab tests before treatment, and answer any insurance-related questions.
• May be taken with or without food.
• Available as 0.25mg and 2mg tablets.
• No dosage adjustments are needed in people with liver or kidney disease. Has not been studied in end-stage renal disease or hemodialysis, but due to the high protein binding of Mayzent (>99.9%), hemodialysis is not expected to alter the blood levels of Mayzent.

3. Downsides

If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:

• A headache, high blood pressure, elevations in certain liver function tests, such as transaminases, an increased risk of falls, edema in the feet and legs, nausea, or dizziness. Serious side effects may include slowed heart rate (bradycardia), infections, or macular edema (a build-up of fluid in the eyes that may affect your vision). macular edema was reported in 1.8% of Mayzent-treated patients compared to 0.2% of patients receiving a placebo. Most cases occurred within the first four months of therapy.
• Long-term treatment may increase a person's risk of developing basal cell carcinomas. Periodic skin examinations are recommended for all patients.
• Several tests are required before starting Mayzent, such as CYP2C9 genotype determination, a complete blood count, an eye examination that includes an evaluation of the fundus (including the macula), recent (within 6 months) liver function tests (including transaminase and bilirubin levels), and a cardiac evaluation (including an ECG) to determine if preexisting conduction abnormalities are present.
• Not suitable for people who have experienced a heart attack, unstable angina, stroke, or certain other cardiovascular events in the past 6 months, of CYP2C93/3 genotype, or with Mobitz type II second-degree heart block or other cardiac conduction abnormalities.
• Mayzent needs to be titrated up slowly over 5 days to the recommended maintenance dose of 2 mg/day. If treatment with Mayzent is interrupted for 4 or more consecutive days then the titration regimen will need to be reinitiated.
• Reduces lymphocyte count by 20% to 30% in a dose-dependent way. This increases the risk for infection, some of which may be serious or fatal, such as cryptococcal meningitis. Delay initiation of treatment with Mayzent in patients with a severe active infection until resolution. S1P receptor modulators have also been associated with Progressive multifocal leukoencephalopathy (PML), an opportunistic viral infection of the brain. Symptoms include progressive weakness on one side of the body, vision disturbances, confusion, and personality changes. Posterior reversible encephalopathy syndrome (PRES) has also been reported in people receiving an S1P receptor modulator. Symptoms include cognitive deficits, behavioral changes, or visual disturbances.
• Mayzent interacts with several other medications. Some may not be suitable for coadministration with Mayzent including drugs that could slow the heart rate or atrioventricular conduction, and antineoplastic, immunosuppressive, or immune-modulating treatments (or a prior history of use). See interactions below for more details.
• May cause reactivation of herpes viral infections. Patients should be tested for antibodies to varicella-zoster virus before starting Mayzent treatment. Vaccinate antibody-negative patients before commencing treatment.
• Avoid administration of live attenuated vaccines while patients are taking Mayzent and for 4 weeks after stopping treatment. Vaccines may be less effective if administered during Mayzent treatment. Discontinue Mayzent one week before and for 4 weeks after a planned vaccination.
• People with certain cardiovascular conditions (such as a slow heart rate of fewer than 55 beats per minute), or a history of heart attack or heart failure should have their first dose of Mayzent administered in a setting where resources are available (such as hourly pulse and blood pressure measurement) to appropriately manage symptomatic bradycardia for the next six hours after the first dose. An ECG should also be obtained from these patients at the end of the Day 1 observation period. Further monitoring is required if the heart rate 6 hours post-dose is less than 45bpm, the lowest value post-dose, or the ECG post-dose shows new onset second-degree or higher AV block.
• Only suitable for people with a certain CYP2C9 genetic type. The dosage of Mayzent needs to be reduced in people with CYP2C9 1/3 or 2/3 genotype. Not suitable for people with a CYP2C93/3 genotype.
• Expensive. The cash price for Mayzent 2 mg oral tablet can range from $7600 to $8,000 for a supply of 30 tablets using a free online coupon. The 0.25 mg tablet is about $1,900 for 30 tablets. However, most people do not pay these prices.
• Safety in children has not been established.
• Most people will have to obtain Mayzent through a specialty pharmacy.
• Mayzent may cause harm to a developing baby. All females of reproductive potential should use effective contraception to avoid pregnancy during and for 10 days after stopping Mayzent treatment. No data is available regarding Mayzent and breastfeeding so risks vs benefits need to be considered.
• Not available as a generic; however, a generic is expected in 2024.

Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects

4. Bottom Line

Mayzent is an S1P receptor modulator that may be used to treat relapsing forms of multiple sclerosis in adults. It is only suitable for people with a certain CYP2C9 genetic type and genotype testing must be carried out before initiation. Some people may require monitoring for at least 6 hours after the first dose of Mayzent because it can cause slowing of the heart rate and cardiac conduction abnormalities.

5. Tips

• You must take your medicine every day unless your doctor tells you otherwise. If your treatment is stopped for 4 or more days in a row, you must restart Mayzent with the 4- or 5-day titration schedule. If you stop during the initial titration period, you may need to retake blood tests. Do not discontinue Mayzent without your doctor's advice.
• Mayzent is taken once a day, with or without food. Do not split, crush, or chew Mayzent tablets.
• You can store your Mayzent tablets at room temperature for up to 3 months. Use a refrigerator until use if you need to store them for longer than this.
• Before starting Mayzent, your doctor will perform several tests such as a determination of your CYP2D6 genotype, a complete blood count, an eye examination, liver function tests, and an evaluation of your heart. If you have a preexisting cardiac condition that may be affected by Mayzent, your doctor will monitor you for 6 hours after the first dose of Mayzent and then perform an ECG of your heart to check for any conduction abnormalities.
• Report any side effects of concern, such as vision problems, a racing or irregular heartbeat, shortness of breath, confusion, unexplained nausea, abdominal pain, dark urine, difficulty walking, or edema to your doctor.
• Mayzent interacts with several other medications. Talk to your doctor or pharmacist before taking any other medications because some may not be suitable for coadministration with Mayzent.
• May cause reactivation of herpes viral infections. Your doctor should test you for antibodies to varicella-zoster virus before starting Mayzent treatment and will vaccinate you if you are antibody-negative.
• You should not get vaccinated with vaccines composed of live attenuated viruses during Mayzent treatment and for 4 weeks after stopping treatment.
• Mayzent is not safe to use during pregnancy and is not recommended during breastfeeding. If you are of child-bearing potential you may have to undertake a pregnancy test before starting Mayzent and use reliable contraception while taking it. If you inadvertently become pregnant during Mayzent treatment or within 10 days of stopping it, tell your doctor straight away. Breastfeeding during Mayzent administration is not recommended unless the benefits outweigh the risks.
• Mayzent can increase your risk of developing skin cancers such as basal cell carcinomas. Protect your skin from sunlight and wear protective clothing and use sunscreen with a high sun protection factor. Tell your doctor if you have any changes in the appearance of your skin, including changes in a mole or sores that do not heal.
• Once you stop taking Mayzent, its effects can persist for three or four weeks.

6. Response and effectiveness

• In the pivotal Phase 3 EXPAND study, a placebo-controlled clinical trial of Mayzent significantly lowered disease progression at 3 months by 21%, as well as decreasing the number of relapses and physical and cognitive decline in 1,651 patients with SPMS. Nearly 3 out of 4 people taking Mayzent showed no confirmed disability progression compared to a placebo (74%, compared to 68% taking a placebo). In patients with non-active SPMS, the results were not statistically significant.
• Mayzent is taken as long as it is having a positive effect and the patient is tolerating the medication. In 3-year studies, the length of time patients stayed in the study was variable. For individual patients, the median study duration was 21 months, but this ranged from 1 day to 37 months.
• Rarely, severe exacerbation of disease and disease rebound has been reported after discontinuation of an S1P receptor modulator.
• After stopping Mayzent it remains in the blood for up to 10 days. Lymphocyte counts returned to the normal range in 90% of patients within 10 days of stopping Mayzent; however, low lymphocyte levels may persist for up to 3 to 4 weeks after the last dose. The use of immunosuppressants can have an additive effect.

7. Interactions

Medicines that interact with Mayzent may either decrease its effect, affect how long it works, increase side effects, or have less of an effect when taken with Mayzent. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.

Mayzent interacts with over 500 medications; the majority of these interactions are considered major. Common medications that may interact with Mayzent include:

• antibiotics such as azithromycin, ciprofloxacin, or norfloxacin
• antineoplastics, such as capecitabine, or cyclophosphamide
• antipsychotics, such as clozapine, aripiprazole, or haloperidol
• astemizole
• biologics, such as adalimumab, etanercept, golimumab, or infliximab
• busulfan
• corticosteroids (such as prednisone or dexamethasone)
• CYP2D6 strong inhibitors, such as bupropion, fluoxetine, paroxetine, quinidine, or terbinafine. Avoid
• CYP2D6 moderate inhibitors, such as celecoxib, cimetidine, clobazam, cobicistat, escitalopram, or fluvoxamine. Caution needed
• CYP2D6 moderate inducers such as rifampin
• CYP3A4 moderate or strong inhibitors (such as amprenavir, ciprofloxacin, cyclosporine, clarithromycin, erythromycin, diltiazem, itraconazole, ketoconazole, ritonavir, verapamil, goldenseal, or grapefruit). Avoid
• CYP3A4 inducers (such as carbamazepine, efavirenz, modafinil, prednisone, rifampin, and St. John's Wort). Avoid
• heart medications, particularly those that also slow the heart rate, such as beta-blockers (eg, atenolol, sotalol), digoxin, amiodarone, or flecainide (may be associated with severe bradycardia or heart block)
• herbals, such as black cohosh or brewer's yeast
• HIV medications, such as atazanavir or zidovudine
• hydroxychloroquine
• immunosuppressants such as azathioprine, cyclosporine, or tacrolimus
• interferon
• ketoconazole
• lithium
• live vaccines and some other vaccines, such as BCG, cholera, measles, hepatitis b vaccines, yellow fever, or live influenza vaccines (Mayzent reduces the immune response to vaccination if vaccines are given within 1 week of a Mayzent dose or Mayzent is given 4 weeks after vaccination)
• methotrexate
• oxytocin
• probiotics, such as lactobacillus
• promethazine
• quinine
• tamoxifen.

Mayzent has not been studied in people taking QT-prolonging medications, such as citalopram, chlorpromazine, haloperidol, methadone, or erythromycin. Initiation of Mayzent treatment results in a decreased heart rate which may prolong the QT interval. Use of Class Ia (eg, quinidine, procainamide) and Class III medications (such as amiodarone or sotalol) has been associated with cases of Torsades de Pointes in patients with bradycardia. Consult with a cardiologist.

Mayzent may have additive immune-suppressing effects when given with any other medications such as anticancer drugs, immune-modulating, or immunosuppressive therapies, which may increase a person's risk for infection. Take this into account when switching from drugs with prolonged immune effects, such as natalizumab, teriflunomide, or mitoxantrone.

Note that this list is not all-inclusive and includes only common medications that may interact with Mayzent. You should refer to the prescribing information for Mayzent for a complete list of interactions.

References

• Kappos L, Bar-Or A, Cree BAC, et al. Siponimod versus placebo in secondary progressive multiple sclerosis (EXPAND): a double-blind, randomised, phase 3 study. Lancet. 2018;391(10127):1263‐1273. doi:10.1016/S0140-6736(18)30475-6
• Mayzent (siponimod) [package insert]. Novartis Pharmaceuticals Corporation 01/2023 https://www.drugs.com/pro/mayzent.html

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use Mayzent only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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