|Drug class||Sphingosine-1-phosphate receptor modulator|
|Main uses||Multiple sclerosis (MS)|
|Side effects||Headache, high blood pressure, liver problems|
|Typical dose||1 to 2 mg per day|
|Chemical and physical data|
|Molar mass||516.605 g·mol−1|
|3D model (JSmol)|
Siponimod, sold under the brand name Mayzent, is a medication used to treat multiple sclerosis (MS). Specifically it is used for relapsing forms of MS including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease. It is taken by mouth.
Common side effects include headache, high blood pressure, and liver problems. Other side effects may include infection, macular edema, arrhythmias, and posterior reversible encephalopathy syndrome. It should not be used in people who are allergic to peanuts or to soya. It works by blocking sphingosine-1-phosphate receptors.
Siponimod was approved for medical use in the United States in 2019 and Europe in 2020. At a dose of 2 mg per day, it costs about 8,400 USD per month in the United States as of 2021. In the United Kingdom this amount costs the NHS about £1,800. In the United States it is only available through a specialty pharmacy.
Siponimod is indicated for the treatment of secondary progressive multiple sclerosis (SPMS), which is the progressive neurological decline of multiple sclerosis that happens independent of acute relapses. In active SPMS, siponimod decreases the risk of disability and MS relapses.
It is started at 0.25 mg once per day and increased over the first to 1 to 2 mg per day.
Mechanism of action
This binding inhibits the migration of the lymphocytes to the location of the inflammation (e.g. in MS).
Siponimod may be very similar to fingolimod but preventing lymphopenia, one of its main side effects, by preventing egress of lymphocytes from lymph nodes. Siponimod may be more selective in the particular sphingosine-1-phosphate receptors (five in number) that it modulates. It is selective for the -1 and -5 SIP receptors.
In March 2019, siponimod was approved in the United States to treat adults with relapsing forms of multiple sclerosis (MS), to include clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease.
The efficacy of siponimod was shown in a clinical trial of 1,651 patients that compared siponimod to placebo in people with secondary progressive multiple sclerosis (SPMS) who had evidence of disability progression in the prior two years and no relapses in the three months prior to enrollment. The primary endpoint of the study was the time to three-month confirmed progression in disability. The trial was conducted at 294 centers in Asia, Australia, Canada, Europe, South America, and the United States.
Siponimod was approved for medical use in Australia in October 2019.
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- "Drug Trials Snapshots: Mayzent". U.S. Food and Drug Administration (FDA). 19 April 2019. Archived from the original on 28 September 2019. Retrieved 24 November 2019. This article incorporates text from this source, which is in the public domain.
- "Drug Approval Package: Mayzent (siponimod)". U.S. Food and Drug Administration (FDA). 3 May 2019. Retrieved 22 January 2020. This article incorporates text from this source, which is in the public domain.
- Clinical trial number NCT01665144 for "Exploring the Efficacy and Safety of Siponimod in Patients With Secondary Progressive Multiple Sclerosis (EXPAND)" at ClinicalTrials.gov
- "Novartis announces EU approval of Mayzent (siponimod) for adult patients with secondary progressive multiple sclerosis (SPMS) with active disease". Novartis (Press release). 20 January 2020. Retrieved 23 January 2020.
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- "Siponimod fumarate". Drug Information Portal. U.S. National Library of Medicine.
- "Australian Public Assessment Report for Siponimod" (PDF). Therapeutic Goods Administration (TGA).