Siponimod (formerly known as BAF312) is a selective modulator of specific types of the sphingosine-1-phosphate (S1P) receptor. It is currently being developed as a therapy for secondary progressive multiple sclerosis (SPMS).

Siponimod, under development by Novartis, binds to S1P1 (sub-receptor) on lymphocytes (immune cells) and keeps them inside lymph nodes, preventing them from entering the central nervous system of patients with multiple sclerosis (MS). The anti-inflammatory effect prevents the activation of B- and T-cells that are responsible for myelin damage, while helping to reduce the loss of physical and cognitive function associated with SPMS.

The S1P receptors targeted by siponimod are also found on the surface of brain cells, which play a role in the origin of SPMS. Siponimod crosses the blood-brain barrier and binds to these receptors, potentially controlling activity that would otherwise damage cells and lead to the loss of neurological functions.

Studies of siponimod in MS

Novartis announced positive results from its Phase 3 EXPAND study (NCT01665144). Taking siponimod twice daily significantly reduced the risk of three-month disability progression by 21 percent, compared to study participants who took a placebo. Additionally, siponimod showed a significant positive difference in relapses, brain volume, and number of relapses. Its safety and tolerance profile was comparable to similar drugs.

EXPAND was the largest randomized and controlled trial using patients with SPMS. All of the participants had demonstrated progression of disability for two years prior to the study. The majority of them had non-relapsing SPMS.

Previous Phase 2 studies (NCT00879658) showed that siponimod reduced relapse rates compared to a placebo. MRI brain scans also showed reduced amounts of brain lesions.

The most common side effects reported by study participants were headache, slowing of heart rate, dizziness, and nose and throat infections.

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