Siponimod (BAF312)

Experimental Medications: NEW S1P Receptor Modulators

Company: Novartis

  • Oral medication studied at several doses
  • Siponimod is being studied in SPMS

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Data from a Phase II dose-finding study of siponimod in people with RRMS were also reported in 2012. Siponimod has a relatively short half-life compared to Gilenya, which means that the drug does not stay in the body as long. Researchers hope that this will minimize cardiac issues.

The trial had a complex design, with the primary goal to determine the most appropriate dosing regimen. One group of 188 patients received placebo or once-daily siponimod in doses of 10 mg, 2 mg, or 0.5 mg for six months. A second group of 109 patients were given one of two additional intermediate doses of 1.25 mg or 0.25 mg for three months.

At six months, the proportion of relapse-free patients as compared to placebo was 84 percent for the 10 mg group, 92 percent for the 2 mg group, and 77 percent for the 0.5 mg group. In the placebo group, 72 percent were relapse-free. After six months, the ARR (annual relapse rate) was lower for the individuals who were taking one of the three higher doses. Additionally, MRI findings showed a reduction in active lesions. The 2 mg dose reached statistical significance versus placebo, with a reduction in active lesions of approximately 80 percent.

A Phase III trial of siponimod in SPMS (the EXPAND trial)18 began recruitment in 2013 and is expected to run through fall 2016. This is the first S1P receptor modulator to be studied in SPMS.

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