Ozanimod (formerly RPC1063)

Experimental Medications: NEW S1P Receptor Modulators

Company: Celgene

  • Oral medication being studied at several doses
  • Ozanimod is being studied in RRMS

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Ozanimod (RPC1063) is a selective modulator of one type of S1P receptor, S1P1. [Correction: Ozanimod is actually a selective modulator of two types of S1P receptors: S1P1 and S1P5. This note was added after publication.] It is given as a once-daily pill, and was studied in a Phase II trial called RADIANCE, where the experimental medicine was compared at two different doses with placebo. A total of 258 RRMS patients were studied in this trial, which began with a seven-day gradual titration of ozanimod up to the full dose under investigation. The double-blind study then ran for 24 weeks, followed by a yearlong safety-extension period.

At the end of the initial 24-week treatment period, patients in both groups taking ozanimod showed an 86-percent decrease in the cumulative number of gadolinium-enhanced lesions compared to the placebo group. The relapse rates also decreased in the treatment groups compared with placebo, with a 31-percent decrease in the 0.5-mg group and a 53-percent decrease in the 1-mg group.

The most common side effects reported were nasopharyngitis, headache, and urinary tract infections, as well as mild elevations in liver enzymes in some participants. Notably, no serious cardiac events were reported in the subjects receiving ozanimod.

In February 2016, the 72-week extension data of the RADIANCE trial were presented. These showed a continued reduction in relapses and gadolinium-enhancing lesions for those patients who remained on ozanimod, with all efficacy results favoring the 1-mg dose over the lower 0.5-mg dose. No new safety or tolerability issues were identified during this blinded extension phase of the trial. The drug has moved into a larger, Phase III version of the RADIANCE trial,17 where it is being compared with Avonex in 1,200 subjects with RRMS. This trial is expected to run through the end of 2017.
Siponimod (BAF312)

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