Puneet Varma (Editor)

Siponimod

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Routes of administration
  
By mouth

Synonyms
  
BAF-312

PubChem CID
  
44599207

Molar mass
  
516.26 g/mol

ATC code
  
None

CAS Number
  
1230487-00-9

ChemSpider
  
29315058

Siponimod fileselleckchemcomdownloadsstructbaf312sipon

Siponimod shows promise for secondary progressive multiple sclerosis


Siponimod (INN, code name BAF312) is a selective sphingosine-1-phosphate receptor modulator for oral use that is an investigational drug for multiple sclerosis (MS). It is intended for once-daily oral administration.

Contents

As of January 2016 it is in a phase III clinical trial for secondary progressive MS due to complete December 2016.

Gavin talks about the results of the siponimod trial


Clinical trials

(June 8, 2009) It is in Phase II trial. "A back-up compound for fingolimod, BAF 312" is in Phase II studies. It is being tested for the first time on people having multiple sclerosis. Worldwide 275 patients will participate in this phase II trial the outcome of which is to establish what the optimal dosage of BAF312 is for patients affected with multiple sclerosis for use in further trials. In order to identify "the optimal dosage", participants in group I will be randomly selected to take either placebo, or BAF312 in doses of 0.5 mg/day, 2 mg/day, or 10 mg/day and will be regularly controlled in order to measure and determine the effectiveness, the tolerability and the safety of the dosages.

A phase III trial should run from December 2012 to December 2016.

Approvals and indications

None yet

Mechanism of action

Siponimod binds selectively to some of the Sphingosine-1-phosphate receptor forms — including Sphingosine-1-phosphate receptor 1 — found on lymphocytes and other cell types.

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 (8 in number) that it modulates. It is selective for the -1 and -5 SIP receptors.

References

Siponimod Wikipedia