Siponimod

Siponimod
Clinical data
Synonyms BAF-312
Routes of
administration		 By mouth
ATC code
  • None
Identifiers
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
Formula C29H35F3N2O3
Molar mass 516.26 g/mol
3D model (JSmol)

Siponimod (INN,[1] 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.[2]

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

Clinical trials

(June 8, 2009) It is in Phase II trial. "A back-up compound for fingolimod, BAF 312" is in Phase II studies.[3] 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.[4]

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.[5] It is selective for the -1 and -5 SIP receptors.[2]

References

  1. ↑ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 67" (PDF). World Health Organization. 2012. p. 86. Retrieved 18 February 2017.
  2. 1 2 Siponimod (BAF312) for the Treatment of Secondary Progressive Multiple Sclerosis: Design of the Phase 3 EXPAND Trial (P07.126)
  3. ↑ Multiple sclerosis and the pharmaceutical industry/Medicines in development for MS: abpi.org.uk 2009
  4. ↑ Exploring the Efficacy and Safety of Siponimod in Patients With Secondary Progressive Multiple Sclerosis (EXPAND)
  5. ↑ WO 2008000419, Hiestand, Peter C; Schnell, Christian, "S1P Receptor modulators for treating multiple sclerosis", assigned to Novartis
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