Ponesimod is a sphingosine 1-phosphate receptor modulator indicated to treat relapsing multiple sclerosis. Fingolimod's activity at sphingosine 1-phosphate receptor 3 was suspected to be responsible for a portion of it's adverse effects, and so more selective modulators were developed.
- Mechanism
- Curator reviewed · 7 references
The sphingosine 1-phosphate receptor 1 (S1P1R) is expressed on the surface of lymphocytes and detects sphingosine 1-phosphate (S1P) at nanomolar concentrations. S1P is a metabolite of the cell membrane component, sphingomyelin. As sphingomyelin degrades, lymphocytes respond to agonism of S1P1R by concentration gradients of S1P. Lymphocytes leave the lymphoid organs in response to higher concentrations of S1P in blood and lymph. Ponesimod modulates this response by stimulating and internalizing S1P1R on lymphocytes, effectively blinding them to concentration gradients of S1P, reducing the number of lymphocytes in blood. Ponesimod is roughly 650 times more selective for S1P1R than S1P.
- Primary indication
- Ponesimod is indicated to treat adults with relapsing forms of multiple sclerosis, including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease.Curator reviewed · 4 structured indications
- Formula / weight
- C23H25ClN2O4S · 460.97 g/mol (avg)
- First approval
- Canada, 2025 · United States, 2021 · European Union, 2022
- Code names
- ACT-128800
- Brand names
Resolves to
LPAUOXUZGSBGDU-STDDISTJSA-NSMILESCCC\N=C1/S\C(=C/C2=CC=C(OC[C@H](O)CO)C(Cl)=C2)C(=O)N1C1=CC=CC=C1CWhat you can answer from here — as of April 23, 2024
Which drugs share a target with Ponesimod, and which of those have an active Phase 3 trial?
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