Ponesimod (ACT-128800) is a directly bioavailable, rapidly reversible sphingosine-1-phosphate (S1P) receptor modulator, highly selective for the subtype 1 (S1P1 receptor). It acts by blocking the egress of lymphocytes from the lymphoid organs, thus limiting the entry of autoreactive cells into the central nervous system. Unlike fingolimod, ponesimod does not require monitoring of the first dose, thanks to a 14-day uptitration regimen, which markedly reduces the incidence of cardiodynamic effects related to the initiation of therapy. Results from the OPTIMUM phase III trial demonstrated the superiority of ponesimod over teriflunomide on disease activity markers, without unexpected safety concerns. Furthermore, the drug is eliminated within 1 week of discontinuation, allowing for the reversibility of its effects. Ponesimod was recently approved in both the U.S. and E.U. for the treatment of relapsing forms of multiple sclerosis. This review summarizes the pharmacological characteristics of ponesimod and the main studies that led to its approval.
Ponesimod to treat multiple sclerosis / Ianniello, A; Pozzilli, C. - In: DRUGS OF TODAY. - ISSN 1699-3993. - 57:12(2021), pp. 745-758. [10.1358/dot.2021.57.12.3353166]
Ponesimod to treat multiple sclerosis
Ianniello, A
Primo
;Pozzilli, CUltimo
2021
Abstract
Ponesimod (ACT-128800) is a directly bioavailable, rapidly reversible sphingosine-1-phosphate (S1P) receptor modulator, highly selective for the subtype 1 (S1P1 receptor). It acts by blocking the egress of lymphocytes from the lymphoid organs, thus limiting the entry of autoreactive cells into the central nervous system. Unlike fingolimod, ponesimod does not require monitoring of the first dose, thanks to a 14-day uptitration regimen, which markedly reduces the incidence of cardiodynamic effects related to the initiation of therapy. Results from the OPTIMUM phase III trial demonstrated the superiority of ponesimod over teriflunomide on disease activity markers, without unexpected safety concerns. Furthermore, the drug is eliminated within 1 week of discontinuation, allowing for the reversibility of its effects. Ponesimod was recently approved in both the U.S. and E.U. for the treatment of relapsing forms of multiple sclerosis. This review summarizes the pharmacological characteristics of ponesimod and the main studies that led to its approval.File | Dimensione | Formato | |
---|---|---|---|
Ianniello_Ponesimod_2021.pdf
solo gestori archivio
Note: Ianniello_Ponesimod_2021
Tipologia:
Versione editoriale (versione pubblicata con il layout dell'editore)
Licenza:
Tutti i diritti riservati (All rights reserved)
Dimensione
268.94 kB
Formato
Adobe PDF
|
268.94 kB | Adobe PDF | Contatta l'autore |
Ponesimod to treat Multiple Sclerosis_revised draft.pdf
accesso aperto
Note: Ianniello_Ponesimod_2021_preprint
Tipologia:
Documento in Pre-print (manoscritto inviato all'editore, precedente alla peer review)
Licenza:
Creative commons
Dimensione
281.28 kB
Formato
Adobe PDF
|
281.28 kB | Adobe PDF |
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.