Routes of
administration Oral Legal status Investigational Biological half-life 31–34 hrs Molar mass 460.974 g/mol | ATC code none Metabolism Formula C23H25ClN2O4S | |
 | ||
Excretion Feces (57–80%, 26% unchanged), urine (10–18%) | ||
Ponesimod (INN, codenamed ACT-128800) is an experimental drug for the treatment of multiple sclerosis (MS) and psoriasis. It is being developed by Actelion.
Contents
Clinical trials
In a 2009–2011 Phase II clinical trial including 464 MS patients, ponesimod treatment resulted in fewer new active brain lesions than placebo, measured during the course of 24 weeks.
In a 2010–2012 Phase II clinical trial including 326 patients with psoriasis, 46 or 48% of patients (depending on dosage) had a reduction of at least 75% Psoriasis Area and Severity Index (PASI) score compared to placebo in 16 weeks.
Adverse effects
Common adverse effects in studies were temporary bradycardia (slow heartbeat), usually at the beginning of the treatment, dyspnoea (breathing difficulties), and increased liver enzymes (without symptoms). No significant increase of infections was observed under ponesimod therapy. QT prolongation is detectable but was considered to be too low to be of clinical importance in a study.
Mechanism of action
Like fingolimod, which is already approved for the treatment of MS, ponesimod blocks the sphingosine-1-phosphate receptor. This mechanism prevents lymphocytes (a type of white blood cells) from leaving lymph nodes. Ponesimod is selective for subtype 1 of this receptor, S1P1.