Journal
EXPERT OPINION ON DRUG METABOLISM & TOXICOLOGY
Volume 12, Issue 8, Pages 879-895Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/17425255.2016.1196188
Keywords
Autoimmune diseases; cardiodynamic effect; fingolimod; first dose; lymphocytes; ponesimod; S1P(1) receptor modulators
Funding
- Actelion Pharmaceuticals Ltd.
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Introduction: Sphingosine-1-phosphate (S1P) receptor modulators, of which one has received marketing approval and several others are in clinical development, display promising potential in the treatment of a spectrum of autoimmune diseases. Areas covered: Administration of S1P(1) receptor modulators leads to functional receptor antagonism triggering sustained inhibition of the egress of lymphocytes from lymphoid organs. First-dose administration is associated with transient cardiovascular effects. We compiled and discussed available pharmacokinetic, pharmacodynamic, and safety data of selective and non-selective S1P receptor modulators that were investigated in recent years. Expert opinion: The safety profile of S1P receptor modulators is considered better than other classes of immunomodulators and was further improved by the development of up-titration regimens to mitigate first-dose effects. S1P receptor modulators display similar pharmacodynamic effects but have very different pharmacokinetic profiles. Drugs with a rapid elimination are of interest in case of opportunistic infections or pregnancy, whereas the need of re-initiation of up-titration in case of treatment interruption can present a challenge.
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