鞘氨醇-1-磷酸受体
药理学
药代动力学
1-磷酸鞘氨醇
药效学
受体
医学
临床药理学
鞘氨醇
内科学
作者
Pierre-Éric Juif,Stephan Kraehenbuehl,Jasper Dingemanse
标识
DOI:10.1080/17425255.2016.1196188
摘要
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 S1P1 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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