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Sphingosine 1-Phosphate Receptor Modulator

Molecular classification
Immunomodulatory agent
01

Overview

Sphingosine 1-phosphate receptor modulators (S1PR modulators) are a class of drugs that target sphingosine 1-phosphate receptors (S1PRs), which are G protein-coupled receptors involved in regulating immune cell trafficking, vascular integrity, and other physiological processes. These drugs have become important in the treatment of autoimmune diseases, especially multiple sclerosis (MS), due to their ability to modulate lymphocyte movement and reduce neuroinflammation. The main mechanism by which these modulators exert their effect is by binding to the receptor on lymphocytes, effectively antagonizing it, limiting lymphocyte egress from lymph nodes.

Other names
S1PR modulatorS1P receptor modulator
02

Mechanism of action

Functional antagonism via ligand-induced internalization; blocks egress of immune cells from lymph nodes, reducing circulating lymphocytes.

03

Biological functions

Immune response modulationLymphocyte trafficking regulation
04

Disease associations

Multiple sclerosisPsoriasisHost vs. graft diseaseAutoimmune diseases
05

Safety considerations

BradycardiaOff-target effects due to receptor subtype non-selectivity
06

Interacting drugs

Fingolimod

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