Investor Presentaiton
Etrasimod: A Selective S1P1, S1P4, and S1P5 Receptor Modulator
Etrasimod is a novel oral, selective sphingosine 1-
phosphate (S1P) receptor modulator in development
for immuno-inflammatory diseases
S1PR modulators induce internalization and
degradation of the S1P receptor, selectively reducing
migration of T and B lymphocytes out of lymphoid
organs into blood
Etrasimod's unique specificity for the receptor
subtypes S1P1, S1P4, and S1P5 may contribute to its
clinical benefit:risk profile
Why Etrasimod is Potentially Best-In-Class Agent
Differentiated
pharmacology
Lower first-dose
HR effect
Etrasimod is a potent agonist of the S1P1R and a
partial agonist of S1P4R and S1P5R, differentiated
from other S1Ps
Modest, transient, and asymptomatic first-dose
heart rate effect which does not require dose
titration
Rapid onset/offset Rapid depletion of circulating lymphocytes and
rapid recovery upon treatment cessation
of effect
No long-acting
active metabolites
No active metabolites with long t₁/2 nor any
significant DDI liabilities
Pfizer
Inflammation & Immunology
6View entire presentation