Discovery of APD334: Design
of a Clinical Stage Functional
Antagonist of the Sphingosine-1-phosphate‑1 Receptor
Posted on 2014-12-11 - 00:00
APD334
was discovered as part of our internal effort to identify
potent, centrally available, functional antagonists of the S1P1 receptor for use as next generation therapeutics for treating
multiple sclerosis (MS) and other autoimmune diseases. APD334 is a
potent functional antagonist of S1P1 and has a favorable
PK/PD profile, producing robust lymphocyte lowering at relatively
low plasma concentrations in several preclinical species. This new
agent was efficacious in a mouse experimental autoimmune encephalomyelitis
(EAE) model of MS and a rat collagen induced arthritis (CIA) model
and was found to have appreciable central exposure.
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Buzard, Daniel J.; Kim, Sun Hee; Lopez, Luis; Kawasaki, Andrew; Zhu, Xiuwen; Moody, Jeanne; et al. (2016). Discovery of APD334: Design
of a Clinical Stage Functional
Antagonist of the Sphingosine-1-phosphate‑1 Receptor. ACS Publications. Collection. https://doi.org/10.1021/ml500389m
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AUTHORS (43)
- DBDaniel J. BuzardSKSun Hee KimLLLuis LopezAKAndrew KawasakiXZXiuwen ZhuJMJeanne MoodyLTLars ThoresenICImelda CalderonBUBrett UllmanSHSangdon HanJLJuerg LehmannTGTawfik GharbaouiDSDipanjan SenguptaLCLorene CalvanoAMAntonio Garrido MontalbanYMYou-An MaCSCarleton SageYGYinghong GaoGSGraeme SempleJEJeff Edwards
