This is the Part I of a two-part account on the discovery and development of clinical candidate BAF312 (siponimod), a sphingosine-1-phosphate receptor 1 and 5 modulator. After extensive structure-activity-relationship studies, we discovered BAF312 through de novo design using FTY720 as the chemical starting point. BAF312 demonstrated good efficacy in preclinical models of multiple sclerosis, and clinical studies in both relapse-remitting multiple sclerosis and secondary progressive multiple sclerosis. This presentation will be focused on the preclinical discovery of BAF312.

Discovery of BAF312, a S1P receptor 1 and 5 modulator

256th National Meeting (2018)

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