Drug intelligence / Profile preview

BI-1002494

Development stage
Preclinical
Lead developer
Boehringer
Modality
Small Molecules
Administration
Oral
01

Overview

**BI-1002494** is a potent, selective small molecule inhibitor of spleen tyrosine kinase (SYK), developed as an in vitro and in vivo tool compound and for experimental therapeutic use. It displays strong oral bioavailability and sustained plasma exposure in animal models. BI-1002494 shows high selectivity for SYK, with an IC50 of approximately 115 nM for inhibition of high-affinity IgE receptor-mediated mast cell and basophil degranulation, and higher concentrations are required to inhibit B-cell receptor-mediated activation. It is used to modulate SYK-mediated immune processes and has shown efficacy in preclinical models of allergy, asthma, arthritis, and thrombosis, including reduction of platelet activation, arterial thrombosis, and infarct size in ischemic stroke models[1][3][5][6][7][9].

Other names
(R)-4-{(R)-1-[7-(3,4,5-trimethoxy-phenyl)-[1,6]naphthyridin-5-yloxy]-ethyl}pyrrolidin-2-one
02

Targets

SYK (Spleen Tyrosine Kinase)

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