Drug intelligence / Profile preview

GSK2646264

Development stage
Phase 1
Lead developer
GSK
Modality
Small Molecules
Administration
Topical
01

Overview

GSK2646264 is a small molecule inhibitor of spleen tyrosine kinase (SYK) developed by GSK (GlaxoSmithKline). It was designed as a topical agent for the treatment of IgE-mediated skin diseases, such as chronic spontaneous urticaria and cutaneous lupus erythematosus. The drug acts by inhibiting SYK, thereby reducing the signaling cascade following activation of the IgE–FCεR1α complex on mast cells, which leads to decreased release of inflammatory mediators like histamine. Preclinical and early clinical studies demonstrated its potency and selectivity for SYK over other kinases, with dose-dependent inhibition observed in ex vivo human skin models. Development was discontinued after phase 1 trials for both urticaria and cutaneous lupus erythematosus[1][2][5][7].

Other names
Compound 44Compound44Compound-44
02

Targets

SYK (Spleen Tyrosine Kinase)

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