A Syk inhibitor
Lanraplenib is an inhibitor of spleen tyrosine kinase (Syk; IC50 = 6.2 nM).1 It is selective for Syk over a panel of 395 kinases but does inhibit JAK2 (IC50 = 120 nM). Lanraplenib reduces anti-IgM- and anti-CD40-induced proliferation of isolated human B cells (EC50 = 108 nM). It also inhibits immune complex-induced production of TNF-α, IL-1β, and IL-6 in human macrophages (EC50s = 180, 90, and 700 nM, respectively). It reduces proteinuria and increases survival in the NZBWF1 mouse model of systemic lupus erythematosus (SLE).
1.Blomgren, P., Chandrasekhar, J., Di Paolo, J.A., et al.Discovery of lanraplenib (GS-9876): A once-daily spleen tyrosine kinase inhibitor for autoimmune diseasesACS Med. Chem. Lett.11(4)506-513(2020)
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