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Elsubrutinib is an inhibitor of Bruton’s tyrosine kinase (BTK; IC50 = 0.18 µM for the catalytic domain).1 It inhibits IgG-stimulated IL-6 release in primary human monocytes, decreases IgM-mediated proliferation of primary human B cells, and reduces IgE-stimulated increases in histamine plasma levels. Elsubrutinib reduces anti-dsDNA IgG antibody plasma levels, reduces proteinuria, and increases survival in a mouse model of lupus nephritis accelerated by IFN-α. It inhibits paw swelling and ankle joint bone volume loss in a rat model of collagen-induced arthritis.
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