Remibrutinib

Remibrutinib is a covalent inhibitor of Bruton’s tyrosine kinase (BTK; IC₅₀ = 1.3 nM).¹ It selectively binds to BTK over bone marrow tyrosine kinase on chromosome X (BMX) and Tec (K_ds = 0.63, 540, and 110 nM, respectively), as well as IL-2-inducible T cell kinase (Itk), EGFR, HER2, HER4, and JAK3 (K_ds = >10,000 nM for all). Remibrutinib is also selective for BTK over a panel of 456 kinases at 1 µM and a panel of 85 receptors, transporters, enzymes, and ion channels at 10 µM. It inhibits anti-IgM-induced activation of primary human B cells (IC₅₀ = 18 nM). Remibrutinib (3 mg/kg) inhibits the formation of IgM antibodies against sheep red blood cells in mice. It also decreases paw swelling in a rat model of collagen-induced arthritis. Formulations containing remibrutinib have been used in the treatment of chronic spontaneous urticaria.

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1. Angst, D., Gessier, F., Janser, P., et al. Discovery of LOU064 (remibrutinib), a potent and highly selective covalent inhibitor of Bruton’s tyrosine kinase. J. Med. Chem. 63(10), 5102-5118 (2020).