Remibrutinib CAS# 1787294-07-8

Remibrutinib (LOU064) is a highly selective, covalent Bruton’s tyrosine kinase (BTK) inhibitor developed by Novartis for autoimmune and inflammatory disorders. In vitro, Remibrutinib exhibits potent inhibition of BTK with an IC₅₀ of approximately 1.3 nM and demonstrates over 400-fold selectivity versus related kinases such as ITK, TEC, and EGFR. In human B cells, it potently blocks B-cell receptor (BCR)-induced CD69 expression with an IC₅₀ of ~3–5 nM, and in basophils, it inhibits IgE-dependent CD63 upregulation with an IC₅₀ of ~6 nM, confirming functional suppression of BTK-mediated signaling. In vivo, Remibrutinib shows strong efficacy in multiple rodent models of inflammation: in the rat collagen-induced arthritis model, oral dosing at 3–10 mg/kg significantly reduced paw swelling and histopathological inflammation scores; in a mouse passive cutaneous anaphylaxis model, ≥1 mg/kg achieved complete suppression of antigen-induced vascular permeability.