BTK is a non-receptor kinase that plays a crucial role in cancer signaling. BTK plays a crucial role in cancer signaling. BTK is a key mediator in B cell receptor signaling in adaptive immune development and function. In the immune system, BTK plays a role in many pathways and cells outside of B cells, such as T cells and macrophages. Recently, BTK acts as a direct regulator of NLRP3 inflammasome, a key innate inflammatory mechanism. Therefore, people are currently very interested in BTK inhibition as an anti-cancer therapy. It is not only applicable to B-cell malignant tumors, but also to solid tumors. Here, we will introduce a selective orally active BTK inhibitor, Remibrutinib.
Remibrutinib is an Orally Active BTK Inhibitor for Chronic Urticaria Research.
Firstly, Remibrutinib is a potent and orally active bruton tyrosine kinase (BTK) inhibitor with an IC50 value of 1 nM. Meanwhile, Remibrutinib inhibits BTK activity with an IC50 value of 0.023 μM in blood. Importantly, Remibrutinib has the potential for Chronic urticaria (CU) treatment. Secondly, Remibrutinib inhibits Btk enzymatic activity with an IC50 value of 1 nM in a biochemical enzyme assay. In vitro B cell activation assay, Remibrutinib inhibits Btk enzymatic activity in blood with an IC50 value of 0.023 μM. The whole blood is collected from the abdominal aorta of anaesthetized adult male Lewis rats.
Finally, Remibrutinib is a potent and orally active BTK inhibitor for Chronic urticaria (CU) research.
References:
[1] Kolkhir P, et al. Ann Allergy Asthma Immunol. 2019 Aug 23.