Remibrutinib is a highly selective oral, novel covalent Bruton tyrosine kinase inhibitor that might be effective in chronic spontaneous urticaria.
Chronic spontaneous urticaria is characterized by the occurrence of itchy wheals and/or swelling lasting 6 weeks or more. Chronic hives affects about 1% of the population.
First line treatment is the use of a non-sedating second generation antihistamine up to 4 times a day. Stepwise approach to Chronic Urticaria (Chronic Hives)
Many patients do not achieve successful results and then omalizumab, an anti-IgE monoclonal antibody is the next recommended step. However some patients are still symptomatic even with that.
Bruton’s tyrosine kinase (BTK), is located downstream from the IgE receptor, and it is expressed in mast cells, basophils, B cells, macrophages and platelets. BTK inhibitors may be a therapeutic option in chronic hives. It is already being used to treat rheumatoid arthritis and lupus. Activating BTK in mast cells and basophils have resulted in the release of histamine and inflammatory cytokines. Targeting BTK may hinder mast cell mediated histamine release and disrupt autoantibody production. Fenebrutinib another BTK inhibitor has shown promise in chronic hives.
The first BTK inhibitor was introduced in 2013 for the treatment of mantle cell lymphoma and other B cell cancers. Though they can have adverse effects as a result of inhibiting of other kinases besides BTK. Side effects see are diarrhea, fatigue, musculoskelatal pain, neutropenia and an increased risk of infection.
Remibrutinib, is a highly selective BTK inhibitor that is being investigated in patients with moderate to severe chronic hives inadequately controlled with antihistamines.
Patients received remibrutinib for 12 weeks at different doses to study its efficacy in 311 patients. Reduced symptom scores were reported for all doses (from 10mg daily to 100 mg twice a day) and adverse effects were mild or moderate.
Overall, remibrutinib shows potential as a preferred oral treatment for patients with moderate to severe chronic spontaneous urticaria. It has a rapid onset of action and a favorable safety profile.