Bruton's tyrosine kinase inhibition—An emerging therapeutic strategy in immune-mediated dermatological conditions

Pedro Mendes-Bastos, Ana Brasileiro, Pavel Kolkhir, Stefan Frischbutter, Jörg Scheffel, Sherezade Moñino-Romero, Marcus Maurer

Research output: Contribution to journalReview articlepeer-review

25 Citations (Scopus)
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Bruton's tyrosine kinase (BTK), a member of the Tec kinase family, is critically involved in a range of immunological pathways. The clinical application of BTK inhibitors for B-cell malignancies has proven successful, and there is strong rationale for the potential benefits of BTK inhibitors in some autoimmune and allergic conditions, including immune-mediated dermatological diseases. However, the established risk-to-benefit profile of “first-generation” BTK inhibitors cannot be extrapolated to these emerging, non-oncological, indications. “Next-generation” BTK inhibitors such as remibrutinib and fenebrutinib entered clinical development for chronic spontaneous urticaria (CSU); rilzabrutinib and tirabrutinib are being studied as potential treatments for pemphigus. Promising data from early-phase clinical trials in CSU suggest potential for these agents to achieve strong pathway inhibition, which may translate into measurable clinical benefits, as well as other effects such as the disruption of autoantibody production. BTK inhibitors may help to overcome some of the shortcomings of monoclonal antibody treatments for immune-mediated dermatological conditions such as CSU, pemphigus, and systemic lupus erythematosus. In addition, the use of BTK inhibitors may improve understanding of the pathophysiological roles of mast cells, basophils, and B cells in such conditions.

Original languageEnglish
Pages (from-to)2355-2366
JournalAllergy: European Journal of Allergy and Clinical Immunology
Issue number8
Early online date17 Feb 2022
Publication statusPublished - Aug 2022


  • Bruton's tyrosine kinase inhibitor
  • chronic spontaneous urticaria
  • fenebrutinib
  • pemphigus
  • remibrutinib


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