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Spotlight -

This Year In Medicine 2025

Opinion|Videos|February 27, 2025

Overview of BTK Inhibitors in Development for CSU Treatment

Author(s)Giselle Mosnaim, MD, MS , Shyam Joshi, MD , Mark Lebwohl, MD

Panelists discuss how newer Bruton tyrosine kinase (BTK) inhibitors being developed for chronic spontaneous urticaria (CSU), particularly remibrutinib (in phase 3 trials) and rilzabrutinib (in phase 2), are designed to be more selective than earlier oncology-focused BTK inhibitors, potentially reducing off-target effects like bleeding, cardiovascular complications, and GI issues.

Episodes in this series

EP. 1 Chronic Spontaneous Urticaria and Bruton Tyrosine Kinase: A Multispecialty Expert Discussion

EP. 1 Chronic Spontaneous Urticaria and Bruton Tyrosine Kinase: A Multispecialty Expert Discussion

EP. 2 Pathophysiology of Chronic Spontaneous Urticaria

EP. 3 Current CSU Treatment Approach and the Role of Bruton Tyrosine Kinase

EP. 3 Current CSU Treatment Approach and the Role of Bruton Tyrosine Kinase

EP. 4 BTK Inhibition as a Strategy for CSU Treatment

EP. 4 BTK Inhibition as a Strategy for CSU Treatment

EP. 5 How BTK Inhibitors Differ From Current CSU Treatment Approaches

EP. 5 How BTK Inhibitors Differ From Current CSU Treatment Approaches

EP. 6 Overview of BTK Inhibitors in Development for CSU Treatment

EP. 6 Overview of BTK Inhibitors in Development for CSU Treatment

EP. 7 Differentiating BTK Inhibition From Genetic BTK Deficiency

EP. 7 Differentiating BTK Inhibition From Genetic BTK Deficiency

EP. 8 Overview of Remibrutinib Phase 3 Clinical Trials in CSU

EP. 8 Overview of Remibrutinib Phase 3 Clinical Trials in CSU

EP. 9 CSU Burden of Disease and Quality of Life

EP. 9 CSU Burden of Disease and Quality of Life

EP. 10 Early Clinical Trial Data for Rilzabrutinib in CSU and Future Study Directions

EP. 10 Early Clinical Trial Data for Rilzabrutinib in CSU and Future Study Directions

EP. 11 How BTK Inhibitors Might Address Unmet Treatment Needs in CSU

EP. 11 How BTK Inhibitors Might Address Unmet Treatment Needs in CSU

EP. 12 Evolving Paradigm for CSU Treatment

EP. 12 Evolving Paradigm for CSU Treatment

EP. 13 Additional Data Needs for BTK Inhibitors in CSU

EP. 13 Additional Data Needs for BTK Inhibitors in CSU

EP. 14 Key Takeaways and Considerations for the Use of BTK Inhibitors in CSU Treatment

EP. 14 Key Takeaways and Considerations for the Use of BTK Inhibitors in CSU Treatment

Video content above is prompted by the following:

Let’s talk a bit about the BTK inhibitors currently being developed and studied for the treatment of CSU:
Remibrutinib: phase 3 trials, with 12-, 24-, and 52-week data available; inhibits BTK in mast cells, basophils, and B cells
Rilzabrutinib: currently in phase 2 trials
How do the BTK inhibitors under development for CSU treatment differ from earlier generations of BTK inhibitors used in oncology and other autoimmune diseases?
Older BTK inhibitors have limited selectivity and irreversibly inhibit additional kinases, increasing potential for off-target adverse effects (AEs; bleeding effects, cardiotoxicity [hypertension, atrial fibrillation], gastrointestinal effects, and rash).
Remibrutinib binds to the inactive conformation of BTK and shows higher selectivity, limiting the potential for these off-target AEs

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