Chronic Spontaneous Urticaria and Bruton Tyrosine Kinase: A Multispecialty Expert Discussion - Episode 6
Overview of BTK Inhibitors in Development for CSU Treatment
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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.
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
