Novartis Announces FDA Approval of Remibrutinib, First Oral BTK Inhibitor for Chronic Spontaneous Urticaria

On November 10, Novartis announced that Remibrutinib tablets have been approved by the U.S. FDA for the treatment ofAdult patients with chronic spontaneous urticaria (CSU) who still have symptoms after receiving H1 antihistamine treatmentRimibutinib tablets are taken orally twice daily, with no need for injections or laboratory monitoring. According to the press release, this product is the first Bruton's tyrosine kinase inhibitor (BTKi) approved by the FDA for the treatment of CSU.Rimibrutinib tablets inhibit the release of histamine and other pro-inflammatory mediators in mast cells by targeting and blocking the BTK signaling pathway, offering a new option for CSU treatment.

CSU is a mast cell-driven disease believed to be caused by immune dysregulation. In patients with CSU, the immune system can be activated via immunoglobulin E (IgE) or immunoglobulin G (IgG) pathways, leading to the activation of the BTK pathway in certain immune cells—mast cells and basophils. Once BTK is activated, it triggers the release of histamine and other pro-inflammatory mediators, causing common CSU clinical symptoms such as angioedema and pruritic wheals. The symptoms of CSU are unpredictable and may recur repeatedly and persist for six weeks or longer without a clear trigger, negatively impacting sleep, work, and mental health. Currently, antihistamines are the first-line treatment, but even with increased doses, more than half of patients continue to experience symptoms. For patients who respond poorly to antihistamines, injectable treatments are available, but fewer than 20% of eligible patients receive this therapy.

The approval of Rilzabrutinib Tablets for CSU indication is based on the results of the Phase 3 REMIX-1 and REMIX-2 clinical trials, which enrolled patients who still had symptoms under second-generation H1 antihistamine treatment. Rilzabrutinib Tablets demonstrated superiority over placebo at week 12 in terms of baseline changes in pruritus (ISS7), hives (HSS7), and weekly urticaria activity (UAS7). Compared with placebo, a significantly higher proportion of patients treated with Rilzabrutinib Tablets achieved well-controlled disease (UAS7≤6) as early as week 2 and at week 12.About one-third of patients achieved complete resolution of pruritus and wheals by Week 12.。Symptom relief can be observed in as fast as two weeks., with good safety and no need for laboratory index monitoring. The most common adverse reactions (incidence rate ≥3%) of Remibrutinib Tablets include upper respiratory tract infection, petechiae, headache, etc.

Novartis has submitted marketing applications for Remibrutinib Tablets for the treatment of CSU in multiple countries and regions, including the EU, Japan, and China. The marketing application for this product in China has been granted priority review by the NMPA.

References:
[1] The U.S. Food and Drug Administration (FDA) approved Novartis' Rilabutin tablets for the treatment of chronic spontaneous urticaria (CSU). Rilabutin tablets are currently the only oral, targeted BTK inhibitor approved for CSU. From https://www.prnasia.com/story/511086-1.shtml

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