remibrutinib (LOU064) / Novartis - LARVOL DELTA

Bruton's Tyrosine Kinase Inhibitor Attenuates Skin Lesions in an Atopic Dermatitis Mouse Model by Suppressing Th2 Inflammation and Mast Cell Activation (EAACI 2025) - "Method An atopic dermatitis (AD)-like mouse model was established through topical application of MC903 from day 0 (D0) to D14. These findings were corroborated at the protein level using IHC and ELISA, confirming the suppression of key cytokine expression. Conclusion This study highlights the role of remibrutinib in reducing clinical symptoms, suppress mast cell degranulation, and downregulate key Th2 cytokines, supporting its role as a promising therapeutic strategy for AD."

IO biomarker • Late-breaking abstract • Preclinical • Atopic Dermatitis • Dermatitis • Immunology • Inflammation

Bruton's Tyrosine Kinase Inhibitor Attenuates Mast Cell Activation via Both FceRI- and MRGPRX2-Mediated Pathways (EAACI 2025) - "Method Remibrutinib and fenebrutinib were used to inhibit BTK signaling. Conclusion BTK inhibitors attenuate both FceRI- and MRGPRX2-mediated mast cell activation. These findings highlight the protective role of BTK inhibitors in the treatment of CSU, not only by suppressing immunoglobulin synthesis but also by directly inhibiting mast cell activation."

Immunology

Remibrutinib improves chronic spontaneous urticaria independent of baseline immunoglobulin E levels in the phase 3 REMIX studies (EAACI 2025) - "Ertas et al. Allergy 2018; 73(3):705-712"

P3 data • Immunology

Remibrutinib demonstrates sustained control of angioedema in patients with chronic spontaneous urticaria: 52-week treatment results from the phase 3 REMIX studies (EAACI 2025) - "Remibrutinib also showed greater reduction in weekly Urticaria Activity Scores vs placebo, with improvement observed as early as week 1 (−13.1 vs −3.4), and the effect was sustained up to week 52 (at week 52: −24.3 for remibrutinib patients and −24.4 for placebo-remibrutinib transitioned patients). Conclusion In patients with angioedema at BL, remibrutinib showed fast improvements in angioedema activity, achieving higher AAS7=0 response rates vs placebo as early as week 1, with effects sustained up to week 52 in 82% of patients."

Clinical • P3 data • Immunology

Evaluating remibrutinib in the treatment of chronic spontaneous urticaria. (PubMed, Immunotherapy) - "The next step involves administering omalizumab, a monoclonal antibody targeting IgE, however, a subset of patients may not respond to this treatment underscoring the necessity for alternative treatment options. The safety profile was also commendable, with no significant treatment-related adverse events requiring therapy cessation or posing immediate health risks to patients. These results indicate that remibrutinib may become a preferred oral treatment for patients with moderate to severe CSU who do not adequately respond to standard therapies."

Journal • Review • Chronic Spontaneous Urticaria • Dermatology • Immunology • Inflammation • Urticaria

Remibrutinib in Chronic Spontaneous Urticaria. (PubMed, N Engl J Med) - No abstract available

Journal • Chronic Spontaneous Urticaria • Dermatology • Immunology • Urticaria

Remibrutinib in Chronic Spontaneous Urticaria. Reply. (PubMed, N Engl J Med) - No abstract available

Journal • Chronic Spontaneous Urticaria • Dermatology • Immunology • Urticaria

Remibrutinib in Chronic Spontaneous Urticaria. (PubMed, N Engl J Med) - No abstract available

Journal • Chronic Spontaneous Urticaria • Dermatology • Immunology • Urticaria

Remibrutinib in Chronic Spontaneous Urticaria. (PubMed, N Engl J Med) - No abstract available

Journal • Chronic Spontaneous Urticaria • Dermatology • Immunology • Urticaria

Study of Remibrutinib (LOU064) Efficacy and Safety and Exploration of Its Mechanism of Action in Participants With Chronic Urticaria (clinicaltrials.gov) - P2 | N=44 | Recruiting | Sponsor: Novartis Pharmaceuticals | Not yet recruiting ➔ Recruiting

Enrollment open • Chronic Spontaneous Urticaria • Dermatology • Immunology • Urticaria

Novel inhibitors of the scaffolding function of BTK selectively and potently block BTK signaling and are efficacious in preclinical models of chronic spontaneous urticaria (SID 2025) - "Although no BTK inhibitors are yet approved for dermatologic diseases, LOU064 (remibrutinib, Novartis) has demonstrated Phase 3 efficacy in CSU and encouraging Phase 2 data in hidradenitis suppurativa...In a clinically-relevant mouse model of CSU, BTK SH2 inhibitors achieve efficacy equivalent to BTK TKIs. Selective, potent, and durable inhibitors of BTK's scaffolding function have the potential to safely enable broader clinical efficacy in dermatologic disease."

Late-breaking abstract • Preclinical • Chronic Spontaneous Urticaria • CNS Disorders • Dermatology • Hidradenitis Suppurativa • Immunology • Inflammatory Arthritis • Multiple Sclerosis • Rheumatoid Arthritis • Rheumatology • Urticaria • PLCG2

Next generation Bruton's tyrosine kinase inhibitors - characterization of in vitro potency and selectivity. (PubMed, Eur J Pharmacol) - "BTKi ranked in their selectivity as follows (most selective to least): remibrutinib, fenebrutinib, evobrutinib, orelabrutinib, rilzabrutinib and tolebrutinib. These data suggest that next generation BTKi show important differences in their in vitro target binding and selectivity when compared under the same conditions."

Journal • Preclinical • Allergy • Immunology

Biological and target synthetic treatments for chronic spontaneous urticaria: A systematic review and network meta-analysis. (PubMed, Clin Transl Allergy) - "The findings of this study indicate that the biological agent omalizumab 300 mg and the oral small molecule remibrutinib at doses of 35 mg, 25 mg, or 10 mg are recommended for patients with antihistamine-refractory CSU."

Clinical • Journal • Retrospective data • Chronic Spontaneous Urticaria • Dermatology • Immunology • Urticaria

Remibrutinib: FDA decision for chronic spontaneous urticaria in H2 205 (Novartis) - Q1 2025 Results: Regulatory submission for Hidradenitis suppurativa in 2028 or later

FDA approval • Filing • Chronic Spontaneous Urticaria • Hidradenitis Suppurativa • Immunology

Remibrutinib: Data readout from P3 RECHARGE1 trial (NCT06799000) for Hidradenitis suppurativa in 2028 (Novartis) - Q1 2025 Results: Data readout from P3 RECHARGE2 trial (NCT06840392) for Hidradenitis suppurativa in 2028

P3 data • Hidradenitis Suppurativa

24 Weeks Double-blind Randomized Placebo-controlled Trial to Evaluate Efficacy, PK, Safety of LOU064 in Adolescents (12 - <18) With CSU and Inadequate Response to H1-antihistamine Followed by Optional 3 Years Open-label Extension and an Optional 3 Years Safety Long-term Treatment-free Follow-up (clinicaltrials.gov) - P3 | N=100 | Recruiting | Sponsor: Novartis Pharmaceuticals | Trial primary completion date: Nov 2025 ➔ Apr 2026

Trial primary completion date • Chronic Spontaneous Urticaria • Dermatology • Immunology • Urticaria

Remibrutinib Shows Promise for Chronic Hives Relief. (PubMed, JAMA) - No abstract available

Journal • Dermatology • Urticaria

Study of Efficacy, Safety and Tolerability of Remibrutinib in Adult Participants With an Allergy to Peanuts (clinicaltrials.gov) - P2 | N=76 | Completed | Sponsor: Novartis Pharmaceuticals | Active, not recruiting ➔ Completed

Trial completion • Allergy • Food Hypersensitivity • Immunology

Update on the Treatment of Chronic Spontaneous Urticaria. (PubMed, Drugs) - "About 70% of patients with antihistamine-refractory CSU do not reach complete control with omalizumab, the second-line treatment...Several emerging treatments can address these unmet needs including Bruton tyrosine kinase inhibitors, e.g., remibrutinib and rilzabrutinib; anti-KIT monoclonal antibodies, e.g., barzolvolimab; and anti-cytokine therapies, e.g., dupilumab...The most common adverse events were injection site reactions for dupilumab (12%), respiratory tract infections (11%), headache (6%), and petechiae (4%) for remibrutinib and changes in hair color (14%), neutropenia / decreased neutrophil count (9%) and skin hypopigmentation (1%) for barzolvolimab. This review provides an update on the current state of development of treatments for CSU."

Journal • Cardiovascular • Chronic Spontaneous Urticaria • Dermatology • Hematological Disorders • Immunology • Infectious Disease • Neutropenia • Pain • Respiratory Diseases • Urticaria

Study of Remibrutinib (LOU064) Efficacy and Safety and Exploration of Its Mechanism of Action in Participants With Chronic Urticaria (clinicaltrials.gov) - P2 | N=44 | Not yet recruiting | Sponsor: Novartis Pharmaceuticals

New P2 trial • Chronic Spontaneous Urticaria • Dermatology • Immunology • Urticaria

RECHARGE 2: Study to Assess Efficacy Safety and Tolerability of Remibrutinib in Adult Patients With Moderate to Severe Hidradenitis Suppurativa (clinicaltrials.gov) - P3 | N=555 | Recruiting | Sponsor: Novartis Pharmaceuticals | Not yet recruiting ➔ Recruiting

Enrollment open • Dermatology • Hidradenitis Suppurativa • Immunology

Novartis BTK inhibitor to be included in priority review in China for the treatment of urticaria [Google translation] (vbdata.cn) - "Novartis' application for the marketing of a Class 1 new drug, remibrutinib tablets, is planned to be included in the priority review. It is suitable for adult patients with chronic spontaneous urticaria (CSU) who still have symptoms after treatment with H1 antihistamines. This marketing application was previously accepted by the CDE on February 27 this year....The first indication of this product is the treatment of chronic spontaneous urticaria. The Phase 3 clinical study for this indication has achieved positive results."

Priority review • Chronic Spontaneous Urticaria • Immunology

Remibrutinib in Chronic Spontaneous Urticaria. (PubMed, N Engl J Med) - P3 | "Treatment with oral remibrutinib resulted in a significant improvement in a composite measure of itching and hives at week 12. (Funded by Novartis Pharmaceuticals; REMIX-1 and REMIX-2 ClinicalTrials.gov numbers, NCT05030311 and NCT05032157, respectively.)."

Clinical • Journal • Cardiovascular • Chronic Spontaneous Urticaria • Dermatology • Immunology • Urticaria

Remibrutinib Exposure in Cerebrospinal Fluid: Insights from a Study in Healthy Participants (AAN 2025) - P3 | "The distribution of remibrutinib into the CSF may imply that remibrutinib may exert pharmacotherapeutic effects in the central nervous system, potentially benefiting conditions such as MS."

Clinical • CNS Disorders • Multiple Sclerosis

RELIEVE: A Study to Investigate the Efficacy, Safety and Tolerability of Remibrutinib Versus Placebo in Adult Patients With Generalized Myasthenia Gravis (clinicaltrials.gov) - P3 | N=180 | Recruiting | Sponsor: Novartis Pharmaceuticals | Not yet recruiting ➔ Recruiting

Enrollment open • CNS Disorders • Myasthenia Gravis