Remibrutinib

Medication used to treat chronic spontaneous urticaria From Wikipedia, the free encyclopedia

Remibrutinib, sold under the brand name Rhapsido, is a medication used for the treatment of chronic spontaneous urticaria.[1] Remibrutinib is an oral, small molecule kinase inhibitor that inhibits Bruton's tyrosine kinase (BTK).[1] It is taken by mouth.[1]

Trade namesRhapsido
License data
Quick facts Clinical data, Trade names ...
Remibrutinib
Clinical data
Trade namesRhapsido
License data
Routes of
administration
By mouth
ATC code
Legal status
Legal status
Identifiers
  • N-[3-[6-Amino-5-[2-[methyl(prop-2-enoyl)amino]ethoxy]pyrimidin-4-yl]-5-fluoro-2-methylphenyl]-4-cyclopropyl-2-fluorobenzamide
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
PDB ligand
Chemical and physical data
FormulaC27H27F2N5O3
Molar mass507.542 g·mol−1
3D model (JSmol)
  • CC1=C(C=C(C=C1NC(=O)C2=C(C=C(C=C2)C3CC3)F)F)C4=C(C(=NC=N4)N)OCCN(C)C(=O)C=C
  • InChI=1S/C27H27F2N5O3/c1-4-23(35)34(3)9-10-37-25-24(31-14-32-26(25)30)20-12-18(28)13-22(15(20)2)33-27(36)19-8-7-17(11-21(19)29)16-5-6-16/h4,7-8,11-14,16H,1,5-6,9-10H2,2-3H3,(H,33,36)(H2,30,31,32)
  • Key:CUABMPOJOBCXJI-UHFFFAOYSA-N
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Medical uses

Remibrutinib is indicated for the treatment of chronic spontaneous urticaria in adults who remain symptomatic despite H1 antihistamine treatment[1]

Side effects

Remibrutinib is generally well-tolerated in patients with chronic spontaneous urticaria, but common side effects include upper respiratory tract infections, headache, nasopharyngitis, and mild gastrointestinal symptoms such as diarrhea and nausea. Most adverse events are classified as mild to moderate, with serious side effects being rare; elevations in liver enzymes and transient neutropenia have also been reported but typically do not require treatment discontinuation.[2][3]

Mechanism of action

Remibrutinib is a selective inhibitor of Bruton's tyrosine kinase (BTK), a key signaling protein found in mast cells and basophils that regulates their activation and degranulation via pathways involving the FcεRI and B-cell receptor. By irreversibly binding to BTK, remibrutinib blocks intracellular signaling required for the release of histamine and other inflammatory mediators, thereby reducing the immune cell-driven processes underlying chronic spontaneous urticaria. This mechanism enables suppression of urticaria symptoms upstream from antihistamines, and may also modulate autoimmune activity in some patients.[3]

Society and culture

Remibrutinib was approved for medical use in the United States in September 2025.[4]

Names

Remibrutinib is the international nonproprietary name.[5]

Remibrutinib is sold under the brand name Rhapsido.[4]

References

Further reading

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