Remibrutinib

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]

Remibrutinib

Clinical data
Trade names	Rhapsido
License data	US DailyMed: Remibrutinib
Routes of administration	By mouth
ATC code	L04AA60 (WHO)
Legal status
Legal status	US: ℞-only[1]
Identifiers
IUPAC name 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	1787294-07-8
PubChem CID	118107483
IUPHAR/BPS	10457
DrugBank	DB16852
ChemSpider	78317000
UNII	I7MVZ8HDNU
KEGG	D12285
ChEMBL	ChEMBL4483575
PDB ligand	N6Z (PDBe, RCSB PDB)
Chemical and physical data
Formula	C27H27F2N5O3
Molar mass	507.542 g·mol−1
3D model (JSmol)	Interactive image
SMILES 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 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

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

Legal status

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]