Remibrutinib

Remibrutinib
Clinical data
ATC code	L04AA60 (WHO) ;
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;
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;

Remibrutinib is a small molecule drug that acts as a selective and covalent Bruton's tyrosine kinase (BTK) inhibitor. It is in development for the treatment of chronic spontaneous urticaria.^[1]^[2] In November 2023, Novartis announced that the compound "demonstrated clinically meaningful and statistically significant reduction in urticaria activity vs placebo" in a Phase III trial.^[3]

References

^ Maurer, Marcus; Berger, William; Giménez-Arnau, Ana; Hayama, Koremasa; Jain, Vipul; Reich, Adam; Haemmerle, Sibylle; Lheritier, Karine; Walsh, Pauline; Xia, Summer; Storim, Julian (December 2022). "Remibrutinib, a novel BTK inhibitor, demonstrates promising efficacy and safety in chronic spontaneous urticaria". The Journal of Allergy and Clinical Immunology. 150 (6): 1498–1506.e2. doi:10.1016/j.jaci.2022.08.027. hdl:10230/55511. ISSN 1097-6825. PMID 36096203.
^ Maurer, Marcus; Giménez-Arnau, Ana; Jain, Vipul; Tillinghast, Jeffrey; Tolcachier, Alberto; Nigen, Simon; Hayam, Koremasa; Lheritier, Karine; Walsh, Pauline; Haemmerle, Sibylle (February 2022). "Remibrutinib Treatment Improves Quality of Life in Patients with Chronic Spontaneous Urticaria". Journal of Allergy and Clinical Immunology. 149 (2): AB179. doi:10.1016/j.jaci.2021.12.589. S2CID 246522006.
^ "Novartis data show potential of remibrutinib as an oral treatment for chronic spontaneous urticaria providing significant symptom improvement as early as Week 2". Novartis. Retrieved 11 November 2023.

[1] Maurer, Marcus; Berger, William; Giménez-Arnau, Ana; Hayama, Koremasa; Jain, Vipul; Reich, Adam; Haemmerle, Sibylle; Lheritier, Karine; Walsh, Pauline; Xia, Summer; Storim, Julian (December 2022). "Remibrutinib, a novel BTK inhibitor, demonstrates promising efficacy and safety in chronic spontaneous urticaria". The Journal of Allergy and Clinical Immunology. 150 (6): 1498–1506.e2. doi:10.1016/j.jaci.2022.08.027. hdl:10230/55511. ISSN 1097-6825. PMID 36096203.

[2] Maurer, Marcus; Giménez-Arnau, Ana; Jain, Vipul; Tillinghast, Jeffrey; Tolcachier, Alberto; Nigen, Simon; Hayam, Koremasa; Lheritier, Karine; Walsh, Pauline; Haemmerle, Sibylle (February 2022). "Remibrutinib Treatment Improves Quality of Life in Patients with Chronic Spontaneous Urticaria". Journal of Allergy and Clinical Immunology. 149 (2): AB179. doi:10.1016/j.jaci.2021.12.589. S2CID 246522006.

[3] "Novartis data show potential of remibrutinib as an oral treatment for chronic spontaneous urticaria providing significant symptom improvement as early as Week 2". Novartis. Retrieved 11 November 2023.

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