Tirabrutinib

Tirabrutinib
Clinical data
Trade names	Velexbru
Other names	GS-4059; ONO-4059
ATC code	L01EL06 ( WHO );
Legal status
Legal status	JP: Rx-only;
Identifiers
	IUPAC name 6-amino-9-[(3R)-1-(but-2-ynoyl)pyrrolidin-3-yl]-7-(4-phenoxyphenyl)purin-8-one;
CAS Number	1351636-18-4 ;
PubChem CID	54755438 ;
DrugBank	DB15227 ;
ChemSpider	58171734 ;
UNII	LXG44NDL2T ;
KEGG	D12594 ;
ChEMBL	ChEMBL4071161 ;
PDB ligand	7GB ( PDBe , RCSB PDB );
Chemical and physical data
Formula	C25H22N6O3
Molar mass	454.490 g·mol−1
3D model (JSmol)	Interactive image ;
	SMILES CC#CC(=O)N1CC[C@@H](n2c(=O)n(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1;
	InChI InChI=1S/C25H22N6O3/c1-2-6-21(32)29-14-13-18(15-29)31-24-22(23(26)27-16-28-24)30(25(31)33)17-9-11-20(12-10-17)34-19-7-4-3-5-8-19/h3-5,7-12,16,18H,13-15H2,1H3,(H2,26,27,28)/t18-/m1/s1; Key:SEJLPXCPMNSRAM-GOSISDBHSA-N;

Last updated October 03, 2025

Tirabrutinib (brand name Velexbru) is a drug used for the treatment of autoimmune disorders and hematological malignancies.^[1]^[2]

Tirabrutinib was approved in March 2020 in Japan for the treatment of recurrent or refractory primary central nervous system lymphoma.^[1] In addition, tirabrutinib is in clinical development by Ono Pharmaceutical and Gilead Sciences ^[3] in the United States, Europe, and Japan for autoimmune disorders, chronic lymphocytic leukemia, B cell lymphoma, Sjogren's syndrome, pemphigus, and rheumatoid arthritis.^[1]

Tirabrutinib is an irreversible inhibitor of Bruton's tyrosine kinase.^[4]

References

1 2 3 Dhillon S (June 2020). "Tirabrutinib: First Approval". Drugs. 80 (8): 835–840. doi:10.1007/s40265-020-01318-8. PMID 32382949. S2CID 218531327.
↑ "Tirabrutinib". NCI Drug Dictionary. National Institutes of Health.
↑ "Tirabrutinib - Gilead Sciences/Ono Pharmaceutical". Adis Insight.
↑ Liclican A, Serafini L, Xing W, Czerwieniec G, Steiner B, Wang T, et al. (April 2020). "Biochemical characterization of tirabrutinib and other irreversible inhibitors of Bruton's tyrosine kinase reveals differences in on - and off - target inhibition". Biochimica et Biophysica Acta (BBA) - General Subjects. 1864 (4) 129531. doi: 10.1016/j.bbagen.2020.129531 . PMID 31953125.

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[Dhillon-1] 1 2 3 Dhillon S (June 2020). "Tirabrutinib: First Approval". Drugs. 80 (8): 835–840. doi:10.1007/s40265-020-01318-8. PMID 32382949. S2CID 218531327.

[2] "Tirabrutinib". NCI Drug Dictionary. National Institutes of Health.

[3] "Tirabrutinib - Gilead Sciences/Ono Pharmaceutical". Adis Insight.

[4] Liclican A, Serafini L, Xing W, Czerwieniec G, Steiner B, Wang T, et al. (April 2020). "Biochemical characterization of tirabrutinib and other irreversible inhibitors of Bruton's tyrosine kinase reveals differences in on - and off - target inhibition". Biochimica et Biophysica Acta (BBA) - General Subjects. 1864 (4) 129531. doi: 10.1016/j.bbagen.2020.129531 . PMID 31953125.

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