Tirabrutinib
Clinical data
Trade namesVelexbru
Other namesGS-4059; ONO-4059
ATC code
  • None
Legal status
Legal status
  • Rx-only (Japan)
Identifiers
  • 6-Amino-9-[(3R)-1-but-2-ynoylpyrrolidin-3-yl]-7-(4-phenoxyphenyl)purin-8-one
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC25H22N6O3
Molar mass454.490 g·mol−1

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. 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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