Tirabrutinib

Chemical compound
  • None
Legal statusLegal status
  • Rx-only (Japan)
Identifiers
  • 6-Amino-9-[(3R)-1-but-2-ynoylpyrrolidin-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 dataFormulaC25H22N6O3Molar 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. ^ a b c 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.