Tirabrutinib
Tirabrutinib is a highly selective, irreversible Bruton's tyrosine kinase (BTK) inhibitor that covalently binds to cysteine 481 in the BTK active site, blocking B-cell receptor and toll-like receptor signaling pathways that drive proliferation and survival of malignant B cells in lymphoma and leukemia. It is approved in Japan for primary central nervous system lymphoma and relapsed or refractory B-cell follicular lymphoma. Its CNS penetration makes it particularly valuable for primary CNS lymphoma.
分子量
454.5000 g/mol
LogP
3.00
TPSA
105.00 Ų
Lipinski 五规则
符合
治疗领域
作用机制
Irreversibly inhibits Bruton's tyrosine kinase (BTK), a key enzyme in the B-cell receptor signaling pathway that drives the survival and proliferation of malignant B cells.
Pharmacokinetics (PK)
Pharmacodynamics (PD)
Irreversibly inhibits Bruton's tyrosine kinase (BTK), a key enzyme in the B-cell receptor signaling pathway that drives the survival and proliferation of malignant B cells.
二维结构
Cite this structure
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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
Molecular Formula
C25H22N6O3
HBD / HBA
1 / 6
可旋转键数
4
重原子数
34
No targets recorded
Target interaction data is not yet available for this drug.
No interactions recorded
Drug interaction data is not yet available for this compound.
No side effects recorded
Side effect data is not yet available for this drug.
常见问题
Tirabrutinib is a highly selective, irreversible Bruton's tyrosine kinase (BTK) inhibitor that covalently binds to cysteine 481 in the BTK active site, blocking B-cell receptor and toll-like receptor signaling pathways that drive proliferation and survival of malignant B cells in lymphoma and leukemia. It is approved in Japan for primary central nervous system lymphoma and relapsed or refractory B-cell follicular lymphoma. Its CNS penetration makes it particularly valuable for primary CNS lymphoma.
Irreversibly inhibits Bruton's tyrosine kinase (BTK), a key enzyme in the B-cell receptor signaling pathway that drives the survival and proliferation of malignant B cells.
Yes, Tirabrutinib is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.
References & Data Sources
- ChEMBL — European Bioinformatics Institute (EBI). CHEMBL4071161. Open-access bioactivity database.
- PubChem — National Center for Biotechnology Information (NCBI). CID 54755438. Chemical information database.
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.
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