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.
Молекулярная масса
454,5000 g/mol
LogP
3,00
TPSA
105,00 Ų
Правило пяти Липинского
Соответствует
Терапевтические области
Механизм действия
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.
2D Структура
Cite this structure
Embed this structure
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
Вращаемые Связи
4
Тяжёлые Атомы
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.
Часто задаваемые вопросы
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.
Медицинский отказ от ответственности
This content is for educational and informational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before making medication decisions.
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