Ibrutinib: a first in class covalent inhibitor of Bruton's tyrosine kinase.

@article{Davids2014IbrutinibAF,
  title={Ibrutinib: a first in class covalent inhibitor of Bruton's tyrosine kinase.},
  author={Matthew S. Davids and Jennifer Rose Brown},
  journal={Future oncology},
  year={2014},
  volume={10 6},
  pages={957-67}
}
Ibrutinib (formerly PCI-32765) is a potent, covalent inhibitor of Bruton's tyrosine kinase, a kinase downstream of the B-cell receptor that is critical for B-cell survival and proliferation. In preclinical studies, ibrutinib bound to Bruton's tyrosine kinase with high affinity, leading to inhibition of B-cell receptor signaling, decreased B-cell activation and induction of apoptosis. In clinical studies, ibrutinib has been well-tolerated and has demonstrated profound anti-tumor activity in a… CONTINUE READING
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