Ibrutinib (PCI-32765, PCI32765)，又称依鲁替尼、伊布鲁替尼或伊布替尼，是一种不可逆的Btk选择性抑制剂，IC₅₀值为0.5 nM，可用于治疗慢性淋巴细胞白血病和套细胞淋巴瘤。Ibrutinib与BTK活性位点上Cys481共价结合，阻碍Btk活性，进而抑制BCR信号通路活化，BCR信号通路对B淋巴细胞的增殖、分化和信息传递至关重要。

参考文献

1.Honigberg LA, et al. The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy. Proc Natl Acad Sci U S A. 2010 Jul 20;107(29):13075-80.

2.Herman SE, et al. Bruton tyrosine kinase represents a promising therapeutic target for treatment of chronic lymphocytic leukemia and is effectively targeted by PCI-32765. Blood. 2011 Jun 9;117(23):6287-96.

3.Chang BY, et al. The Bruton tyrosine kinase inhibitor PCI-32765 ameliorates autoimmune arthritis by inhibition of multiple effector cells. Arthritis Res Ther. 2011 Jul 13;13(4):R115.

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