Chronic activation of the B-cell antigen receptor (BCR) signaling pathway performs a critical function in the pathogenesis of numerous subtypes of B-cell malignancies and transforms normal cells into malignant cells. Bruton tyrosine kinase (BTK) is a member of the TEC family of tyrosine kinases and is a key regulator of the BCR signaling pathway. BTK inhibition has emerged as a new target for therapeutic intervention in B-cell malignancies. This review summarizes recent developments of BTK inhibitors in B-cell malignan-cies.%B细胞受体(B-cell receptor,BCR)信号通路在B细胞肿瘤的发生、发展中起关键作用,其慢性持续的激活状态使正常细胞具备转化为恶性肿瘤细胞的能力。布鲁顿酪氨酸激酶(bruton tyrosine kinase,BTK)是非受体型酪氨酸激酶TEC家族的一员,在BCR信号通路的活化过程中起着关键的作用。通过BTK小分子抑制剂调控BCR信号转导,已经成为治疗某些B细胞淋巴瘤的新靶点,并为B细胞非霍奇金淋巴瘤(B-cell non-Hodgkin's lymphoma,B-NHL)的治疗带来新突破。本文将对现有BTK小分子抑制剂在临床上的应用现状作一综述。
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