期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 229, 期 -, 页码 -出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2021.114009
关键词
Bruton's tyrosine kinase (BTK) inhibitors; Ibrutinib; Off-target toxicities; Drug resistance; Combination therapy
资金
- Key R&D Program of Jiangsu Province [BE2021677]
- Key Natural Science Foundation of Jiangsu Higher Education Institutions [20KJA350002]
- China Postdoctoral Science Foundation [2018T110533]
- Applied Research Projects of Nantong City [MS12020047]
Bruton's tyrosine kinase (BTK) plays a crucial role in the treatment of hematologic malignancies, but current therapies have limitations. Therefore, researchers are exploring new treatment strategies, such as next-generation BTK inhibitors, BTK-PROTACs, and combination therapies.
Bruton's tyrosine kinase (BTK) regulates multiple important signaling pathways and plays a key role in the proliferation, survival, and differentiation of B-lineage cells and myeloid cells. BTK is a promising target for the treatment of hematologic malignancies. Ibrutinib, the first-generation BTK inhibitor, was approved to treat several B-cell malignancies. Despite the remarkable potency and efficacy of ibrutinib against various lymphomas and leukemias in the clinics, there are also some clinical limitations, such as off-target toxicities and primary/acquired drug resistance. As strategies to overcome these challenges, second- and third-generation BTK inhibitors, BTK-PROTACs, as well as combination therapies have been explored. In this review, we summarize clinical developments of the first-, second- and third-generation BTK inhibitors, as well as recent advances in BTK-PROTACs and ibrutinib-based combination therapies.(c) 2021 Elsevier Masson SAS. All rights reserved.
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