Syk inhibitors in clinical development for hematological malignancies

被引：0
作者：
Delong Liu
Aleksandra Mamorska-Dyga
机构：
[1] The first Affiliated Hospital of Zhengzhou University,Department of Oncology
[2] Department of Medicine,undefined
[3] New York Medical College and Westchester Medical Center,undefined
来源：
Journal of Hematology & Oncology | / 10卷
关键词：
Fostamatinib; Chronic Lymphoid Leukemia (CLL); Bruton’s Tyrosine Kinase; Venetoclax; Idelalisib;
D O I：
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学科分类号：
摘要：
Spleen tyrosine kinase (Syk) is a cytosolic non-receptor protein tyrosine kinase (PTK) and is mainly expressed in hematopoietic cells. Syk was recognized as a critical element in the B-cell receptor signaling pathway. Syk is also a key component in signal transduction from other immune receptors like Fc receptors and adhesion receptors. Several oral Syk inhibitors including fostamatinib (R788), entospletinib (GS-9973), cerdulatinib (PRT062070), and TAK-659 are being assessed in clinical trials. The second generation compound, entospletinib, showed promising results in clinical trials against B-cell malignancies, mainly chronic lymphoid leukemia. Syk inhibitors are being evaluated in combination regimens in multiple malignancies.
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