Spleen tyrosine kinase (SYK) inhibitor Hematological cancer therapy

Zeng Hui Wei, Jagadish Koya, Xing Duo Dong, Sandra E. Reznik, Zhe Sheng Chen

Research output: Contribution to journalArticlepeer-review


Non-Hodgkin lymphoma (NHL) is the most common malignant hematologic malignancy in the world. B-cell NHL, which accounts for 90% of NHL cases, includes various refractory subtypes with high rates of recurrence. Available treatments are not curative and have significant adverse effects. Thus, novel agents currently in clinical trials should be considered for treating B-cell NHL. Entospletinib (GS-9973), a selective inhibitor of spleen tyrosine kinase (SYK), inactivates SYK, Bruton tyrosine kinase (BTK) and phosphoinositide 3-kinase (PI3K), and inhibits the B-cell receptor (BCR) signaling pathway, which further suppresses malignant cell proliferation and induces apoptosis. It showed a high efficacy profile in both preclinical and clinical studies in treatments for B-cell NHL, especially for diffuse large B-cell lymphoma, mantle cell lymphoma and B-cell chronic lymphocytic leukemia. This review summarizes the mechanism of entospletinib and its potential application for B-cell NHL and other hematologic malignancies.

Original languageEnglish (US)
Pages (from-to)99-107
Number of pages9
JournalDrugs of the Future
Issue number2
StatePublished - Feb 2022


  • Acute myeloid leukemia
  • B-cell chronic lymphocytic leukemia
  • B-cell non-Hodgkin lymphoma
  • Diffuse large B-cell lymphoma
  • Entospletinib
  • GS-9973
  • Mantle cell lymphoma
  • SYK inhibitors
  • Spleen tyrosine kinase

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)


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