Pharmacological effects of small molecule BCR-ABL tyrosine kinase inhibitors on platelet function.

ABSTRACT: Tyrosine kinase inhibitors (TKIs) targeting the breakpoint cluster region-ABL fusion protein, such as imatinib (Gleevec), have revolutionized targeted cancer therapies. However, drug resistance and side effects, particularly those affecting hemostasis, continue to pose significant challenges for TKI therapies. As tyrosine kinases serve pivotal roles in platelet hemostatic function, we investigated the potential impact of both established and emerging ABL TKIs on human platelet activities ex vivo. Our study included standard-of-care agents (eg, imatinib and nilotinib) and second-generation ABL inhibitors, including ponatinib and bosutinib, designed to mitigate drug resistance. Additionally, we explored the effects of allosteric inhibitors targeting the myristoyl pocket of ABL (eg, asciminib

SUBMITTER: Zhang Y 

PROVIDER: S-EPMC12920053 | biostudies-literature | 2025 Jan

REPOSITORIES: biostudies-literature