Abstract
Tyrosine kinase inhibitors, such as imatinib, have dramatically improved the outcomes for patients with selected cancers. For imatinib, western blotting of phospho-CrkL was an insensitive, indirect, and descriptive method to determine drug efficacy. Greater use of targeted therapies should involve more quantitative evaluation of the target's dose-inhibition. The Src/Abl kinase inhibitor dasatinib has recently been approved for use in Ph+ leukemias after failure with imatinib. Src family kinases (SFK) also play a critical role in nonhematologic cancers. We have developed a flow cytometric assay to measure SFK autophosphorylation levels in blood mononuclear cells and observed a direct correlation between its inhibition and patient dosage. This method provides a sensitive, quick, and quantitative tool to assess drug efficacy.
Original language | English (US) |
---|---|
Pages (from-to) | 1132-1135 |
Number of pages | 4 |
Journal | Pediatric Blood and Cancer |
Volume | 53 |
Issue number | 6 |
DOIs | |
State | Published - 2009 |
Keywords
- Dasatinib
- Phase I
- Src kinases
- Tyrosine kinase inhibitor
ASJC Scopus subject areas
- Oncology
- Pediatrics, Perinatology, and Child Health
- Hematology