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Association details:
| Biomarker: | BCR-ABL1 F317V |
|---|---|
| Cancer: | Chronic Myeloid Leukemia |
| Drug: | dasatinib (c-KIT inhibitor, Bcr-abl tyrosine kinase inhibitor, Src kinase inhibitor, EphA2 receptor antagonist, PDGFR β antagonist) |
| Direction: | Resistant |
Evidence:
Source:
Excerpt:
Treatment recommendations based on BCR-ABL1 mutation profile...The table below lists the BCR-ABL1 mutations that should not be treated with bosutinib, dasatinib or nilotinib in the second-line setting…Dasatinib…T315I/A, F317L/V/I/C, or V299L
Source:
Title:
Chronic myeloid leukaemia: ESMO Clinical Practice Guidelines for diagnosis, treatment and follow-up
Excerpt:
In particular, V299L, T315A and F317L/V/I/C are resistant to dasatinib. Y253H, E255K/V and F359V/C/I are resistant to nilotinib, and V299L to bosutinib.
DOI:
10.1093/annonc/mdx219
Source:
Title:
Comparative analysis of two clinically active BCR-ABL kinase inhibitors reveals the role of conformation-specific binding in resistance
Excerpt:
To examine the potential role of conformational binding properties in drug resistance, we mapped the mutations in BCR-ABL capable of conferring resistance to BMS-354825....T315I conferred the greatest degree of resistance to BMS-354825 with an IC50 >750-fold over WT BCR-ABL. T315A and F317V, two previously uncharacterized mutants, show the next highest IC50s, 40- to 90-fold over WT.
DOI:
10.1073/pnas.0409770102
Source:
Title:
Comparison of imatinib mesylate, dasatinib (BMS-354825), and nilotinib (AMN107) in an N-ethyl-N-nitrosourea (ENU)–based mutagenesis screen: high efficacy of drug combinations
Excerpt:
F317V was also recovered from an E coli–based mutagenesis screen in the presence of 50 nM dasatinib and has 40-fold reduced sensitivity to dasatinib compared with unmutated BCR-ABL.
DOI:
10.1182/blood-2006-02-004580
