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Association details:
| Biomarker: | BCR-ABL1 F486S |
|---|---|
| Cancer: | Chronic Myeloid Leukemia |
| Drug: | imatinib (c-KIT inhibitor, Bcr-abl tyrosine kinase inhibitor, PDGFR inhibitor) |
| Direction: | Resistant |
Evidence:
Source:
Title:
Detection of BCR-ABL mutations in patients with CML treated with imatinib is virtually always accompanied by clinical resistance, and mutations in the ATP phosphate-binding loop (P-loop) are associated with a poor prognosis
Excerpt:
The mutations, Leu248Val at the N-terminal and Ser417Tyr, Glu459Lys, and Phe486Ser at the C-terminal of the kinase domain have not previously been described….Lost CCR (17), dose increased to 800 mg, lost MCR (24), acquired imatinib resistance.
DOI:
https://doi.org/10.1182/blood-2002-09-2896
Source:
Title:
Activity of Bosutinib, Dasatinib, and Nilotinib Against 18 Imatinib-Resistant BCR/ABL Mutants
Excerpt:
In our study, we investigated the activity of bosutinib, dasatinib, imatinib, and nilotinib against a panel of 18 mutated forms of BCR/ABL associated with imatinib resistance in CML and Ph+ acute lymphoblastic leukemia patients. The results are listed in Figure 1 (Table 1 lists all the actual values for the relative concentration that inhibits 50%).
DOI:
10.1200/JCO.2008.19.8853
