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Association details:
| Biomarker: | BCR-ABL1 T315I |
|---|---|
| Cancer: | Chronic Myeloid Leukemia |
| Drug: | dasatinib (c-KIT inhibitor, Bcr-abl tyrosine kinase inhibitor, Src kinase inhibitor, EphA2 receptor antagonist, PDGFR β antagonist) + Tasigna (nilotinib) (Bcr-abl tyrosine kinase inhibitor) |
| Direction: | Resistant |
Evidence:
Source:
Title:
BCR-ABL tyrosine kinase inhibitors in the treatment of Philadelphia chromosome positive chronic myeloid leukemia: A review
Excerpt:
The second-generation BCR-ABL TKIs nilotinib (Tasigna®) and dasatinib (Sprycel®), showed significant activity in clinical trials in patients intolerant or resistant to imatinib therapy, except in those patients with the T315I BCR-ABL mutation.
DOI:
https://doi.org/10.1016/j.leukres.2010.04.016
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:
Compared with single agents, each of the 3 combinations (imatinib mesylate + nilotinib, imatinib mesylate + dasatinib, and nilotinib + dasatinib) was more effective at reducing the outgrowth of resistant cell clones (Figure 3)In all cases, a more profound suppression of growth was observed with the combinations as compared with single agents. Sequencing revealed only T315I in resistant clones, with the exception of the lowest concentrations of imatinib mesylate (400 nM) and nilotinib (50 nM), whereby F359C and Y253H were recovered in addition to T315I (Table S2).
DOI:
10.1182/blood-2006-02-004580
