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Association details:
| Biomarker: | ER Y537N |
|---|---|
| Cancer: | Breast Cancer |
| Drug: | tamoxifen (Estrogen receptor antagonist) + fulvestrant (Selective estrogen receptor degrader) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
Activating ESR1 mutations in hormone-resistant metastatic breast cancer
Excerpt:
Interestingly, ESR1 with each of the five LBD alterations identified in this study was inhibited by tamoxifen and fulvestrant in a dose-dependent fashion and did not exhibit the inverted response to anti-estrogens that the synthetic Inv-mut-AA2 mutant did....The IC50 (half-maximal inhibitory concentration) values for both 4-hydroxytamoxifen and fulvestrant were two- to fourfold higher for all mutants compared to wild-type ESR1. Fulvestrant exhibited greater maximal inhibition than 4-hydroxytamoxifen for all the mutants tested (Supplementary Figs. 4 and 5).
DOI:
10.1038/ng.2823
