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Association details:
| Biomarker: | ER Y537S |
|---|---|
| Cancer: | Estrogen Receptor Positive Breast Cancer |
| Drug: | palazestrant (OP-1250) (Estrogen receptor antagonist, Selective estrogen receptor degrader) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
OP-1250 prevents tumor spread in a model of metastatic mutant ERa+ breast cancer
Published date:
03/09/2022
Excerpt:
MCF7 cells engineered to express one of the most common and aggressive ERα mutations, Y537S...Mice were treated with 3 and 10 mg/kg of OP-1250 alone or in combination with palbociclib at 70mg/kg and tumor growth was monitored...Our results also suggest that the efficacy seen in the combination study was driven primarily by OP-1250. In total, these results demonstrate the potential use of OP-1250, both alone and in combination with a CDK4/6 inhibitor, to inhibit tumor growth and metastasis in a model of aggressive mutant ER+ MBC.
Source:
Title:
The complete estrogen receptor antagonist OP-1250 shrinks tumors in xenograft models and has favorable preclinical pharmacokinetic attributes
Published date:
11/17/2020
Excerpt:
...orally administered OP-1250 and its ability to shrink breast tumors...OP-1250 shrank ER+ tumors in multiple patient-derived tumor xenografts in mice at daily doses of 3 mg/kg, including in tumors expressing the Y537S allele of ERalpha that confers estrogen-independent growth and tumor resistance.
