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Association details:
| Biomarker: | ER Y537S |
|---|---|
| Cancer: | Breast Cancer |
| Drug: | palazestrant (OP-1250) (Estrogen receptor antagonist, Selective estrogen receptor degrader) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
OP-1250: a potent orally available complete antagonist of estrogen receptor-mediated signaling that shrinks wild type and mutant breast tumors
Published date:
10/09/2020
Excerpt:
...identified OP-1250, an orally available complete antagonist with activity in multiple xenograft models expressing wild type and Y537S mutant ER....OP-1250 completely blocked AF1 signaling of both wild type and mutant ER, degraded the receptor, blocked estrogen-stimulated proliferation in breast cells, and shrank breast tumors expressing wild type and mutant ER in xenograft models....OP-1250 is a potent, novel ER antagonist with best in class potential. OP-1250 is orally available in all tested species, completely antagonizes both AF1 and AF2 of the ER, degrades the receptor, and shrinks breast tumors expressing both wild type and mutant receptor.
