ESR1 mutations

ESR1 mutations occur commonly in women with acquired hormonal resistance in endocrine breast cancer treatment.

Studies suggests 30-50% of patients with acquired endocrine resistance have this mutation.

ESR1 mutations occur in the ligand-binding domain of the estrogen receptor.

The mutations activate ER independent of ligand binding.

The presence of the mutation confers activation of the ER, which can lead to resistance to standard endocrine therapies.

ESR1
mutations are largely acquired with hormonal treatment.

Fulvestrant has activity in ESR1 muted tumors.

CDK 4/6 inhibitors have anti-tumor activity in patients with ESR1 mutations who have progressed on prior endocrine therapy.

Lasofoxifene may be effective in the ESR1 mutation breast cancers.

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