Indication

ER-positive, HER2-negative, ESR1-mutated breast cancer

Estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative, ESR1-mutated breast cancer is a distinct molecular subtype of mammary carcinoma affecting breast glandular tissue, most frequently identified in patients with locally advanced or metastatic disease. Read more about ER-positive, HER2-negative, ESR1-mutated breast cancer

5 drugs 4 manufacturers

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Drugs that treat it

Common ER-positive, HER2-negative, ESR1-mutated breast cancer therapies.

Showing 1–5 of 5 drugs

VERZENIO (abemaciclib)

ANTINEOPLASTIC- CYCLIN-DEPENDENT KINASE (CDK) 4/6 INHIBITORS·HORMONE RECEPTOR (HR)-POSITIVE, HER2-NEGATIVE ADVANCED BREAST CANCER·+2
Eli Lilly and Company

ETCAMAH (camizestrant)

ANTIESTROGEN·ER-POSITIVE, HER2-NEGATIVE, ESR1-MUTATED BREAST CANCER
AstraZeneca Pharmaceuticals
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About ER-positive, HER2-negative, ESR1-mutated breast cancer.

Estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative, ESR1-mutated breast cancer is a distinct molecular subtype of mammary carcinoma affecting breast glandular tissue, most frequently identified in patients with locally advanced or metastatic disease.

Tumors express functional estrogen receptors without HER2 protein overexpression or gene amplification, but they harbor somatic activating mutations within the ligand-binding domain of the ESR1 gene.

These mutations typically arise as an acquired resistance mechanism under the selective pressure of prior anti-estrogen therapies, particularly aromatase inhibitors, causing constitutive, ligand-independent estrogen receptor signaling and transcription that drives continued tumor proliferation.

Clinically, this biomarker profile defines a state of endocrine therapy resistance, necessitating targeted interventions that effectively degrade or inhibit the mutated receptor complex.

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