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17β-estradiol + aromatase inhibitor

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination therapy consisting of 17β-estradiol (E2), a natural estrogen hormone, and an aromatase inhibitor (AI), which is a class of drugs that block the enzyme aromatase responsible for converting androgens to estrogens. The combination has been studied primarily in the context of hormone receptor-positive breast cancer, particularly in cases resistant to standard AI monotherapy. While AIs alone reduce estrogen production and are standard for postmenopausal women with ER-positive breast cancer, adding estradiol may have unique effects on tumor biology—such as promoting degradation of estrogen receptor alpha (ERα) protein and sensitizing certain resistant cancer cells to treatment. This approach remains investigational; it is not an approved or widely used clinical regimen but has shown potential in preclinical models and early research settings[2][4].

Other names
estradiol + aromatase inhibitorE2 + AI
02

Targets

CYP19A1 (Aromatase)ESR1 (ERα)

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