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Nebenwirkungen Tamoxifen Mechanism

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Häufig Gestellte Fragen

1What Is The Mechanism Of Action Of Tamoxifen?

Tamoxifen (TAM) is known to have a dual mechanism of action: (1) to compete with 17β-estradiol (E2) at the receptor site and to block the promotional role of E2 in breast cancer; and (2) to bind DNA after metabolic activation and to initiate carcinogenesis.

2What Is The Mechanism Of Action Of Tamoxifen And Aromatase Inhibitors?

Next to radiation therapy, endocrine hormonal treatments, primarily tamoxifen (TAM) and aromatase inhibitors (AIs), are the most common adjuvant treatment for women with hormone receptor-positive breast cancer [3–7]. TAM acts by blocking estrogen binding to its receptor, while AIs block estrogen production [8].

3Why Is Tamoxifen A Serm?

Selective estrogen receptor modulators (SERMs) are synthetic molecules which bind to estrogen receptors (ER) and can modulate its transcriptional capabilities in different ways in diverse estrogen target tissues. Tamoxifen, the prototypical SERM, is extensively used for targeted therapy of ER positive breast cancers.

4Is Tamoxifen A Serm Or Ai?

These medications include selective estrogen receptor modulators (SERMs), of which there are two: tamoxifen and raloxifene.

5What Is The Difference Between Tamoxifen And Aromatase Inhibitors?

For women with early-stage oestrogen receptor (ER)-positive breast cancer, adjuvant tamoxifen reduces 15-year breast cancer mortality by a third. Aromatase inhibitors are more effective than tamoxifen in postmenopausal women but are ineffective in premenopausal women when used without ovarian suppression.

6How Does The Aromatase Inhibitor Work?

What are aromatase inhibitors? Aromatase inhibitors (AIs) lower estrogen levels by stopping an enzyme in fat tissue (called aromatase) from changing other hormones into estrogen. (Estrogen can fuel the growth of breast cancer cells.) These drugs don’t stop the ovaries from making estrogen.

7Is Tamoxifen An Estrogen Agonist Or Antagonist?

Tamoxifen is both an antagonist and an agonist of the estrogen receptor. However, a molecular explanation exists for this apparent paradox. The dual action is a function of the estrogen receptor complex present in a particular cell or tissue.