Tamoxifen to endoxifen
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Tamoxifen is a medication that is primarily used to prevent breast cancer in women and treat breast cancer in women and men. It is also being studied for other types of cancer. It has been in the list of essential medicines of the World Health Organization, the most effective and safe medicines needed in a health system.
Endoxifen is one of the primary active metabolites of tamoxifen that has anti-estrogen effects and is typically formed in the liver by the enzyme CYP2D6.
Tamoxifen is administered orally, and as it passes through the liver, it is metabolized into several metabolites, including endoxifen. The process is as follows:
- Tamoxifen is ingested orally.
- It is absorbed in the gut and then reaches the liver.
- In the liver, the enzyme CYP2D6 metabolizes tamoxifen into endoxifen.
The effectiveness of tamoxifen can be influenced by the activity of the CYP2D6 enzyme in the liver. Some people have variations in the gene that produces this enzyme which can affect how well their bodies convert tamoxifen to endoxifen. Therefore, genetic testing may be done to determine how well a person might respond to tamoxifen therapy.
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