Endoxifen

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Endoxifen

Endoxifen (pronounced en-dox-i-fen) is a pharmacologically active metabolite of the drug tamoxifen, which is widely used in the treatment of estrogen receptor-positive breast cancer.

Etymology

The term "Endoxifen" is derived from the parent drug "Tamoxifen". The prefix "endo-" is derived from the Greek word "endon" meaning "within", referring to the fact that Endoxifen is produced within the body as a metabolite of Tamoxifen.

Pharmacology

Endoxifen is primarily produced in the liver by the enzyme CYP2D6, which converts Tamoxifen into Endoxifen. It is a potent selective estrogen receptor modulator (SERM), meaning it can either block or activate estrogen receptors, depending on the tissue type. This makes it effective in preventing the growth of estrogen receptor-positive breast cancer cells.

Clinical Use

Endoxifen is not typically administered directly, but is produced in the body from Tamoxifen. The effectiveness of Tamoxifen therapy can be influenced by the individual's CYP2D6 enzyme activity level, as this affects the amount of Endoxifen produced. Some studies suggest that measuring Endoxifen levels in the blood could be useful in personalizing Tamoxifen therapy.

Related Terms

  • Tamoxifen: The parent drug of Endoxifen, used in the treatment of estrogen receptor-positive breast cancer.
  • Estrogen receptor: A protein within cells that binds to the hormone estrogen, influencing cell growth and development.
  • Selective estrogen receptor modulator (SERM): A type of drug that can either block or activate estrogen receptors, depending on the tissue type.
  • CYP2D6: An enzyme in the liver that metabolizes many drugs, including Tamoxifen into Endoxifen.
  • Metabolite: A substance produced by metabolism.

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