Arimidex (anastrozole) is the aromatase inhibitor of choice. Arimidex’s mechanism of action - blocking conversion of aromatizable steroids to estrogen - is in contrast to the mechanism of action of anti-estrogens such as clomiphene (Clomid) or tamoxifen (Nolvadex), which block estrogen receptors in some tissues, and activate estrogen receptors in others.
Anastrozole, sold under the trade name Arimidex among others, is a medication used in addition to other treatments for breast cancer. Specifically it is used for hormone receptor-positive breast cancer. It has also been used to prevent breast cancer in those at high risk. It is taken by mouth.
Anastrozole, sold under the trade name Arimidex among others, is a medication used in addition to other treatments for breast cancer. Specifically it is used for hormone receptor-positive breast cancer. It has also been used to prevent breast cancer in those at high risk. It is taken by mouth.
How does Anastrozole work?
Anastrozole reversibly binds to the aromatase enzyme, and through competitive inhibition blocks the conversion of androgens to estrogens in peripheral (extra-gonadal) tissues.
Anastrozole is an inhibitor for the triazole aromatase with a strong selectivity. It can inhibits aromatase which is prerequisite for the synthesis of pigment cells P-450 thereby blocking the biosynthesis of estrogens, and the estrogen is the essential part of the growth of breast cancer cells. The 50% inhibitory concentration (IC50) value of anastrozole to placental aromatase is 15nmol/L.
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