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An antiestrogen is a substance that blocks the production or utilization of estrogens, or inhibits their effects.

Antiestrogens like tamoxifen can promote an invasive phenotype in estrogen receptor (ER)-positive breast cancer cells with deficient intercellular adhesion.

Although aromatase inhibitors could be considered antiestrogens by some definitions, they are often considered to be a distinct class. Aromatase inhibitors reduce the production of estrogen, while the term "antiestrogen" is usually reserved for agents reducing the response to estrogen.