An antiandrogen competes for androgen receptor binding and acts as an androgen receptor antagonist, i.e. blocking or interfering with the actions of androgen hormones. Androgens regulate differentiation and development of male genitalia; initiate and maintain spermatogenesis; stimulate sexual hair development; regulate sexual behavior; and stimulate of bone growth.

Exposure to a synthetic antiandrogen, such as flutamide, during sexual differentiation and puberty can alter sexual development. Antiandrogenic alterations include the demasculinization and feminization of male offspring, and the masculinization and defeminization of female offspring. Male rats exposed to an anti-androgen during sexual differentiation in utero display reproductive malformations such as shortened anogenital distance, retained nipples, and cleft phallus with hypospadias.

Some pesticides and fungicides are known antiandrogens. In utero exposure to these compounds during sexual differentiation in rats induces some of the reproductive malformations noted above.

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