NAPLEX (North American Pharmacist Licensure Examination) Practice Exam

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What is the action mechanism of first-generation antiandrogens like Bicalutamide?

  1. Increase androgen receptor upregulation

  2. Directly inhibit GnRH receptors

  3. Inhibit testosterone from binding to prostate cancer cells

  4. Decrease testosterone synthesis

The correct answer is: Inhibit testosterone from binding to prostate cancer cells

First-generation antiandrogens, such as Bicalutamide, work by inhibiting testosterone from binding to prostate cancer cells. This mechanism of action is crucial in the treatment of prostate cancer, as prostate cancer cells are stimulated by androgens like testosterone. By blocking the binding of testosterone to these cells, first-generation antiandrogens help to slow down the growth and spread of prostate cancer. The other options are not correct because first-generation antiandrogens do not work by increasing androgen receptor upregulation, directly inhibiting GnRH receptors, or decreasing testosterone synthesis.

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