Antiandrogene

Antiandrogene, or antiandrogens, are substances that reduce the effects of androgens by blocking androgen receptor signaling or by lowering androgen production. They are used to treat conditions driven by androgens and play a role in research on male sex hormone action.

They are typically categorized into two groups: androgen receptor antagonists, which bind the androgen receptor and prevent activation by testosterone or dihydrotestosterone, and androgen synthesis inhibitors, which reduce production of these hormones by interfering with steroidogenesis. Some agents have multiple actions or additional hormonal effects.

Common examples include non-steroidal receptor antagonists such as flutamide, bicalutamide, nilutamide, enzalutamide, and apalutamide, and the synthesis inhibitor abiraterone acetate. These drugs are central to androgen deprivation therapy for prostate cancer; they are also used to treat hirsutism or severe androgenic acne in women and, as part of transgender regimens, to suppress endogenous testosterone.

Adverse effects vary by drug but commonly include hot flashes, fatigue, decreased libido, and breast tenderness; hepatotoxicity is associated with some agents. Abiraterone can cause hypertension and mineralocorticoid excess and often requires concurrent steroids. Drug interactions via hepatic enzymes necessitate monitoring.

Safety, efficacy, and selecting among antiandrogens depend on the underlying condition and patient factors. Ongoing research explores new receptor antagonists and synthesis inhibitors with improved tolerability and activity.