Male sex hormones are also known as androgens; antiandrogens may also be called androgen receptor blockers. Some antiandrogens work by lowering the body's production of androgens while others block androgen receptors, limiting the body's ability to …

2022年7月21日 · Enzalutamide (also named MDV3100) is the first FDA-approved second-generation AR antagonist for the treatment of CRPC and exhibits a much higher AR-binding affinity in comparison to the...

They belong to a class of medications called “androgen receptor inhibitors” that work by blocking the effects of androgen (a male reproductive hormone) to stop the growth and spread of cancer cells.

Androgen deprivation therapy (ADT) still remains the first-line PCa therapy. Insufficiency of ADT over time leads to castration-resistant PCa (CRPC) in which the AR axis is still active, despite castrate levels of circulating androgens.

Androgen receptor antagonists include bicalutamide, flutamide, and enzalutamide, while abiraterone is an irreversible CYP17A1 enzyme blocker (the enzyme that regulates the conversion of 17-hydroxyprogenolone to dehydroepiandrosterone). LHRH agonists such as triptorelin and goserelin, reduce serum androgen levels.

Enzalutamide, apalutamide, and darolutamide are second-generation antiandrogens that were developed after the first-generation antiandrogens flutamide, nilutamide, and bicalutamide.

Androgen receptor antagonists. Normal phenotypic sexual differentiation of the male fetus, as well as all of the postnatal events which result in the delivery of fertile spermatozoa to the female reproductive tract, is dependent on appropriately timed androgenic stimulation of the male.

A substance that keeps androgens (male sex hormones) from binding to proteins called androgen receptors, which are found in normal prostate cells, some prostate cancer cells, and in cells of some other tissues. Preventing this binding blocks the effects of these hormones in the body.

Some doctors advise androgen deprivation (orchiectomy or an LHRH agonist or antagonist) plus an anti-androgen for initial hormone therapy for advanced prostate cancer. Studies have suggested this may be more helpful than androgen deprivation alone.

There has been significant interest in developing AR antagonists that do not target the LBD so that the activity of AR-SVs which are constitutively active and lack the LBD can be inhibited.