As used herein, the term “anti-androgen” refers to a group of hormone receptor antagonist compounds that are capable of preventing or inhibiting the biologic effects of androgens, male sex hormones, on normally responsive tissues in the body. Antiandrogens usually work by blocking the appropriate receptors, competing for binding sites on intracellular receptors, and obstructing androgen signaling pathways. As well as the compounds of Formula I and II, anti-androgens include, but are not limited to, coumarins, bicalutamide, flutamide, hydroxyflutamide, nilutamide, spionolactone, cyproterone acetate, ketoconazole, finasteride, dutasteride, harman, norharman, harmine, harmaline, tetrahydroharmine, harmol, harmalol, ethyl harmol, n-butyl harmol and other beta-carboline derivatives.
Antiandrogens are often indicated to treat severe male sexual disorders, such as hypersexuality (excessive sexual desire) and sexual deviation, specifically paraphilias, as well as use as an antineoplastic agent and palliative, adjuvant or neoadjuvant hormonal therapy in prostate cancer. Antiandrogens can also be used for treatment of benign prostatic hyperplasia (prostate enlargement), acne vulgaris, androgenetic alopecia (male pattern baldness), and hirsutism (excessive hair growth). Anti-androgens are also occasionally used as a male contraceptive agent, to purposefully prevent or counteract masculinisation in the case of transgender women undergoing gender reassignment therapy, and to prevent the symptoms associated with reduced testosterone, such as hot flashes, following castration. Other conditions treatable with an anti-androgen are prostate cancer, including primary and hormone refractory prostate cancer, ovarian cancer, hepatocellular carcinoma, acne vulgaris, endometriosis, acanthosis nigricans, hypertrichosis, breast cancer, precocious puberty, polycystic ovary syndrome, benign prostatic hyperplasia, alopecia (such as androgen-dependent alopecia), hirsutism and hypersexuality/paraphilia.
