<unk> s are used in the treatment of an assortment of androgen-dependent conditions in both males and females. They are used to treat men with prostate cancer, benign prostatic hyperplasia, pattern hair loss, hypersexuality, paraphilias, and priapism, as well as boys with precocious puberty. In women and girls,<unk> s are used to treat acne, seborrhea, hidradenitis suppurativa, hirsutism, and hyperandrogenism.<unk> s are also used in transgender women as a component of feminizing hormone therapy and as puberty blockers in transgender girls. Men and boys Prostate cancer Androgens like testosterone and particularly DHT are importantly involved in the development and progression of prostate cancer. They act as growth factors in the prostate gland, stimulating cell division and tissue growth. In accordance, therapeutic modalities that reduce androgen signaling in the prostate gland, referred to collectively as androgen deprivation therapy, are able to significantly slow the course of prostate cancer and extend life in men with the disease. Although<unk> s are effective in slowing the progression of prostate cancer, they are not generally curative, and with time, the disease adapts and androgen deprivation therapy eventually becomes ineffective. When this occurs, other treatment approaches, such as chemotherapy, may be considered. The most common methods of androgen deprivation therapy currently employed to treat prostate cancer are castration (with a GnRH modulator or orchiectomy), nonsteroidal<unk> s, and the androgen synthesis inhibitor abiraterone acetate. Castration may be used alone or in combination with one of the other two treatments. When castration is combined with a nonsteroidal<unk>  like bicalutamide, this strategy is referred to as combined androgen blockade (also known as complete or maximal androgen blockade). Enzalutamide, apalutamide, and abiraterone acetate are specifically approved for use in combination with castration to treat castration-resistant prostate cancer. Monotherapy with the nonsteroidal<unk>  bicalutamide is also used in the treatment of prostate cancer as an alternative to castration with comparable effectiveness but with a different and potentially advantageous side effect profile. High-dose estrogen was the first functional<unk>  used to treat prostate cancer. It was widely used, but has largely been abandoned for this indication in favor of newer agents with improved safety profiles and fewer feminizing side effects. Cyproterone acetate was developed subsequently to high-dose estrogen and is the only steroidal<unk>  that has been widely used in the treatment of prostate cancer, but it has largely been replaced by nonsteroidal<unk> s, which are newer and have greater effectiveness, tolerability, and safety. Bicalutamide, as well as enzalutamide, have largely replaced the earlier nonsteroidal<unk> s flutamide and nilutamide, which are now little used. The earlier androgen synthesis inhibitors aminoglutethimide and ketoconazole have only limitedly been used in the treatment of prostate cancer due to toxicity concerns and have been replaced by abiraterone acetate. In addition to active treatment of prostate cancer,<unk> s are effective as prophylaxis (preventatives) in reducing the risk of ever developing prostate cancer.<unk> s have only limitedly been assessed for this purpose, but the 5α-reductase inhibitors finasteride and dutasteride and the steroidal AR antagonist spironolactone have been associated with significantly reduced risk of prostate cancer. In addition, it is notable that prostate cancer is extremely rare in transgender women who have been on feminizing hormone therapy for an extended period of time. Enlarged prostate The 5α-reductase inhibitors finasteride and dutasteride are used to treat benign prostatic hyperplasia, a condition in which the prostate becomes enlarged and this results in urinary obstruction and discomfort. They are effective because androgens act as growth factors in the prostate gland. The<unk> s chlormadinone acetate and oxendolone and the functional<unk> s allylestrenol and gestonorone caproate are also approved in some countries for the treatment of benign prostatic hyperplasia. Scalp hair loss 5α-Reductase inhibitors like finasteride, dutasteride, and alfatradiol and the topical nonsteroidal AR antagonist topilutamide (fluridil) are approved for the treatment of pattern hair loss, also known as scalp hair loss or baldness. This condition is generally caused by androgens, so<unk> s can slow or halt its progression. Systemic<unk> s besides 5α-reductase inhibitors are not generally used to treat scalp hair loss in males due to risks like feminization (e.g., gynecomastia) and sexual dysfunction. However, they have been assessed and reported to be effective for this indication. Acne<unk> s are generally not used to treat acne in males due to their high risk of feminization (e.g., gynecomastia) and sexual dysfunction. However, they have been studied for acne in males and found to be effective. Clascoterone, a topical<unk> , is effective for acne in males and may become approved for this indication in the future. Sexual deviance Androgens increase sex drive, and for this reason,<unk> s are able to reduce sex drive in men. In accordance,<unk> s are used in the treatment of conditions of sexual deviance such as hypersexuality (excessively high sex drive) and paraphilias (atypical and sometimes societally unacceptable sexual interests) like pedophilia (sexual attraction to children). They have been used to decrease sex drive in sex offenders so as to reduce the likelihood of recidivism (repeat offenses).<unk> s used for these indications include cyproterone acetate, medroxyprogesterone acetate, and GnRH modulators. Early puberty<unk> s are used to treat precocious puberty in boys. They work by opposing the effects of androgens and delaying the development of secondary sexual characteristics and onset of changes in sex drive and function until a more appropriate age.<unk> s that have been used for this purpose include cyproterone acetate, medroxyprogesterone acetate, GnRH modulators, spironolactone, bicalutamide, and ketoconazole. Spironolactone and bicalutamide require combination with an aromatase inhibitor to prevent the effects of unopposed estrogens, while the others can be used alone. Long-lasting erections<unk> s are effective in the treatment of recurrent priapism (potentially painful penile erections that last more than four hours). Women and girls Skin and hair conditions<unk> s are used in the treatment of androgen-dependent skin and hair conditions including acne, seborrhea, hidradenitis suppurativa, hirsutism, and pattern hair loss in women. All of these conditions are dependent on androgens, and for this reason,<unk> s are effective in treating them. The most commonly used<unk> s for these indications are cyproterone acetate and spironolactone. Flutamide has also been studied extensively for such uses, but has fallen out of favor due to its association with hepatotoxicity. Bicalutamide, which has a relatively minimal risk of hepatotoxicity, has been evaluated for the treatment of hirsutism and found effective similarly to flutamide and may be used instead of it. In addition to AR antagonists, oral contraceptives containing ethinylestradiol are effective in treating these conditions, and may be combined with AR antagonists. High androgen levels Hyperandrogenism is a condition in women in which androgen levels are excessively and abnormally high. It is commonly seen in women with PCOS, and also occurs in women with intersex conditions like congenital adrenal hyperplasia. Hyperandrogenism is associated with virilization – that is, the development of masculine secondary sexual characteristics like male-pattern facial and body hair growth (or hirsutism), voice deepening, increased muscle mass and strength, and broadening of the shoulders, among others. Androgen-dependent skin and hair conditions like acne and pattern hair loss may also occur in hyperandrogenism, and menstrual disturbances, like amenorrhea, are commonly seen. Although<unk> s do not treat the underlying cause of hyperandrogenism (e.g., PCOS), they are able to prevent and reverse its manifestation and effects. As with androgen-dependent skin and hair conditions, the most commonly used<unk> s in the treatment of hyperandrogenism in women are cyproterone acetate and spironolactone. Other<unk> s, like bicalutamide, may be used alternatively. Transgender hormone therapy<unk> s are used to prevent or reverse masculinization and to facilitate feminization in transgender women who are undergoing hormone therapy and who have not undergone sex reassignment surgery or orchiectomy. Besides estrogens, the main<unk> s that have been used for this purpose are cyproterone acetate, spironolactone, and GnRH modulators. Nonsteroidal<unk> s like bicalutamide are also used for this indication. In addition to use in transgender women,<unk> s, mainly GnRH modulators, are used as puberty blockers to prevent puberty in transgender girls until they are older and ready to begin hormone therapy. Available forms There are several different types of<unk> s, including the following: * Androgen receptor antagonists: Drugs that bind directly to and block the AR. These drugs include the steroidal<unk> s cyproterone acetate, megestrol acetate, chlormadinone acetate, spironolactone, oxendolone, and osaterone acetate (veterinary) and the nonsteroidal<unk> s flutamide, bicalutamide, nilutamide, topilutamide, enzalutamide, and apalutamide. Aside from cyproterone acetate and chlormadinone acetate, a few other progestins used in oral contraceptives and/or in menopausal HRT including dienogest, drospirenone, medrogestone, nomegestrol acetate, promegestone, and trimegestone also have varying degrees of AR antagonistic activity. * Androgen synthesis inhibitors: Drugs that directly inhibit the enzymatic biosynthesis of androgens like testosterone and/or DHT. Examples include the CYP17A1 inhibitors ketoconazole, abiraterone acetate, and seviteronel, the CYP11A1 (P450scc) inhibitor aminoglutethimide, and the 5α-reductase inhibitors finasteride, dutasteride, epristeride, alfatradiol, and saw palmetto extract (Serenoa repens). A number of other<unk> s, including cyproterone acetate, spironolactone, medrogestone, flutamide, nilutamide, and bifluranol, are also known to weakly inhibit androgen synthesis. * Antigonadotropins: Drugs that suppress the gonadotropin-releasing hormone (GnRH)-induced release of gonadotropins and consequent activation
Antiandrogen
Antiestrogen
Antiglucocorticoid
Thyroid blocker
Aromatase inhibitor
Nonsteroidal antiandrogen
Antiprogestogen
Phytoestrogen