A steroidal antiandrogen (SAA) is an

antiandrogen Antiandrogens, also known as androgen antagonists or testosterone blockers, are a class of drugs that prevent androgens like testosterone and dihydrotestosterone (DHT) from mediating their biological effects in the body. They act by blocking the ...

with a

steroid A steroid is a biologically active organic compound with four rings arranged in a specific molecular configuration. Steroids have two principal biological functions: as important components of cell membranes that alter membrane fluidity; and a ...

chemical structure A chemical structure determination includes a chemist's specifying the molecular geometry and, when feasible and necessary, the electronic structure of the target molecule or other solid. Molecular geometry refers to the spatial arrangement of at ...

. They are typically

antagonist An antagonist is a character in a story who is presented as the chief foe of the protagonist. Etymology The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ...

s of the

androgen receptor The androgen receptor (AR), also known as NR3C4 (nuclear receptor subfamily 3, group C, member 4), is a type of nuclear receptor that is activated by binding any of the androgenic hormones, including testosterone and dihydrotestosterone in th ...

(AR) and act both by blocking the effects of

androgen An androgen (from Greek ''andr-'', the stem of the word meaning "man") is any natural or synthetic steroid hormone that regulates the development and maintenance of male characteristics in vertebrates by binding to androgen receptors. This inc ...

s like

testosterone Testosterone is the primary sex hormone and anabolic steroid in males. In humans, testosterone plays a key role in the development of Male reproductive system, male reproductive tissues such as testes and prostate, as well as promoting secondar ...

and

dihydrotestosterone Dihydrotestosterone (DHT, 5α-dihydrotestosterone, 5α-DHT, androstanolone or stanolone) is an endogenous androgen sex steroid and hormone. The enzyme 5α-reductase catalyzes the formation of DHT from testosterone in certain tissues includi ...

(DHT) and by suppressing

gonad A gonad, sex gland, or reproductive gland is a mixed gland that produces the gametes and sex hormones of an organism. Female reproductive cells are egg cells, and male reproductive cells are sperm. The male gonad, the testicle, produces sper ...

al androgen production. SAAs lower concentrations of testosterone through simulation of the negative feedback inhibition of the

hypothalamus The hypothalamus () is a part of the brain that contains a number of small nuclei with a variety of functions. One of the most important functions is to link the nervous system to the endocrine system via the pituitary gland. The hypothalamu ...

. SAAs are used in the treatment of

androgen-dependent condition An androgen-dependent condition, disease, disorder, or syndrome, is a medical condition that is, in part or full, dependent on, or is sensitive to, the presence of androgenic activity in the body. Known androgen-dependent conditions include acne, s ...

s in men and women, and are also used in

veterinary medicine Veterinary medicine is the branch of medicine that deals with the prevention, management, diagnosis, and treatment of disease, disorder, and injury in animals. Along with this, it deals with animal rearing, husbandry, breeding, research on nutri ...

for the same purpose. They are the converse of

nonsteroidal antiandrogen A nonsteroidal antiandrogen (NSAA) is an antiandrogen with a nonsteroidal chemical structure. They are typically selective and full or silent antagonists of the androgen receptor (AR) and act by directly blocking the effects of androgens like t ...

s (NSAAs), which are antiandrogens that are not

s and are structurally unrelated to testosterone.

Medical uses

SAAs are used in clinical medicine for the following indications: *

Prostate cancer Prostate cancer is cancer of the prostate. Prostate cancer is the second most common cancerous tumor worldwide and is the fifth leading cause of cancer-related mortality among men. The prostate is a gland in the male reproductive system that sur ...

in men *

Benign prostatic hyperplasia Benign prostatic hyperplasia (BPH), also called prostate enlargement, is a noncancerous increase in size of the prostate gland. Symptoms may include frequent urination, trouble starting to urinate, weak stream, inability to urinate, or loss o ...

in men * Androgen-dependent skin and hair conditions like

acne Acne, also known as ''acne vulgaris'', is a long-term Cutaneous condition, skin condition that occurs when Keratinocyte, dead skin cells and Sebum, oil from the skin clog hair follicles. Typical features of the condition include comedo, black ...

hirsutism Hirsutism is excessive body hair on parts of the body where hair is normally absent or minimal. The word is from early 17th century: from Latin ''hirsutus'' meaning "hairy". It usually refers to a "male" pattern of hair growth in a female that ...

seborrhea A sebaceous gland is a microscopic exocrine gland in the skin that opens into a hair follicle to secrete an oily or waxy matter, called sebum, which lubricates the hair and skin of mammals. In humans, sebaceous glands occur in the greatest numbe ...

, and

pattern hair loss Pattern hair loss (also known as androgenetic alopecia (AGA)) is a hair loss condition that primarily affects the top and front of the scalp. In male-pattern hair loss (MPHL), the hair loss typically presents itself as either a receding front ha ...

(androgenic alopecia) in women *

Hyperandrogenism Hyperandrogenism is a medical condition characterized by high levels of androgens. It is more common in women than men. Symptoms of hyperandrogenism may include acne, seborrhea (inflamed skin), hair loss on the scalp, increased body or facial ...

, such as due to

polycystic ovary syndrome Polycystic ovary syndrome, or PCOS, is the most common endocrine disorder in women of reproductive age. The syndrome is named after the characteristic cysts which may form on the ovaries, though it is important to note that this is a sign and no ...

congenital adrenal hyperplasia Congenital adrenal hyperplasia (CAH) is a group of autosomal recessive disorders characterized by impaired cortisol synthesis. It results from the deficiency of one of the five enzymes required for the synthesis of cortisol in the adrenal cortex. ...

, in women * As a component of

hormone therapy Hormone therapy or hormonal therapy is the use of hormones in medical treatment. Treatment with hormone antagonists may also be referred to as hormonal therapy or antihormone therapy. The most general classes of hormone therapy are oncologic horm ...

for

transgender women A trans woman or a transgender woman is a woman who was assigned male at birth. Trans women have a female gender identity, may experience gender dysphoria, and may transition; this process commonly includes hormone replacement therapy and som ...

Precocious puberty In medicine, precocious puberty is puberty occurring at an unusually early age. In most cases, the process is normal in every aspect except the unusually early age and simply represents a variation of normal development. In a minority of childr ...

in boys *

Hypersexuality Hypersexuality is extremely frequent or suddenly increased libido. It is controversial whether it should be included as a clinical diagnosis used by mental healthcare professionals. Nymphomania and satyriasis were terms previously used for the c ...

and

paraphilia Paraphilia (previously known as sexual perversion and sexual deviation) is the experience of intense sexual arousal to atypical objects, situations, fantasies, behaviors, or individuals. It has also been defined as sexual interest in anything ot ...

s in men and

sex offender A sex offender (sexual offender, sex abuser, or sexual abuser) is a person who has committed a sex crime. What constitutes a sex crime differs by culture and legal jurisdiction. The majority of convicted sex offenders have convictions for crime ...

s *

Priapism Priapism is a condition in which a penis remains erect for hours in the absence of stimulation or after stimulation has ended. There are three types: ischemic (low-flow), nonischemic (high-flow), and recurrent ischemic (intermittent). Most cases ...

in men

Available forms

Pharmacology

Unlike NSAAs, most SAAs show off-target hormonal activity such as

progestogen Progestogens, also sometimes written progestagens or gestagens, are a class of natural or synthetic steroid hormones that bind to and activate the progesterone receptors (PR). Progesterone is the major and most important progestogen in the body. ...

ic,

glucocorticoid Glucocorticoids (or, less commonly, glucocorticosteroids) are a class of corticosteroids, which are a class of steroid hormones. Glucocorticoids are corticosteroids that bind to the glucocorticoid receptor that is present in almost every vertebr ...

, or

antimineralocorticoid An antimineralocorticoid, also known as a mineralocorticoid receptor antagonist (MRA or MCRA) or aldosterone antagonist, is a diuretic drug which antagonizes the action of aldosterone at mineralocorticoid receptors. This group of drugs is often u ...

activity, possess

antigonadotropic An antigonadotropin is a drug which suppresses the activity and/or downstream effects of one or both of the gonadotropins, follicle-stimulating hormone (FSH) and luteinizing hormone (LH). This results in an inhibition of the hypothalamic-pituita ...

effects, and are weak

partial agonist In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonistic e ...

s of the AR with some capacity to activate the receptor. Due to their antigonadotropic effects, SAAs lower androgen levels in addition to directly blocking the actions of androgens at the AR; at sufficiently high dosages, they are able to lower circulating testosterone levels by up to 70 to 80% in men, to just above the castrate range. However, due to their other hormonal effects, suppression of estrogen levels alongside testosterone levels, and AR activation, SAAs have increased

side effect In medicine, a side effect is an effect, whether therapeutic or adverse, that is secondary to the one intended; although the term is predominantly employed to describe adverse effects, it can also apply to beneficial, but unintended, consequence ...

s and show lower

efficacy Efficacy is the ability to perform a task to a satisfactory or expected degree. The word comes from the same roots as ''effectiveness'', and it has often been used synonymously, although in pharmacology a pragmatic clinical trial#Efficacy versu ...

in the treatment of prostate cancer relative to NSAAs.

List of SAAs

Marketed

Used specifically as antiandrogens (major)

Cyproterone acetate Cyproterone acetate (CPA), sold alone under the brand name Androcur or Ethinylestradiol/cyproterone acetate, with ethinylestradiol under the brand names Diane or Diane-35 among others, is an antiandrogen and progestin medication used in the treat ...

(Androcur): A combined AR antagonist and progestogen/antigonadotropin. Also has weak glucocorticoid activity. Previously used widely in the treatment of prostate cancer, but since largely replaced by NSAAs. Also used for androgen-dependent indications in women and transgender women, precocious puberty in boys, and as a means of chemical castration for

sexual deviation Paraphilia (previously known as sexual perversion and sexual deviation) is the experience of intense sexual arousal to atypical objects, situations, fantasies, behaviors, or individuals. It has also been defined as sexual interest in anything o ...

in men. Widely used in oral contraceptives as well (with ethinylestradiol under the brand names Diane and Diane-35). Not available in the United States. Uniquely among most SAAs, has a high risk of

liver The liver is a major Organ (anatomy), organ only found in vertebrates which performs many essential biological functions such as detoxification of the organism, and the Protein biosynthesis, synthesis of proteins and biochemicals necessary for ...

changes and

hepatotoxicity Hepatotoxicity (from ''hepatic toxicity'') implies chemical-driven liver damage. Drug-induced liver injury is a cause of acute and chronic liver disease caused specifically by medications and the most common reason for a drug to be withdrawn fro ...

. Also has a high incidence of

psychiatric Psychiatry is the medical specialty devoted to the diagnosis, prevention, and treatment of mental disorders. These include various maladaptations related to mood, behaviour, cognition, and perceptions. See glossary of psychiatry. Initial psychi ...

s such as depression,

anxiety Anxiety is an emotion which is characterized by an unpleasant state of inner turmoil and includes feelings of dread over anticipated events. Anxiety is different than fear in that the former is defined as the anticipation of a future threat wh ...

, and

fatigue Fatigue describes a state of tiredness that does not resolve with rest or sleep. In general usage, fatigue is synonymous with extreme tiredness or exhaustion that normally follows prolonged physical or mental activity. When it does not resolve ...

. *

Spironolactone Spironolactone, sold under the brand name Aldactone among others, is a medication that is primarily used to treat fluid build-up due to heart failure, liver scarring, or kidney disease. It is also used in the treatment of high blood pressure ...

(Aldactone): An

(

aldosterone Aldosterone is the main mineralocorticoid steroid hormone produced by the zona glomerulosa of the adrenal cortex in the adrenal gland. It is essential for sodium conservation in the kidney, salivary glands, sweat glands, and colon. It plays a c ...

antagonist) with additional/coincidental antiandrogen activity. Specifically acts as an AR antagonist, weak antigonadotropin, and weak steroidogenesis inhibitor. Used for androgen-dependent indications in women and transgender women, particularly in the United States where cyproterone acetate is unavailable. Studied in the treatment of benign prostatic hyperplasia but was found to be ineffective. Contraindicated in prostate cancer due to weak androgenic activity and stimulation of

tumor A neoplasm () is a type of abnormal and excessive growth of tissue. The process that occurs to form or produce a neoplasm is called neoplasia. The growth of a neoplasm is uncoordinated with that of the normal surrounding tissue, and persists ...

growth. Most commonly used as a

diuretic A diuretic () is any substance that promotes diuresis, the increased production of urine. This includes forced diuresis. A diuretic tablet is sometimes colloquially called a water tablet. There are several categories of diuretics. All diuretics in ...

and

antihypertensive Antihypertensives are a class of drugs that are used to treat hypertension (high blood pressure). Antihypertensive therapy seeks to prevent the complications of high blood pressure, such as stroke and myocardial infarction. Evidence suggests tha ...

for

cardiovascular disease Cardiovascular disease (CVD) is a class of diseases that involve the heart or blood vessels. CVD includes coronary artery diseases (CAD) such as angina and myocardial infarction (commonly known as a heart attack). Other CVDs include stroke, h ...

. Commonly associated with

gynecomastia Gynecomastia (also spelled gynaecomastia) is the abnormal non-cancerous enlargement of one or both breasts in males due to the growth of breast tissue as a result of a hormone imbalance between estrogens and androgens. Updated by Brent Wisse (1 ...

(breast development) and

menstrual disturbance A menstrual disorder is characterized as any abnormal condition with regards to a person's menstrual cycle. There are many different types of menstrual disorders that vary with signs and symptoms, including pain during menstruation, heavy bleeding, ...

Used specifically as antiandrogens (minor)

Chlormadinone acetate Chlormadinone acetate (CMA), sold under the brand names Belara, Gynorelle, Lutéran, and Prostal among others, is a progestin and antiandrogen medication which is used in birth control pills to prevent pregnancy, as a component of menopausal hor ...

(Prostal): A combined AR antagonist and progestogen/antigonadotropin. Also has weak

activity. Widely used in the treatment of prostate cancer in

Japan Japan ( ja, 日本, or , and formally , ''Nihonkoku'') is an island country in East Asia. It is situated in the northwest Pacific Ocean, and is bordered on the west by the Sea of Japan, while extending from the Sea of Okhotsk in the north ...

, but little used for this purpose elsewhere. Has largely been replaced by NSAAs. Mostly used throughout the world in oral contraceptives (with

ethinylestradiol Ethinylestradiol (EE) is an estrogen medication which is used widely in birth control pills in combination with progestins. In the past, EE was widely used for various indications such as the treatment of menopausal symptoms, gynecological disord ...

under the brand names Belara and Belarina). Not available in the

United States The United States of America (U.S.A. or USA), commonly known as the United States (U.S. or US) or America, is a country primarily located in North America. It consists of 50 states, a federal district, five major unincorporated territorie ...

. *

Gestonorone caproate Gestonorone caproate, also known as gestronol hexanoate or norhydroxyprogesterone caproate and sold under the brand names Depostat and Primostat, is a progestin medication which is used in the treatment of enlarged prostate and cancer of the en ...

(Depostat, Primostat): A pure progestogen/antigonadotropin without any direct AR antagonism or other hormonal activity. Injected intramuscularly. Used in the treatment of benign prostatic hyperplasia in certain countries such as the

United Kingdom The United Kingdom of Great Britain and Northern Ireland, commonly known as the United Kingdom (UK) or Britain, is a country in Europe, off the north-western coast of the continental mainland. It comprises England, Scotland, Wales and North ...

. Not available in the United States. *

Hydroxyprogesterone caproate Hydroxyprogesterone caproate (OHPC), sold under the brand names Proluton and Makena among others, is a progestin medication which is used to prevent preterm birth in pregnant women with a history of the condition and to treat gynecological dis ...

(Proluton, Proluton Depot): A pure progestogen/antigonadotropin without any direct AR antagonism or other hormonal activity. Injected intramuscularly. Studied in the treatment of benign prostatic hyperplasia and showed some albeit only marginal effectiveness. Associated with hypogonadism and causes

impotence Erectile dysfunction (ED), also called impotence, is the type of sexual dysfunction in which the penis fails to become or stay erect during sexual activity. It is the most common sexual problem in men.Cunningham GR, Rosen RC. Overview of male ...

in two-thirds of men. Mostly used for

gynecological Gynaecology or gynecology (see spelling differences) is the area of medicine that involves the treatment of women's diseases, especially those of the reproductive organs. It is often paired with the field of obstetrics, forming the combined area ...

and

obstetric Obstetrics is the field of study concentrated on pregnancy, childbirth and the postpartum period. As a medical specialty, obstetrics is combined with gynecology under the discipline known as obstetrics and gynecology (OB/GYN), which is a surgic ...

indications in women. *

Medrogestone Medrogestone, sold under the brand name Colprone among others, is a progestin medication which has been used in menopausal hormone therapy and in the treatment of gynecological disorders. It is available both alone and in combination with an estr ...

(Colprone): A progestogen/antigonadotropin with additional activity as an AR antagonist and

steroidogenesis inhibitor A steroidogenesis inhibitor, also known as a steroid biosynthesis inhibitor, is a type of drug which inhibits one or more of the enzymes that are involved in the process of steroidogenesis, the biosynthesis of endogenous steroids and steroid horm ...

. Also has weak glucocorticoid activity. Formerly used in the treatment of benign prostatic hyperplasia in men. Most commonly used in the treatment of

gynecological disorder Gynaecology or gynecology (see spelling differences) is the area of medicine that involves the treatment of women's diseases, especially those of the reproductive organs. It is often paired with the field of obstetrics, forming the combined are ...

s and in

menopause Menopause, also known as the climacteric, is the time in women's lives when menstrual periods stop permanently, and they are no longer able to bear children. Menopause usually occurs between the age of 47 and 54. Medical professionals often d ...

. It is an older progestin that has mostly been discontinued and is now rarely used. *

Medroxyprogesterone acetate Medroxyprogesterone acetate (MPA), also known as depot medroxyprogesterone acetate (DMPA) in injectable form and sold under the brand name Depo-Provera among others, is a hormonal medication of the progestin type. It is used as a method of bi ...

(Depo-Provera): A progestogen/antigonadotropin without any direct AR antagonism. Also has weak androgenic and glucocorticoid activity and acts as a steroidogenesis inhibitor at very high dosages. Injected intramuscularly. Used as a means of chemical castration for sexual deviation in men, particularly in the United States where cyproterone acetate is unavailable. Studied in the treatment of prostate cancer but never widely used. Has also been used to prevent precocious puberty. Most commonly used as a long-lasting injectable contraceptive in women. *

Megestrol acetate Megestrol acetate (MGA), sold under the brand name Megace among others, is a progestin medication which is used mainly as an appetite stimulant to treat wasting syndromes such as cachexia.https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/ ...

(Megace): A combined AR partial antagonist and progestogen/antigonadotropin. Also has weak androgenic and glucocorticoid activity. Studied in the treatment of prostate cancer but showed poor effectiveness. Mostly used as an

appetite stimulant An orexigenic, or appetite stimulant, is a drug, hormone, or chemical compound, compound that increases appetite and may induce hyperphagia. This can be a medication or a naturally occurring neuropeptide hormone, such as ghrelin, orexin or neuropep ...

in patients with

cachexia Cachexia () is a complex syndrome associated with an underlying illness, causing ongoing muscle loss that is not entirely reversed with nutritional supplementation. A range of diseases can cause cachexia, most commonly cancer, congestive heart f ...

. *

Oxendolone Oxendolone, sold under the brand names Prostetin and Roxenone, is an antiandrogen and progestin medication which is used in Japan in the treatment of enlarged prostate. However, this use is controversial due to concerns about its clinical effica ...

(Prostetin, Roxenone): A combined AR antagonist and progestogen/antigonadotropin. Marketed in Japan only for the treatment of benign prostatic hyperplasia. Controversial due to low effectiveness observed in clinical studies.

Used as antiandrogens in veterinary medicine

Delmadinone acetate Delmadinone acetate (DMA), sold under the brand name Tardak among others, is a progestin and antiandrogen which is used in veterinary medicine to treat androgen-dependent conditions such as benign prostatic hyperplasia. It must be used with care ...

(Tardak): A combined AR antagonist and progestogen/antigonadotropin. Also has weak glucocorticoid activity. Used in

only. Marketed in

Europe Europe is a large peninsula conventionally considered a continent in its own right because of its great physical size and the weight of its history and traditions. Europe is also considered a Continent#Subcontinents, subcontinent of Eurasia ...

and

Oceania Oceania (, , ) is a region, geographical region that includes Australasia, Melanesia, Micronesia, and Polynesia. Spanning the Eastern Hemisphere, Eastern and Western Hemisphere, Western hemispheres, Oceania is estimated to have a land area of ...

for the treatment of

s such as

benign prostatic hyperplasia Benign prostatic hyperplasia (BPH), also called prostate enlargement, is a noncancerous increase in size of the prostate gland. Symptoms may include frequent urination, trouble starting to urinate, weak stream, inability to urinate, or loss o ...

in dogs. *

Osaterone acetate Osaterone (developmental code name TZP-5258), also known as 17α-hydroxy-6-chloro-2-oxa-6-dehydroprogesterone, as well as 2-oxachloromadinone, is a steroidal antiandrogen and progestin that was never marketed. The C17α acetate ester In chem ...

(Ypozane): A combined AR antagonist and progestogen/antigonadotropin. Used in veterinary medicine only. Marketed in Europe specifically for the treatment of benign prostatic hyperplasia in dogs. Has been associated with transiently

elevated liver enzymes In medicine, the presence of elevated transaminases, commonly the transaminases alanine transaminase (ALT) and aspartate transaminase (AST), may be an indicator of liver dysfunction. Other terms include transaminasemia, transaminitis, and elevated ...

Used exclusively as progestins in women

Dienogest Dienogest, sold under the brand name Visanne among others, is a progestin medication which is used in birth control pills and in the treatment of endometriosis. It is also used in menopausal hormone therapy and to treat heavy periods. Dienogest ...

(Visanne, Dinagest): Progestin with some AR antagonist activity. Used as an oral contraceptive (with

estradiol valerate Estradiol valerate (EV), sold for use by mouth under the brand name Progynova and Primiwal E4 and for use by injection under the brand names Delestrogen and Progynon Depot among others, is an estrogen medication. It is used in hormone therapy fo ...

as Natazia and Qlaira and with ethinylestradiol as Valette) and in the treatment of

endometriosis Endometriosis is a disease of the female reproductive system in which cells similar to those in the endometrium, the layer of tissue that normally covers the inside of the uterus, grow outside the uterus. Most often this is on the ovaries, f ...

. *

Drospirenone Drospirenone is a progestin and antiandrogen medication which is used in birth control pills to prevent pregnancy and in menopausal hormone therapy, among other uses. It is available both alone under the brand name Slynd and in combination with ...

: Progestin with antimineralocorticoid and AR antagonist activity. Used in combination with estrogen in hormonal replacement therapy and oral contraceptives (with ethinylestradiol as Yasmin, Yasminelle, and Yaz and with

estradiol Estradiol (E2), also spelled oestradiol, is an estrogen steroid hormone and the major female sex hormone. It is involved in the regulation of the estrous and menstrual female reproductive cycles. Estradiol is responsible for the development of f ...

as Angeliq). Also used (as an oral contraceptive) in the treatment of

. *

Nomegestrol acetate Nomegestrol acetate (NOMAC), sold under the brand names Lutenyl and Zoely among others, is a progestin medication which is used in birth control pills, menopausal hormone therapy, and for the treatment of gynecological disorders.http://www.ema. ...

(Lutenyl): Progestin with AR antagonist activity. Used in the treatment of gynecological disorders and in hormonal replacement therapy and oral contraceptives (with estradiol as Naemis and Zoely).

Miscellaneous

Mifepristone Mifepristone, also known as RU-486, is a medication typically used in combination with misoprostol to bring about a medical abortion during pregnancy and manage early miscarriage. This combination is 97% effective during the first 63 days of p ...

(RU-486; Mifegyne, Mifeprex): An

antiprogestogen Antiprogestogens, or antiprogestins, also known as progesterone antagonists or progesterone blockers, are a class of drugs which prevent progestogens like progesterone from mediating their biological effects in the body. They act by receptor antag ...

which is widely used as an

abortifacient An abortifacient ("that which will cause a miscarriage" from Latin: ''abortus'' "miscarriage" and '' faciens'' "making") is a substance that induces abortion. This is a nonspecific term which may refer to any number of substances or medications, ...

. Also has

antiglucocorticoid An antiglucocorticoid is a drug which reduces glucocorticoid activity in the body. They include direct glucocorticoid receptor antagonists such as mifepristone and synthesis inhibitors such as metyrapone, ketoconazole, and aminoglutethimide. ...

and AR antagonist activity. Has been found to produce gynecomastia as a side effect in men at a relatively high rate in clinical studies. Has been studied as a treatment for prostate cancer. Steroidal

androgen synthesis inhibitor An androgen synthesis inhibitor is a type of drug which inhibits the enzymatic synthesis of androgens, such as testosterone and dihydrotestosterone (DHT). They include: * CYP17A1 inhibitors (17α-hydroxylase/17,20-lyase inhibitors): inhibit the syn ...

s like the

CYP17A1 inhibitor A CYP17A1 inhibitor is a type of drug which enzyme inhibitor, inhibits the enzyme CYP17A1. It may inhibit both of the functions of the enzyme, 17α-hydroxylase and 17,20-lyase, or may be selective for inhibition of one of these two functions (gener ...

abiraterone acetate Abiraterone acetate, sold under the brand name Zytiga among others, is a medication used to treat prostate cancer. Specifically it is used together with a corticosteroid for metastatic castration-resistant prostate cancer (mCRPC) and metastatic ...

(Zytiga) or the

5α-reductase inhibitor 5α-Reductases, also known as 3-oxo-5α-steroid 4-dehydrogenases, are enzymes involved in steroid metabolism. They participate in three metabolic pathways: bile acid biosynthesis, androgen and estrogen metabolism. There are three isozymes of ...

finasteride Finasteride, sold under the brand names Proscar and Propecia among others, is a medication used to treat hair loss and benign prostatic hyperplasia (BPH) in men. It can also be used to treat excessive hair growth in women and as a part of horm ...

and

dutasteride Dutasteride, sold under the brand name Avodart among others, is a medication primarily used to treat the symptoms of a benign prostatic hyperplasia (BPH), an enlarged prostate not associated with cancer. A few months may be required before benefi ...

could also technically be described as "SAAs", but the term is usually reserved to describe AR antagonists (and sometimes progestogenic antigonadotropins).

Not marketed

Under development

Clascoterone Clascoterone, sold under the brand name Winlevi, is an antiandrogen medication which is used topically in the treatment of acne. It is also under development in a higher concentration for the treatment of androgen-dependent scalp hair loss, und ...

(CB-03-01; Breezula, Winlevi): A pure AR antagonist. Topical without any systemic activity. Under development for the treatment of acne and pattern hair loss (androgenic alopecia).

Development discontinued

11α-Hydroxyprogesterone 11α-Hydroxyprogesterone (11α-OHP), or 11α-hydroxypregn-4-ene-3,20-dione is an endogenous steroid and metabolite of progesterone. It is a weak antiandrogen, and is devoid of androgenic, estrogenic, and progestogenic activity. 11α-OHP was in ...

(11α-OHP): Possibly the first antiandrogen to be discovered. Weak antiandrogen used topically. Studied in the 1950s for the treatment of androgen-dependent skin conditions like acne and reportedly showed some effectiveness but was never marketed. * Benorterone (SKF-7690, FC-612): A pure AR antagonist without progestogenic activity, though with some antigonadotropic activity through an undefined mechanism. One of the earliest antiandrogens. Studied in the treatment of acne,

, and

in the 1960s but was found to produce a very high rate of

in males. Development was discontinued in favor of cyproterone acetate, which showed only a low rate of gynecomastia in males. * BOMT (Ro 7-2340): A pure AR antagonist without other progestogenic activity, though with some antigonadotropic activity through an undefined mechanism. One of the earliest antiandrogens. Studied in the treatment of benign prostatic hyperplasia but was never marketed. Was also of interest for the potential treatment of acne, pattern hair loss (androgenic alopecia), and prostate cancer, but was never studied for such uses. *

Cyproterone Cyproterone, also known by its developmental code name SH-80881, is a steroidal antiandrogen which was studied in the 1960s and 1970s but was never introduced for medical use. It is an analogue of cyproterone acetate (CPA), an antiandrogen, pr ...

(SH-80881, SH-881): A pure AR antagonist without progestogenic activity, showing robust progonadotropic activity like NSAAs. One of the earliest antiandrogens. Was studied in the treatment of

precocious puberty In medicine, precocious puberty is puberty occurring at an unusually early age. In most cases, the process is normal in every aspect except the unusually early age and simply represents a variation of normal development. In a minority of childr ...

as well as acne, seborrhea, and hirsutism. Showed surprisingly poor effectiveness in clinical trials and was abandoned in favor of cyproterone acetate. * Delanterone (GBR-21162): An AR antagonist which was described in the literature in 1977. Was under development for the treatment of acne but showed poor effectiveness in preclinical studies and was abandoned. *

Galeterone Galeterone (developmental code names TOK-001, VN/124-1) is a steroidal antiandrogen which was under development by Tokai Pharmaceuticals for the treatment of prostate cancer. It possesses a unique triple mechanism of action, acting as an androgen ...

(TOK-001, VN/124-1): A dual AR antagonist and steroidogenesis inhibitor which was under development for the treatment of prostate cancer but showed insufficient effectiveness in clinical trials and was discontinued. * Inocoterone acetate (RU-38882, RU-882): A steroid-like NSAA. It was under development as a topical medication for the treatment of acne but was discontinued due to insufficient effectiveness in clinical trials. * Metogest (SC-14207): An AR antagonist which was patented in 1975 and briefly investigated for the treatment of acne but was never marketed. * Rosterolone (SH-434): A pure AR antagonist without other hormonal activity. Developed as a topical antiandrogen without systemic activity. Showed some effectiveness in the treatment of acne, but was never marketed. * Topterone (WIN-17665): An AR antagonist which was described in the literature in 1977. Developed as a topical antiandrogen. Was under development for the treatment of acne but showed poor effectiveness and was abandoned. *

Trimethyltrienolone Trimethyltrienolone (TMT), also known by its developmental code name R-2956 or RU-2956, is an antiandrogen medication which was never introduced for medical use but has been used in scientific research. Side effects Due to its close relation to m ...

(R-2956): An extremely potent AR antagonist without other hormonal activity derived from the powerful

anabolic–androgenic steroid Anabolic steroids, also known more properly as anabolic–androgenic steroids (AAS), are steroidal androgens that include natural androgens like testosterone as well as synthetic androgens that are structurally related and have similar effects t ...

metribolone Metribolone (developmental code R1881, also known as methyltrienolone) is a synthetic compound, synthetic and oral administration, orally active anabolic–androgenic steroid (AAS) and a 17α-alkylated anabolic steroid, 17α-alkylated nandrolone ...

(methyltrienolone). Was under investigation for potential clinical use but development was discontinued in favor of NSAAs, which in contrast show a complete lack of intrinsic androgenic activity. * Zanoterone (WIN-49596): A pure AR antagonist without other hormonal activity except some

ic activity in

animal model An animal model (short for animal disease model) is a living, non-human, often genetic-engineered animal used during the research and investigation of human disease, for the purpose of better understanding the disease process without the risk of ha ...

s. Was under development for the treatment of benign prostatic hyperplasia but showed poor effectiveness and a high rate of

breast pain Breast pain is the symptom of discomfort in either one or both breasts. Pain in both breasts is often described as ''breast tenderness'', is usually associated with the menstrual period and is not serious. Pain that involves only one part of a br ...

and gynecomastia in clinical trials and was subsequently abandoned. * Many

spirolactone Spirolactones are a class of functional group in organic chemistry featuring a cyclic ester attached spiro to another ring system. The name is also used to refer to a class of synthetic steroids, called steroid-17α-spirolactones, 17α-spirol ...

antimineralocorticoids that were never marketed like

dicirenone Dicirenone (International Nonproprietary Name, INN, United States Adopted Name, USAN; developmental code name SC-26304; also known as 7α-carboxyisopropylspirolactone) is a synthetic compound, synthetic, steroidal antimineralocorticoid of the spi ...

mespirenone Mespirenone (INN) (developmental code name ZK-94679), also known as Δ1-15β,16β-methylenespironolactone, is a steroidal antimineralocorticoid of the spirolactone group related to spironolactone that was never marketed. Animal research found th ...

mexrenone Mexrenone (code names ZK-32055, SC-25152) is a steroidal antimineralocorticoid of the spirolactone group related to spironolactone that was never marketed. It is the lactonic form of mexrenoic acid (mexrenoate), and mexrenoate potassium (SC-2 ...

prorenone Prorenone (developmental code name SC-23133) is a steroidal antimineralocorticoid of the spirolactone group related to spironolactone that was never marketed. It is the lactonic form of prorenoic acid (prorenoate), and prorenoate potassium (S ...

SC-5233 SC-5233, also known as 6,7-dihydrocanrenone or 20-spirox-4-ene-3,20-dione, is a synthetic, steroidal antimineralocorticoid of the spirolactone group which was developed by G. D. Searle & Company in the 1950s but was never marketed. It was the fi ...

(spirolactone),

spirorenone Spirorenone (INN) (developmental code name ZK-35973) is a steroidal antimineralocorticoid of the spirolactone group that was never marketed. Spirorenone possesses 5–8 times the antimineralocorticoid activity of spironolactone in animal studies ...

, and

spiroxasone Spiroxasone (, ) is a synthetic, steroidal antimineralocorticoid of the spirolactone group which was developed as a diuretic and antihypertensive agent but was never marketed. It was synthesized and assayed in 1963. The drug is 7α-acetylthi ...

also show varying degrees of activity as AR antagonists.

Medical uses

Available forms

Pharmacology

List of SAAs

Marketed

Used specifically as antiandrogens (major)

Used specifically as antiandrogens (minor)

Used as antiandrogens in veterinary medicine

Used exclusively as progestins in women

Miscellaneous

Not marketed

Under development

Development discontinued

See also

References

Further reading