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 t ...

with a

steroid A steroid is an organic compound with four fused compound, fused rings (designated A, B, C, and D) arranged in a specific molecular configuration. Steroids have two principal biological functions: as important components of cell membranes t ...

chemical structure A chemical structure of a molecule is a spatial arrangement of its atoms and their chemical bonds. Its determination includes a chemist's specifying the molecular geometry and, when feasible and necessary, the electronic structure of the target m ...

. They are typically

antagonist An antagonist is a character in a story who is presented as the main enemy or rival of the protagonist and is often depicted as a villain.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 ) is any natural or synthetic steroid hormone that regulates the development and maintenance of male characteristics in vertebrates by binding to androgen receptors. This includes ...

s like

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

and

dihydrotestosterone Dihydrotestosterone (DHT, 5α-dihydrotestosterone, 5α-DHT, androstanolone or stanolone) is an endogenous androgen sex steroid and hormone primarily involved in the growth and repair of the prostate and the penis, as well as the production o ...

(DHT) and by suppressing

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

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

hypothalamus The hypothalamus (: hypothalami; ) is a small part of the vertebrate brain that contains a number of nucleus (neuroanatomy), nuclei with a variety of functions. One of the most important functions is to link the nervous system to the endocrin ...

. 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 in men and women, and are also used in

veterinary medicine Veterinary medicine is the branch of medicine that deals with the prevention, management, medical diagnosis, diagnosis, and treatment of disease, disorder, and injury in non-human animals. The scope of veterinary medicine is wide, covering all a ...

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 lik ...

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 the neoplasm, uncontrolled growth of cells in the prostate, a gland in the male reproductive system below the bladder. Abnormal growth of the prostate tissue is usually detected through Screening (medicine), screening tests, ...

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, urinary retention, inability t ...

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, ...

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 ma ...

seborrhea A sebaceous gland or oil 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 t ...

, 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 h ...

(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, hair loss on the scalp, increased body or facial hair, and infre ...

, such as due to

polycystic ovary syndrome Polycystic ovary syndrome, or polycystic ovarian syndrome, (PCOS) is the most common endocrine disorder in women of reproductive age. The name is a misnomer, as not all women with this condition develop cysts on their ovaries. The name origin ...

congenital adrenal hyperplasia Congenital adrenal hyperplasia (CAH) is a group of Genetic disorder#Autosomal recessive, autosomal recessive disorders characterized by impaired cortisol synthesis. It results from the deficiency of one of the five enzymes required for the Biosy ...

, 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 hormonal therap ...

for

transgender women A trans woman or transgender woman is a woman who was assigned male at birth. Trans women have a female gender identity and may experience gender dysphoria (distress brought upon by the discrepancy between a person's gender identity and their ...

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. There is early developm ...

in boys *

Hypersexuality Hypersexuality is a proposed medical condition said to cause unwanted or excessive sexual arousal, causing people to engage in or think about sexual activity to a point of distress or impairment., according to the website of ''Psychology Toda ...

and

paraphilia A paraphilia is an experience of recurring or intense sexual arousal to atypical objects, places, situations, fantasies, behaviors, or individuals. It has also been defined as a sexual interest in anything other than a legally consenting human ...

s in men and

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

s * Priapism in men

Available forms

Pharmacology

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

progestogen Progestogens, also sometimes written progestins, 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 progestoge ...

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 vertebra ...

, or

antimineralocorticoid A mineralocorticoid receptor antagonist (MRA or MCRA) or aldosterone antagonist, is a diuretic drug which receptor antagonist, antagonizes the action of aldosterone at mineralocorticoid receptors. This group of drugs is often used as adjunctive t ...

activity, possess antigonadotropic effects, and are weak

partial agonist In pharmacology, partial agonists are drugs that bind to and activate a given Receptor (biochemistry), receptor, but have only partial Intrinsic activity, efficacy at the receptor relative to a full agonist. They may also be considered Ligand (bio ...

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 of the use of a medicinal drug or other treatment, usually adverse but sometimes beneficial, that is unintended. Herbal and traditional medicines also have side effects. A drug or procedure usually use ...

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 distinction is now often made betwee ...

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 tre ...

(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 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 metabolic organ (anatomy), organ exclusively found in vertebrates, which performs many essential biological Function (biology), functions such as detoxification of the organism, and the Protein biosynthesis, synthesis of var ...

changes and

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

. Also has a high incidence of

psychiatric Psychiatry is the medical specialty devoted to the diagnosis, treatment, and prevention of deleterious mental conditions. These include matters related to cognition, perceptions, mood, emotion, and behavior. Initial psychiatric assessment of ...

s such as depression,

anxiety Anxiety is an emotion characterised by an unpleasant state of inner wikt:turmoil, turmoil and includes feelings of dread over Anticipation, anticipated events. Anxiety is different from fear in that fear is defined as the emotional response ...

, and

fatigue Fatigue is a state of tiredness (which is not sleepiness), exhaustion or loss of energy. It is a signs and symptoms, symptom of any of various diseases; it is not a disease in itself. Fatigue (in the medical sense) is sometimes associated wit ...

. *

Spironolactone Spironolactone, sold under the brand name Aldactone among others, is classed as a diuretic medication. It can be used to treat edema, fluid build-up due to hepatic cirrhosis, liver disease or kidney disease. It is also used to reduce risk o ...

(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 ...

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 ...

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, heart failure, kidney failure and myocardial infa ...

for

cardiovascular disease Cardiovascular disease (CVD) is any disease involving the heart or blood vessels. CVDs constitute a class of diseases that includes: coronary artery diseases (e.g. angina, heart attack), heart failure, hypertensive heart disease, rheumati ...

. Commonly associated with

gynecomastia Gynecomastia (also spelled gynaecomastia) is the non-cancerous enlargement of one or both breasts in men due to the growth of breast tissue as a result of a hormone imbalance between estrogens and androgens. Updated by Brent Wisse (10 Novemb ...

(breast development) and

menstrual disturbance A menstrual disorder is characterized as any abnormal condition with regards to a woman'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 (Prostal): A combined AR antagonist and progestogen/antigonadotropin. Also has weak

activity. Widely used in the treatment of prostate cancer in

Japan Japan is an island country in East Asia. Located in the Pacific Ocean off the northeast coast of the Asia, Asian mainland, it is bordered on the west by the Sea of Japan and extends from the Sea of Okhotsk in the north to the East China Sea ...

, 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. Ethinylestradiol was widely used for various indications such as the treatment of menopausal symptoms, gynecological ...

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

United States The United States of America (USA), also known as the United States (U.S.) or America, is a country primarily located in North America. It is a federal republic of 50 U.S. state, states and a federal capital district, Washington, D.C. The 48 ...

. * Gestonorone caproate (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 Northwestern Europe, off the coast of European mainland, the continental mainland. It comprises England, Scotlan ...

. Not available in the United States. *

Hydroxyprogesterone caproate Hydroxyprogesterone caproate, sold under the brand name Delalutin among others, is a medication used to reduce the risk of preterm birth in women pregnant with one baby who have a history of spontaneous preterm birth. In March 2023, the manuf ...

(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 referred to as impotence, is a form of sexual dysfunction in males characterized by the persistent or recurring inability to achieve or maintain a Human penis, penile erection with sufficient rigidity and durat ...

in two-thirds of men. Mostly used for gynecological 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 (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 ho ...

. 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 American and British English spelling differences) is the area of medicine concerned with conditions affecting the female reproductive system. It is often paired with the field of obstetrics, which focuses on pre ...

s and in

menopause Menopause, also known as the climacteric, is the time when Menstruation, menstrual periods permanently stop, marking the end of the Human reproduction, reproductive stage for the female human. It typically occurs between the ages of 45 and 5 ...

. 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 ...

(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 (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 syndrome that happens when people have certain illnesses, causing muscle loss that cannot be fully reversed with improved nutrition. It is most common in diseases like cancer, Heart failure, congestive heart failure, chronic o ...

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

only. Marketed in

Europe Europe is a continent located entirely in the Northern Hemisphere and mostly in the Eastern Hemisphere. It is bordered by the Arctic Ocean to the north, the Atlantic Ocean to the west, the Mediterranean Sea to the south, and Asia to the east ...

and

Oceania Oceania ( , ) is a region, geographical region including Australasia, Melanesia, Micronesia, and Polynesia. Outside of the English-speaking world, Oceania is generally considered a continent, while Mainland Australia is regarded as its co ...

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, urinary retention, inability t ...

in dogs. * Osaterone acetate (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.

Used exclusively as progestins in women

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

estradiol valerate Estradiol valerate (EV), sold for use oral administration, by mouth under the brand name Progynova and for use by injection (medicine), injection under the brand names Delestrogen and Progynon Depot among others, is an estrogen (medication), es ...

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

endometriosis Endometriosis is a disease in which Tissue (biology), tissue similar to the endometrium, the lining of the uterus, grows in other places in the body, outside the uterus. It occurs in women and a limited number of other female mammals. Endomet ...

. *

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 ...

: 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 called oestrogen, oestradiol, is an estrogen steroid hormone and the major female sex hormone. It is involved in the regulation of female reproductive cycles such as estrous and menstrual cycles. Estradiol is responsible ...

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. It is available ...

(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, and also known by its developmental code name RU-486, is a drug typically used in combination with misoprostol to bring about a medical abortion during pregnancy. This combination is 97% effective during the first 63 days (9 wee ...

(RU-486; Mifegyne, Mifeprex): An antiprogestogen 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 Antiglucocorticoid drugs are a class of medications that act to reduce the effects of glucocorticoids, primarily cortisol, in the body. They include direct glucocorticoid receptor antagonists such as mifepristone and synthesis inhibitors such as ...

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 inhibitors like the CYP17A1 inhibitor

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 metasta ...

(Zytiga) or the 5α-reductase inhibitors

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

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 bene ...

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 (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-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 (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. There is early developm ...

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

anabolic–androgenic steroid Anabolic steroids, also known as anabolic-androgenic steroids (AAS), are a class of drugs that are structurally related to testosterone, the main male sex hormone, and produce effects by binding to the androgen receptor (AR). Anabolism, Anaboli ...

metribolone (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 antiprogestogenic 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 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 ( INN, USAN; developmental code name SC-26304; also known as 7α-carboxyisopropylspirolactone) is a synthetic, steroidal antimineralocorticoid of the spirolactone group which was developed as a diuretic and antihypertensive agent but ...

mespirenone Mespirenone (International Nonproprietary Name, INN; developmental code ZK-94679; also known as Δ1-15β,16β-methylenespironolactone) is a steroidal antimineralocorticoid of the spirolactone group related to spironolactone that was never market ...

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 f ...

(spirolactone),

spirorenone Spirorenone (International Nonproprietary Name, INN; developmental code ZK-35973) is a steroidal antimineralocorticoid of the spirolactone group that was never marketed. Spirorenone possesses 5–8 times the antimineralocorticoid activity of spir ...

, 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-acetylthios ...

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