Steroidal antiandrogen | |
---|---|
Drug class | |
![]()
Cyproterone acetate, the most widely employed steroidal antiandrogen. | |
Class identifiers | |
Synonyms | Steroidal androgen receptor antagonists |
Use | Prostate cancer; Benign prostatic hyperplasia; Acne; Hirsutism; Seborrhea; Pattern hair loss; Hyperandrogenism; Transgender hormone therapy; Hypersexuality; Paraphilias; Male precocious puberty; Priapism |
ATC code | G03HA |
Biological target | Androgen receptor |
Chemical class | Steroidal |
Legal status | |
In Wikidata |
A steroidal antiandrogen (SAA) is an antiandrogen with a steroidal chemical structure. [1] [2] [3] They are typically antagonists of the androgen receptor (AR) and act both by blocking the effects of androgens like testosterone and dihydrotestosterone (DHT) and by suppressing gonadal androgen production. [2] [3] SAAs lower concentrations of testosterone through simulation of the negative feedback inhibition of the hypothalamus. [4] SAAs are used in the treatment of androgen-dependent conditions in men and women, and are also used in veterinary medicine for the same purpose. [2] They are the converse of nonsteroidal antiandrogens (NSAAs), which are antiandrogens that are not steroids and are structurally unrelated to testosterone. [2] [3]
SAAs are used in clinical medicine for the following indications: [2]
Generic name | Class | Type | Brand name(s) | Route(s) | Launch | Status | Hitsa |
---|---|---|---|---|---|---|---|
Abiraterone acetate | Steroidal | Androgen synthesis inhibitor | Zytiga | Oral | 2011 | Available | 523,000 |
Allylestrenol | Steroidal | Progestin | Gestanin, Perselin | Oral | 1961 | Availableb | 61,800 |
Chlormadinone acetate | Steroidal | Progestin; AR antagonist | Belara, Prostal | Oral | 1965 | Available | 220,000 |
Cyproterone acetate | Steroidal | Progestin; AR antagonist | Androcur, Diane | Oral, IM | 1973 | Available | 461,000 |
Delmadinone acetate | Steroidal | Progestin; AR antagonist | Tardak | Veterinary | 1972 | Veterinary | 42,600 |
Gestonorone caproate | Steroidal | Progestin | Depostat, Primostat | IM | 1973 | Availableb | 119,000 |
Hydroxyprogesterone caproate | Steroidal | Progestin | Delalutin, Proluton | IM | 1954 | Available | 108,000 |
Medroxyprogesterone acetate | Steroidal | Progestin | Provera, Depo-Provera | Oral, IM, SC | 1958 | Available | 1,250,000 |
Megestrol acetate | Steroidal | Progestin; AR antagonist | Megace | Oral | 1963 | Available | 253,000 |
Osaterone acetate | Steroidal | Progestin; AR antagonist | Ypozane | Veterinary | 2007 | Veterinary | 87,600 |
Oxendolone | Steroidal | Progestin; AR antagonist | Prostetin, Roxenone | IM | 1981 | Availableb | 36,100 |
Spironolactone | Steroidal | AR antagonist | Aldactone | Oral, topical | 1959 | Available | 3,010,000 |
Footnotes: a = Hits = Google Search hits (as of February 2018). b = Availability limited / mostly discontinued. Class: Steroidal = Steroidal antiandrogen. Nonsteroidal = Nonsteroidal antiandrogen. Sources: See individual articles. |
Unlike NSAAs, most SAAs show off-target hormonal activity such as progestogenic, glucocorticoid, or antimineralocorticoid activity, possess antigonadotropic effects, and are weak partial agonists of the AR with some capacity to activate the receptor. [2] 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. [8] [9] [10] However, due to their other hormonal effects, suppression of estrogen levels alongside testosterone levels, and AR activation, SAAs have increased side effects and show lower efficacy in the treatment of prostate cancer relative to NSAAs. [2]
Steroidal androgen synthesis inhibitors like the CYP17A1 inhibitor abiraterone acetate (Zytiga) or the 5α-reductase inhibitors finasteride and dutasteride could also technically be described as "SAAs", but the term is usually reserved to describe AR antagonists (and sometimes progestogenic antigonadotropins).
There are many different androgen blockers used for transition care. Spironolactone, an aldosterone receptor antagonist, is frequently used in the United States, whereas cyproterone acetate, a synthetic steroidal antiandrogen with prostogenic properties, is predominantly outside of the United States.
... Hormone therapy is prescribed for male-to-female transsexuals to induce breast formation and ... To achieve these goals, the biologic action of androgens must be almost completely neutralized. ... combining this treatment [of administrating estrogens] with ... other medications that suppress androgen action (e.g., cyproterone acetate, ...) appears to be more effective. ...
Steroidal antiandrogen | |
---|---|
Drug class | |
![]()
Cyproterone acetate, the most widely employed steroidal antiandrogen. | |
Class identifiers | |
Synonyms | Steroidal androgen receptor antagonists |
Use | Prostate cancer; Benign prostatic hyperplasia; Acne; Hirsutism; Seborrhea; Pattern hair loss; Hyperandrogenism; Transgender hormone therapy; Hypersexuality; Paraphilias; Male precocious puberty; Priapism |
ATC code | G03HA |
Biological target | Androgen receptor |
Chemical class | Steroidal |
Legal status | |
In Wikidata |
A steroidal antiandrogen (SAA) is an antiandrogen with a steroidal chemical structure. [1] [2] [3] They are typically antagonists of the androgen receptor (AR) and act both by blocking the effects of androgens like testosterone and dihydrotestosterone (DHT) and by suppressing gonadal androgen production. [2] [3] SAAs lower concentrations of testosterone through simulation of the negative feedback inhibition of the hypothalamus. [4] SAAs are used in the treatment of androgen-dependent conditions in men and women, and are also used in veterinary medicine for the same purpose. [2] They are the converse of nonsteroidal antiandrogens (NSAAs), which are antiandrogens that are not steroids and are structurally unrelated to testosterone. [2] [3]
SAAs are used in clinical medicine for the following indications: [2]
Generic name | Class | Type | Brand name(s) | Route(s) | Launch | Status | Hitsa |
---|---|---|---|---|---|---|---|
Abiraterone acetate | Steroidal | Androgen synthesis inhibitor | Zytiga | Oral | 2011 | Available | 523,000 |
Allylestrenol | Steroidal | Progestin | Gestanin, Perselin | Oral | 1961 | Availableb | 61,800 |
Chlormadinone acetate | Steroidal | Progestin; AR antagonist | Belara, Prostal | Oral | 1965 | Available | 220,000 |
Cyproterone acetate | Steroidal | Progestin; AR antagonist | Androcur, Diane | Oral, IM | 1973 | Available | 461,000 |
Delmadinone acetate | Steroidal | Progestin; AR antagonist | Tardak | Veterinary | 1972 | Veterinary | 42,600 |
Gestonorone caproate | Steroidal | Progestin | Depostat, Primostat | IM | 1973 | Availableb | 119,000 |
Hydroxyprogesterone caproate | Steroidal | Progestin | Delalutin, Proluton | IM | 1954 | Available | 108,000 |
Medroxyprogesterone acetate | Steroidal | Progestin | Provera, Depo-Provera | Oral, IM, SC | 1958 | Available | 1,250,000 |
Megestrol acetate | Steroidal | Progestin; AR antagonist | Megace | Oral | 1963 | Available | 253,000 |
Osaterone acetate | Steroidal | Progestin; AR antagonist | Ypozane | Veterinary | 2007 | Veterinary | 87,600 |
Oxendolone | Steroidal | Progestin; AR antagonist | Prostetin, Roxenone | IM | 1981 | Availableb | 36,100 |
Spironolactone | Steroidal | AR antagonist | Aldactone | Oral, topical | 1959 | Available | 3,010,000 |
Footnotes: a = Hits = Google Search hits (as of February 2018). b = Availability limited / mostly discontinued. Class: Steroidal = Steroidal antiandrogen. Nonsteroidal = Nonsteroidal antiandrogen. Sources: See individual articles. |
Unlike NSAAs, most SAAs show off-target hormonal activity such as progestogenic, glucocorticoid, or antimineralocorticoid activity, possess antigonadotropic effects, and are weak partial agonists of the AR with some capacity to activate the receptor. [2] 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. [8] [9] [10] However, due to their other hormonal effects, suppression of estrogen levels alongside testosterone levels, and AR activation, SAAs have increased side effects and show lower efficacy in the treatment of prostate cancer relative to NSAAs. [2]
Steroidal androgen synthesis inhibitors like the CYP17A1 inhibitor abiraterone acetate (Zytiga) or the 5α-reductase inhibitors finasteride and dutasteride could also technically be described as "SAAs", but the term is usually reserved to describe AR antagonists (and sometimes progestogenic antigonadotropins).
There are many different androgen blockers used for transition care. Spironolactone, an aldosterone receptor antagonist, is frequently used in the United States, whereas cyproterone acetate, a synthetic steroidal antiandrogen with prostogenic properties, is predominantly outside of the United States.
... Hormone therapy is prescribed for male-to-female transsexuals to induce breast formation and ... To achieve these goals, the biologic action of androgens must be almost completely neutralized. ... combining this treatment [of administrating estrogens] with ... other medications that suppress androgen action (e.g., cyproterone acetate, ...) appears to be more effective. ...