U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 221 - 230 of 533 results

Status:
US Previously Marketed
Source:
Stenediol by Organon
(1951)
Source URL:
First approved in 1951
Source:
Stenediol by Organon
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Methandriol is an anabolic steroid. Methandriol is classified as a weak anabolic with weak androgenic properties. Methandriol displays some level of estrogenic activity, making this steroid less useful for dieting. The drug is generally considered too mild and is not widely popular among bodybuilders and athletes. It seems most prominent in Australia now, where it remains included in a number of veterinary anabolic steroid products.
Status:
US Previously Marketed
First approved in 1951
Source:
Tace by Merrell (MerrellNational)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Chlorotrianisene (TACE®) is a powerful synthetic, non-steroidal estrogen used to treat symptoms of menopause, deficiencies in ovary function (including underdevelopment of female sexual characteristics and some types of infertility), and in rare cases, prostate cancer. It may also be used to prevent breast engorgement following childbirth. Chlorotrianisene (TACE®) binds to the estrogen receptor on various estrogen receptor bearing cells. Target cells include cells in the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary.
Pregnenolone sulfate is an endogenous neurosteroid with excitatory effects in the brain, acting as a potent negative allosteric modulator of the GABAA receptor, a positive allosteric modulator of the NMDA receptor, and activator of transient receptor potential cation channel TRPM1 and TRPM3. In the model of schizophrenia, treatment with pregnenolone sulfate normalized the hyperlocomotion and stereotypic bouts, and rescued the PPI deficits of dopamine transporter knockout mice. Promnesic properties of pregnenolone sulfate were demonstrated in rat models of spatial memory performance.
Status:
US Previously Marketed
Source:
MEPRANE DIPROPIONATE by R&C
(1961)
Source URL:
First approved in 1947
Source:
Meprane Dipropionate by Reed & Camrick
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Methestrol is a nonsteroidal synthetic estrogen that has never been marketed.
Status:
US Previously Marketed
First approved in 1947
Source:
Synestrol by White (Schering)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Dienestrol (INN, USAN) (brand names Ortho Dienestrol, Dienoestrol, Dienoestrol Ortho, Sexadien, Denestrolin, Dienol, Dinovex, Follormon, Oestrodiene, Synestrol, numerous others) is a synthetic, non-steroidal estrogen. It is an estrogen receptor agonist. Estrogens work partly by increasing a normal clear discharge from the vagina and making the vulva and urethra healthy. Using or applying an estrogen relieves or lessens: dryness and soreness in the vagina, itching, redness, or soreness of the vulva. Conditions that are treated with vaginal estrogens include a genital skin condition (vulvar atrophy), inflammation of the vagina (atrophic vaginitis), and inflammation of the urethra (atrophic urethritis). Dienestrol currently discontinued in US, but still in market in some other counties
Status:
US Previously Marketed
Source:
Benzestrol by Schieffelin
(1942)
Source URL:
First approved in 1942
Source:
Benzestrol by Schieffelin
Source URL:

Class (Stereo):
CHEMICAL (MIXED)


Benzestrol (originally called 118B and Octofollin), synthetic nonsteroidal estrogen and analog of stilbestrol, was used for oral estrogenic therapy for women and in order to prevent premature births. Besides, benzestrol gave most of the patients’ satisfactory relief of their estrogen deficiency symptoms. However, its use has been discontinued.
Diethylstilbestrol is a synthetic non-steroidal estrogen. It is used in the treatment of menopausal and postmenopausal disorders, prostate cancer and in the prevention of miscarriage or premature delivery in pregnant women prone to miscarriage or premature delivery. Diethylstilbestrol is a very potent full agonist of the estrogen receptors. At the cellular level, estrogens increase the synthesis of DNA, RNA, and various proteins in target tissues. Pituitary mass is also increased. Estrogens reduce the release of gonadotropin-releasing hormone from the hypothalamus, leading to a reduction in release of follicle-stimulating hormone and luteinizing hormone from the pituitary. Adverse effects are: breast pain or tenderness, enlargement of breasts, gynecomastia, peripheral edema and others. Estrogens may interfere with the effects of bromocriptine. Dosage adjustment may be needed. Concurrent use with estrogens may alter the metabolism and protein binding of the glucocorticoids, leading to decreased clearance, increased elimination half-life, and increased therapeutic and toxic effects of the glucocorticoids.
Status:
US Previously Marketed
Source:
PRANONE by SCHERING
(1939)
Source URL:
First approved in 1939

Class (Stereo):
CHEMICAL (ABSOLUTE)



Ethisterone is a metabolite of danazol. Ethisterone is a progestogen hormone. The first orally active progestin, Ethisterone (brand names Pranone, Progestoral, Lutocylol, Proluton C), also known as 17α-ethinyltestosterone, pregneninolone, or anhydrohydroxyprogesterone, is a steroidal progestin with androgenic activity which is derived from testosterone and was introduced for medical use in 1939. Ethisterone is indicated for progesterone supplementation or replacement as part of an Assisted Reproductive Technology (ART) treatment for infertile women with progesterone deficiency and for the treatment of secondary amenorrhea. Also used as a female contraceptive.
Status:
US Previously Marketed
First approved in 1939

Class (Stereo):
CHEMICAL (ABSOLUTE)



Desoxycorticosterone pivalate (DOCP) is a mineralocorticoid hormone and an analog of desoxycorticosterone. DOCP is a long-acting ester of desoxycorticosterone acetate (DOCA) which is recognized as having the same qualitative effects as the natural mineralocorticoid hormone aldosterone. It’s used as Percorten-V for replacement therapy for the mineralocorticoid deficit in dogs with primary adrenocortical insufficiency. Percorten-V is only available in the U.S., Canada, Australia and recently, Denmark. Percorten was originally developed for the treatment of Addison's disease in humans but the demand for it decreased significantly once Florinef was available. Unaware that their product was being prescribed “off-label” for the treatment of canine Addison’s Disease and faced with a decreased demand for Percorten, the manufacturer *almost* discontinued production until the veterinary community rose up and voiced their distress. Field trials were run and the FDA approved the use of Percorten-V (the "v" is for veterinary). DOCP like other adrenocorticoid hormones is thought to act by controlling the rate of synthesis of proteins. It reacts with receptor proteins in the cytoplasm to form a steroid-receptor complex. This complex moves into the nucleus, where it binds to chromatin that result in genetic transcription of cellular DNA to messenger RNA. The steroid hormones appear to induce transcription and synthesis of specific proteins, which produce the physiologic effects seen after administration. The most important effect of DOCP is to increase the rate of renal tubular absorption of sodium. This effect is seen most intensely in the thick portion of the ascending limb of the loop of Henle. It also increases sodium absorption in the proximal convoluted tubule but this effect is less important in sodium retention. Chloride follows the sodium out of the renal tubule. Another important effect of DOCP is enhanced renal excretion of potassium. This effect is driven by the resorption of sodium that pulls potassium from the extracellular fluid into the renal tubules, thus promoting potassium excretion.
Status:
Possibly Marketed Outside US
Source:
NCT01056042: Phase 4 Interventional Completed Endometriosis
(2007)
Source URL:
First approved in 2018

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Gestodene (17alpa-ethynyl-13beta-ethyl-17beta-hydroxy-4,15-gonadien-3-one) is the most potent synthetic progestin currently available and it is widely used as a fertility regulating agent in a number of contraceptive formulations because of its high effectiveness, safety and acceptability. Products containing gestoden include Meliane, which contains 20 ug of ethinylestradiol and 75 ug of gestodene; and Gynera, which contains 30 ug of ethinylestradiol and 75 ug of gestodene. Gestodene is androgenically neutral, meaning that contraceptive pills containing gestodene do not exhibit the androgenic side effects (e.g. acne, hirsutism, weight gain) often associated with second-generation contraceptive pills. Gestodene displays a high binding affinity to the progesterone receptor, also binds to adrogen and glucocorticoid receptors but no measurable affinity for the estrogen receptor.

Showing 221 - 230 of 533 results