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

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Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
US Previously Marketed
Source:
C-Quens by Eli lilly
(1965)
Source URL:
First approved in 1965
Source:
C-Quens by Eli lilly
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Chlormadinone acetate (CMA) is a derivative of naturally secreted progesterone that shows high affinity and activity at the progesterone receptor. It has an anti-estrogenic effect and, in contrast to natural progesterone, shows moderate anti-androgenic properties. CMA acts by blocking androgen receptors in target organs and by reducing the activity of skin 5alpha-reductase. It suppresses gonadotropin secretion and thereby reduces ovarian and adrenal androgen production. CMA shows high contraceptive efficacy by inhibiting ovulation due to its ability to suppress or disrupt endogenous gonadotropin secretion and, by this, inhibits follicular growth and maturation. In addition, it suppresses endometrial thickness and increases the viscosity of cervical mucus. Chlormadinone acetate was withdrawn from the market in the USA, but it is still being used in Europe under the name Belara.
Status:
Possibly Marketed Outside US
Source:
Canada:MELENGESTROL ACETATE
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Melengestrol is a steroidal progestin and antineoplastic agent which was never marketed. An acylated derivative, melengestrol acetate, is used as a growth promoter in animals. Melengestrol acetate (MGA) is one of six steroidal hormone growth promoters approved for use in Canada and USA. These products are used to improve growth rate and feed efficiency, as well as to suppress estrus in beef heifers (CFIA 2008). They are not approved for use in any species other than beef cattle meant for slaughter. MGA is the only drug of its kind that is administered in animal feed, and its labelled dose in Canada is 0.4mg per heifer per day (CFIA 2008). A mandatory withdrawal of 2 days before slaughter is applied to any animal that is administered MGA.
Status:
Possibly Marketed Outside US
Source:
Canada:TRENBOLONE ACETATE
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Trenbolone is an anabolic steroid. It is used on livestock to increase muscle growth and appetite. Trenbolone compounds have a binding affinity for the androgen receptor three times as high as that of testosterone. Once metabolized, the drugs have the effect of increasing nitrogen uptake by muscles, leading to an increase in the rate of protein synthesis. It also has the secondary effects of stimulating appetite, reducing the amount of fat being deposited in the body, and decreasing the rate of catabolism. Short-term side effects include insomnia, high blood pressure, increased aggression, night sweats, and libido.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Cridanimod (Virexxa) is a small-molecule immunomodulator and interferon inducer, which, in preliminary studies, has been shown to increase progesterone receptor expression in endometrial tissue. Restoration of progesterone receptor expression may re-sensitize endometrial tumor tissue to progestin therapy in previously unresponsive tumors. Cridanimod was originally developed by Polysan and Pharmsynthez and licensed to Xenetic Biosciences. Virexxa is currently being studied in an ongoing Phase 2 multi-national study in conjunction with progestin therapy for the treatment of endometrial cancer in women with the recurrent or persistent disease who have failed progestin monotherapy.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Nomegestrol acetate (NOMAC) is a 19-norprogesterone derivative with high biological activity at the progesterone receptor, a weak anti-androgenic effect, but with no binding to estrogen, glucocorticoid or mineralocorticoid receptors. Nomegestrol has been developed by the Monaco-based company Théramex SAM (a Teva subsidiary). Nomegestrol acetate has been used successfully for the treatment of some gynaecological disorders (menstrual disturbances, dysmenorrhoea, premenstrual syndrome) and as a component of hormone replacement therapy in combination with estradiol for the relief of menopausal symptoms; it has been approved in Europe as monotherapy for the treatment of the menopausal syndrome, uterine diseases and menorrhagia, and in combination with an estrogen for the treatment of menopausal symptoms. Nomegestrol acetate in combination with estradiol is used as an oral contraceptive.
FLUROGESTONE (9α-FLUORO-11β,17α-DIHYDROXYPROGESTERONE) is a steroidal progestin of the 17α-hydroxyprogesterone group that was never marketed. An acetate ester, flurogestone acetate, is used in veterinary medicine. It has progestational action higher than that of progesterone itself. It is intended for intravaginal use in sheep and goats to induce oestrus synchronisation. The proposed dosage is 1 sponge, impregnated with 30, 40 (for sheep) or 45 mg (for goats) flugestone acetate, which is to be removed after 12 to 14 days from ewes and after 17 to 21 days from goats. Flugestone acetate is not indicated for use in humans.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



17α-Hydroxyprogesterone (17α-OHP), or hydroxyprogesterone (OHP), also known as 17α-hydroxypregn-4-ene-3, 20-dione is used under the brand name Gestageno, and has been marketed for clinical use in Argentina. It was indicated for female infertility, hypertrichosis, menstrual disorders, premature labour, threatened or recurrent miscarriage. It is used to properly regulate the menstrual cycle and treat unusual stopping of the menstrual periods (amenorrhea). To help a pregnancy occur during egg donor or infertility procedures in women who do not produce enough progesterone. To prevent estrogen from thickening the lining of the uterus (endometrial hyperplasia) in women around menopause who are being treated with estrogen for ovarian hormone therapy (OHT). To treat a condition called endometriosis, to help prevent endometrial hyperplasia, or to treat unusual and heavy bleeding of the uterus (dysfunctional uterine bleeding) by starting or stopping the menstrual cycle. 17α-OHP is an agonist of the progesterone receptor (PR) similarly to progesterone. In addition, it is an antagonist of the mineralocorticoid receptor (MR) as well as a partial agonist of the glucocorticoid receptor (GR), albeit with very low potency (EC50 >100-fold less relative to cortisol) at the latter site, also similarly to progesterone.