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

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Showing 11 - 20 of 27 results

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 Chlormadinone acetate was withdrawn from the market in the USA, but it is still being used in Europe under the name Belara.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:
US Previously Marketed
First approved in 1963
Source:
Duphaston by Philips Roxane
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Dydrogesterone is an orally active progestogen which acts directly on the uterus, producing a complete secretory endometrium in an estrogen-primed uterus. At therapeutic levels, dydrogesterone has no contraceptive effect as it does not inhibit or interfere with ovulation or the corpus luteum. Furthermore, dydrogesterone is non-androgenic, non-estrogenic, non-corticoid, non-anabolic and is not excreted as pregnanediol. Dydrogesterone helps to regulate the healthy growth and normal shedding of the uterus lining. Therefore, it may be useful in the treatment of menstrual disorders such as absent, irregular or painful menstrual periods, infertility, premenstrual syndrome and endometriosis. Dydrogesterone works by regulating the healthy growth and normal shedding of the womb lining by acting on progesterone receptors in the uterus. Used to treat irregular duration of cycles and irregular occurrence and duration of periods caused by progesterone deficiency. Also used to prevent natural abortion in patients who have a history of habitual abortions. Dydrogesterone was first introduced to the market in 1961, and is currently approved in over 100 countries world-wide. Banned in the USA and wthdrawn from the UK, but still used in other countries.
Status:
US Previously Marketed
First approved in 1957
Source:
Enovid by Searle
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Norethynodrel is a steroidal progestin of the 19-nortestosterone group and an isomer of norethisterone. Norethynodrel is a progesteron agonist with very weak estrogenic activiry. Noretynodrel was introduced in 1957 in Enovid, a combination formulation of noretynodrel and mestranol, for the treatment of gynecological and menstrual disorders.A few years later, in May 1960, Enovid was also approved as the first oral contraceptive.
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:
Possibly Marketed Outside US
Source:
Canada:ALTRENOGEST
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Altrenogest (INN, USAN, BAN) (brand name Regumate), also known as allyltrenbolone, is a steroidal progestin that is widely used in veterinary medicine to suppress estrus in animals. Altrenogest is an orally active progestin developed for use in the horse. Altrenogest has been chemically modified by addition of a hydroxyl group and 3 carbon chain placed on carbon 17 of the progestin. Research has demonstrated that Altrenogest has low anabolic activity and is 20 times less potent than testosterone or similar progestins when compared for effects on muscle growth in castrated rats
Status:
Possibly Marketed Outside US
Source:
NCT00195455: Phase 4 Interventional Completed Postmenopause
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Trimegestone is a 19-norpregnane progestin. It has a potent progesterone receptor and very low androgen receptor affinities but no detectable affinity to oestrogen receptor. Trimegestone has been developed for use in conjunction with oestrogen and 17-beta-estradiol for postmenopausal hormone replacement therapy. In vitro studies have shown that trimegestone can inhibit cytochrome P450 2C19 (CYP2C19). Although its clinical importance is unknown, trimegestone can moderately elevate the plasma concentration of drugs metabolized through CYP2C19, such as citalopram, imipramine and diazepam. Trimegestone is an effective and well-tolerated new progestin, which does not negate the beneficial effects of oestrogen on lipids.
Status:
Possibly Marketed Outside US
Source:
Wien Med Wochenschr. 1995;145(1):18-21.: Phase 4 Human clinical trial Completed N/A
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Medrogestone is a progesterone derivative used for the treatment of progesterone deficiency, especially those observed in the premenopausal period, haemorrhages and menorrhagia of fibroids, endometriosis, menstrual cycle disorders, etc. The drug acts by binding and activating progesterone receptors. In Europe, medrogestone is available under the name Colprone, however it is no longer marketed in the USA, Germany and Austria.
Status:
Possibly Marketed Outside US
Source:
Gestageno
Source URL:

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.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Promegestone (R 5020) is a potent progestin devoid of androgenic side-effects and has marked anti-estrogenic activity. Promegestone is an AChR noncompetitive antagonist that may alter AChR function by interactions at the lipid-protein interface. Promegestone is used in the treatment of gynecological disorders due to luteal insufficiency.
Status:
Possibly Marketed Outside US
Source:
PRIMOSTAT by Schering
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Gestonorone is a progesterone analogue indicated for the treatment of benign prostatic hyperplasia and endometrial cancer. The drug is approved in many countries and used under the names Primostat and Depostat.

Showing 11 - 20 of 27 results