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

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Showing 21 - 27 of 27 results

Status:
US Previously Marketed
Source:
Percorten by Ciba
(1940)
Source URL:
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

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.
mixture
Status:
First approved in 2001

Class:
MIXTURE



Norelgestromin, the progestin, is the active metabolite of norgestimate and is structurally related to 19-nortestosterone. Norgestimate and norelgestromin mimic the physiologic effects of progesterone at the progesterone receptor. Johnson & Johnson developed an adhesive female contraceptive patch that contains ethinylestradiol (0.75mg) and the progestogen norelgestromin (6mg). his product is a combination contraceptive acting via the inhibition gonadotropins. Its primary mechanism of action involves the suppression of ovulation, including changes in the cervical mucus and endometrium. The patch delivers a continuous flow of hormones through the skin and into the bloodstream. The contraceptive patch is available in countries worldwide.
mixture
Status:
First approved in 1989

Class:
MIXTURE



Norgestimate is a steroidal progestin of the 19-nortestosterone group that is used in combination with ethinylestradiol as an oral contraceptive and for treatment of acne. and in combination with estradiol in menopausal hormone replacement therapy. Norgestimate shows high selectivity for the progesterone receptor and low androgenic activity.

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Ulipristal acetate (also known as CDB-2914 and PGL4001 and trade name Ella in the U.S) is a novel oral emergency contraceptive designed and developed by HRA Pharma. It is a selective progesterone receptor modulator, which reversibly blocks the progesterone receptors in target tissues it was approved in May 2009 by the European Commission and in August 2010 by the FDA as safe and effective in preventing unintended pregnancy for up to 120 hours – or five days – post- unprotected intercourse or contraceptive failure. Ella is not intended for routine use as a contraceptive. When taken immediately before ovulation is to occur, ella postpones follicular rupture. The likely primary mechanism of action of ulipristal acetate for emergency contraception is therefore inhibition or delay of ovulation; however, alterations to the endometrium that may affect implantation may also contribute to efficacy. The most common side effects are: headache, nausea, stomach (abdominal) pain, menstrual pain. Some women taking ella may have their next period earlier or later than expected. If your period is more than a week late, you should get a pregnancy test.
Estradiol an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Estradiol-17-beta is the most potent form of mammalian estrogenic steroids. In humans, it is produced primarily by the cyclic ovaries and the placenta. It is also produced by the adipose tissue of men and postmenopausal women. The 17-alpha-isomer of estradiol binds weakly to estrogen receptors (receptors, estrogen) and exhibits little estrogenic activity in estrogen-responsive tissues. Estradiol enters target cells freely (e.g., female organs, breasts, hypothalamus, pituitary) and interacts with a target cell receptor. When the estrogen receptor has bound its ligand it can enter the nucleus of the target cell, and regulate gene transcription which leads to formation of messenger RNA. The mRNA interacts with ribosomes to produce specific proteins that express the effect of estradiol upon the target cell. Estradiol is used for the treatment of urogenital symptoms associated with post-menopausal atrophy of the vagina (such as dryness, burning, pruritus and dyspareunia) and/or the lower urinary tract (urinary urgency and dysuria). Estradiol is marketed under the brand name Climara (among others), indicated for: the treatment of moderate to severe vasomotor symptoms due to menopause, treatment of symptoms of vulvar and vaginal atrophy due to menopause, treatment of hypoestrogenism due to hypogonadism, castration or primary ovarian failure and prevention of postmenopausal osteoporosis.
Status:
Investigational
Source:
INN:telapristone [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Telapristone acetate, a selective progesterone receptor modulator (SPRM), was developed for the long-term treatment of symptoms associated with endometriosis and uterine fibroids. It is known, that the progesterone is a steroid hormone that plays an important role in the breast. Deregulation of the progesterone-signaling pathway is implicated in the formation, development, and progression of breast cancer. Thus, the telapristone acetate is studied in phase II clinical trial in stage I-II primary breast cancer. Besides, telapristone acetate participated in phase III clinical trials in pre-menopausal anemic women with symptomatic uterine fibroids. However, FDA terminated these studies because of the safety.