Telapristone (), as telapristone acetate (proposed brand names Proellex, Progenta; former code name CDB-4124), is a
synthetic,
steroid
A steroid is a biologically active organic compound with four rings arranged in a specific molecular configuration. Steroids have two principal biological functions: as important components of cell membranes that alter membrane fluidity; and a ...
al
selective progesterone receptor modulator
A selective progesterone receptor modulator (SPRM) is an agent that acts on the progesterone receptor (PR), the biological target of progestogens like progesterone. A characteristic that distinguishes such substances from full receptor agonists (e ...
(SPRM) related to
mifepristone
Mifepristone, also known as RU-486, is a medication typically used in combination with misoprostol to bring about a medical abortion during pregnancy and manage early miscarriage. This combination is 97% effective during the first 63 days of p ...
which is under development by Repros Therapeutics for the treatment of
breast cancer
Breast cancer is cancer that develops from breast tissue. Signs of breast cancer may include a lump in the breast, a change in breast shape, dimpling of the skin, milk rejection, fluid coming from the nipple, a newly inverted nipple, or a re ...
,
endometriosis
Endometriosis is a disease of the female reproductive system in which cells similar to those in the endometrium, the layer of tissue that normally covers the inside of the uterus, grow outside the uterus. Most often this is on the ovaries, f ...
, and
uterine fibroids
Uterine fibroids, also known as uterine leiomyomas or fibroids, are benign smooth muscle tumors of the uterus. Most women with fibroids have no symptoms while others may have painful or heavy periods. If large enough, they may push on the bl ...
.
It was originally developed by the
National Institutes of Health
The National Institutes of Health, commonly referred to as NIH (with each letter pronounced individually), is the primary agency of the United States government responsible for biomedical and public health research. It was founded in the late ...
(NIH), and, as of 2017, is in
phase II clinical trial
Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, dietar ...
s for the aforementioned indications.
In addition to its activity as an SPRM, the drug also has some
antiglucocorticoid
An antiglucocorticoid is a drug which reduces glucocorticoid activity in the body. They include direct glucocorticoid receptor antagonists such as mifepristone and synthesis inhibitors such as metyrapone, ketoconazole, and aminoglutethimide. ...
activity.
See also
*
List of investigational sex-hormonal agents ยง Progestogenics
*
Aglepristone
Aglepristone () (brand name Alizin; former developmental code names RU-46534, RU-534) is a synthetic, steroidal antiprogestogen related to mifepristone which is marketed by Virbac in several European countries for use in veterinary medicine. It i ...
*
Lilopristone
Lilopristone ( INN) (developmental code names ZK-98734, ZK-734) is a synthetic, steroidal antiprogestogen with additional antiglucocorticoid activity which was developed by Schering and was patented in 1985. It is described as an abortifacient a ...
*
Onapristone
Onapristone () (developmental code names ZK-89299, ZK-299) is a synthetic and steroidal antiprogestogen with additional antiglucocorticoid activity which was developed by Schering in and described in 1984 but was never marketed. in in It is a ...
*
Toripristone
Toripristone (INN) (developmental code name RU-40555) is a synthetic, steroidal antiglucocorticoid as well as antiprogestogen which was never marketed.https://mednet-communities.net/inn/db/media/docs/p-innlist61.pdf It is reported as a potent an ...
References
External links
Telapristone - AdisInsight
Acetate esters
Dimethylamino compounds
Antiglucocorticoids
Estranes
Ketones
Selective progesterone receptor modulators
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