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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 silent antagonist of the progesterone receptor (PR), in contrast to the related antiprogestogen mifepristone (which is a weak partial agonist of the receptor). in Moreover, compared to mifepristone, onapristone has reduced antiglucocorticoid activity, shows little antiandrogenic activity, and has 10- to 30-fold greater potency as an antiprogestogen. The medication was under development for clinical use, for instance in the treatment of breast cancer and as an endometrial contraceptive, but was discontinued during phase III clinical trials in 1995 due to findings that liver function abnormalities developed in a majority patients. in Onapristone has been found to be effective in the treatment of breast cancer. As of 2016, onapristo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Telapristone
Telapristone (), as telapristone acetate (proposed brand names Proellex, Progenta; former code name CDB-4124), is a synthetic, steroidal selective progesterone receptor modulator (SPRM) related to mifepristone which is under development by Repros Therapeutics for the treatment of breast cancer, endometriosis, and uterine fibroids. It was originally developed by the National Institutes of Health (NIH), and, as of 2017, is in phase II clinical trials for the aforementioned indications. In addition to its activity as an SPRM, the drug also has some antiglucocorticoid activity. See also * List of investigational sex-hormonal agents § Progestogenics * Aglepristone * Lilopristone * Onapristone * 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 a ... References External l ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 and highly selective antagonist of the glucocorticoid receptor (GR) (Ki = 2.4 nM), though it also acts as an antagonist of the progesterone receptor (PR). The pharmacological profile of toripristone is said to be very similar to that of mifepristone, except that toripristone does not bind to orosomucoid (α1-acid glycoprotein). The drug has been used to study the hypothalamic-pituitary-adrenal axis and has been used as a radiotracer for the GR. Its INN was given in 1990. See also * Aglepristone * Lilopristone * 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 b ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 and endometrial contraceptive. The drug differs from mifepristone only in the structure of its C17α side chain, and is said to have much reduced antiglucocorticoid activity in comparison. See also * Aglepristone * 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 ... * Telapristone * Toripristone References Further reading * * Abortifacients Alkene derivatives Dimethylamino compounds Antiglucocorticoids Antiprogestogens Estranes Enones Conjugated dienes {{genito-urinary-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 is specifically used as an abortifacient in pregnant animals. Aglepristone, similarly to mifepristone, also possesses some antiglucocorticoid activity. See also * Lilopristone * 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 ... * Telapristone * Toripristone References Abortifacients Alkene derivatives Dimethylamino compounds Antiglucocorticoids Antiprogestogens Estranes Enones Theriogenology Veterinary drugs {{steroid-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
List Of Investigational Sex-hormonal Agents
This is a list of investigational sex-hormonal agents, or sex-hormonal agents that are currently under development for clinical use but are not yet approved. ''Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in parentheses.'' Androgenics Androgen receptor agonists * EC586 – oral prodrug of testosterone ( androgen/anabolic steroid) with improved pharmacokinetics Androgen receptor antagonists * Bavdegalutamide (AVR-110) – androgen receptor antagonist for * Deutenzalutamide (deuterated enzalutamide; HC-1119) – androgen receptor antagonist for prostate cance * [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antiprogestogen
Antiprogestogens, or antiprogestins, also known as progesterone antagonists or progesterone blockers, are a class of drugs which prevent progestogens like progesterone from mediating their biological effects in the body. They act by blocking the progesterone receptor (PR) and/or inhibiting or suppressing progestogen production. Antiprogestogens are one of three types of sex hormone antagonists, the others being antiestrogens and antiandrogens. Antiprogestogens are used as abortifacients and emergency contraceptives and in the treatment of uterine fibroids. They are also being studied in the treatment of breast cancer. Examples of antiprogestogens include the progesterone receptor weak partial agonist mifepristone, the selective progesterone receptor modulator (SPRM) ulipristal acetate, and the silent antagonist aglepristone. For medical abortion, mifepristone is combined with a prostaglandin (e.g., gemeprost). Several hundred antiprogestogens have been developed, but ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Clinical Trial
Clinical trials are prospective biomedical or behavioral research studies on human subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, pharmaceutical drug, drugs, medical nutrition therapy, dietary choices, dietary supplements, and medical devices) and known interventions that warrant further study and comparison. Clinical trials generate data on dosage, safety and efficacy. They are conducted only after they have received institutional review board, health authority/ethics committee approval in the country where approval of the therapy is sought. These authorities are responsible for vetting the risk/benefit ratio of the trial—their approval does not mean the therapy is 'safe' or effective, only that the trial may be conducted. Depending on product type and development stage, investigators initially enroll volunteers or patients into small Pilot experiment, pi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dimethylamino Compounds
Dimethylamine is an organic compound with the formula (CH3)2NH. This secondary amine is a colorless, flammable gas with an ammonia-like odor. Dimethylamine is commonly encountered commercially as a solution in water at concentrations up to around 40%. An estimated 270,000 tons were produced in 2005. Structure and synthesis The molecule consists of a nitrogen atom with two methyl substituents and one proton. Dimethylamine is a weak base and the pKa of the ammonium CH3--CH3 is 10.73, a value above methylamine (10.64) and trimethylamine (9.79). Dimethylamine reacts with acids to form salts, such as dimethylamine hydrochloride, an odorless white solid with a melting point of 171.5 °C. Dimethylamine is produced by catalytic reaction of methanol and ammonia at elevated temperatures and high pressure: :2 CH3OH + NH3 → (CH3)2NH + 2 H2O Natural occurrence Dimethylamine is found quite widely distributed in animals and plants, and is present in many foods at the lev ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Abortifacients
An abortifacient ("that which will cause a miscarriage" from Latin: '' abortus'' "miscarriage" and '' faciens'' "making") is a substance that induces abortion. This is a nonspecific term which may refer to any number of substances or medications, ranging from herbs to prescription medications. Common abortifacients used in performing medical abortions include mifepristone, which is typically used in conjunction with misoprostol in a two-step approach. Synthetic oxytocin, which is routinely used safely during term labor, is also commonly used to induce abortion in the second or third trimester. For thousands of years writers in many parts of the world have described and recommended herbal abortifacients to women who seek to terminate a pregnancy, although their use may carry risks to the health of the woman. Medications Because "abortifacient" is a broad term used to describe a substance's effects on pregnancy, there is a wide range of drugs that can be described as ab ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Uterine Cancer
Uterine cancer, also known as womb cancer, includes two types of cancer that develop from the tissues of the uterus. Endometrial cancer forms from the lining of the uterus, and uterine sarcoma forms from the muscles or support tissue of the uterus. Endometrial cancer accounts for approximately 90% of all uterine cancers in the United States. Symptoms of endometrial cancer include changes in vaginal bleeding or pain in the pelvis. Symptoms of uterine sarcoma include unusual vaginal bleeding or a mass in the vagina. Risk factors for endometrial cancer include obesity, metabolic syndrome, type 2 diabetes, taking pills that contain estrogen without progesterone, a history of tamoxifen use, late menopause, and a family history of the condition. Risk factors for uterine sarcoma include prior radiation therapy to the pelvis. Diagnosis of endometrial cancer is typically based on an endometrial biopsy. A diagnosis of uterine sarcoma may be suspected based on symptoms, a pelvic ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ovarian Cancer
Ovarian cancer is a cancerous tumor of an ovary. It may originate from the ovary itself or more commonly from communicating nearby structures such as fallopian tubes or the inner lining of the abdomen. The ovary is made up of three different cell types including epithelial cells, germ cells, and stromal cells. When these cells become abnormal, they have the ability to divide and form tumors. These cells can also invade or spread to other parts of the body. When this process begins, there may be no or only vague symptoms. Symptoms become more noticeable as the cancer progresses. These symptoms may include bloating, vaginal bleeding, pelvic pain, abdominal swelling, constipation, and loss of appetite, among others. Common areas to which the cancer may spread include the lining of the abdomen, lymph nodes, lungs, and liver. The risk of ovarian cancer increases with age. Most cases of ovarian cancer develop after menopause. It is also more common in women who have ovulat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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