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GTx-758
GTx-758 (tentative brand name Capesaris) is a synthetic nonsteroidal estrogen which was under development by GTx, Inc. for the treatment of advanced prostate cancer. As of 2016, it had completed two phase II clinical trials. Pharmacology Pharmacodynamics GTx-758 acts as a selective agonist of the estrogen receptor (ER), with a more than 10-fold preference for activation of ERα relative to ERβ ( EC50 = 2.1 and 27 nM, respectively). The selectivity of GTx-758 for ERα over ERβ may confer reduced hypercoagulability and thrombophilia, as estradiol directly produces these effects in platelets via activation of ERβ, which is the predominant isoform of the ER expressed in platelets. It has been said that suppression of free testosterone levels by ERα activation-induced increase in hepatic sex hormone-binding globulin (SHBG) production is the primary mechanism of action of GTx-758 in the treatment of prostate cancer. Chemistry GTx-758 is a diphenyl benzamide and has a similar s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GTx Incorporated
GTx, Inc. is a pharmaceutical company that is working on drugs in the selective estrogen receptor modulator (SERM) and selective androgen receptor modulator (SARM) classes. Its drugs in development include enobosarm (ostarine) and GTx-758. The company was founded in Memphis in 1997 by Mitch Steiner and Marc S. Hanover. The company was originally called Genotherapeutics, changed its name to GTx, Inc. in 2001, and reincorporated in Delaware in 2003. The company licensed toremifene from Orion Corporation, and licensed andarine, enobosarm and prostarine from the University of Tennessee Research Foundation; the SARM compounds from Tennessee had been invented by Karen Veverka and Michael Whitt and each later joined the company. The company held its IPO in February 2004. In 2006 GTx signed a partnership with Ipsen Ipsen is a French biopharmaceutical company headquartered in Paris, France, with a focus on transformative medicines in three therapeutic areas: oncology, rare disease ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nonsteroidal Estrogen
A nonsteroidal estrogen is an estrogen with a nonsteroidal chemical structure. The most well-known example is the stilbestrol estrogen diethylstilbestrol (DES). Although nonsteroidal estrogens formerly had an important place in medicine, they have gradually fallen out of favor following the discovery of toxicities associated with high-dose DES starting in the early 1970s, and are now almost never used. On the other hand, virtually all selective estrogen receptor modulators (SERMs) are nonsteroidal, with triphenylethylenes like tamoxifen and clomifene having been derived from DES, and these drugs remain widely used in medicine for the treatment of breast cancer among other indications. In addition to pharmaceutical drugs, many xenoestrogens, including phytoestrogens, mycoestrogens, and synthetic endocrine disruptors like bisphenol A, are nonsteroidal substances with estrogenic activity. Pharmacology Nonsteroidal estrogens act as agonists of the estrogen receptors, ERα an ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oral Administration
Oral administration is a route of administration where a substance is taken through the mouth. Per os abbreviated to P.O. is sometimes used as a direction for medication to be taken orally. Many medications are taken orally because they are intended to have a systemic effect, reaching different parts of the body via the bloodstream, for example. Oral administration can be easier and less painful than other routes, such as injection. However, the onset of action is relatively low, and the effectiveness is reduced if it is not absorbed properly in the digestive system, or if it is broken down by digestive enzymes before it can reach the bloodstream. Some medications may cause gastrointestinal side effects, such as nausea or vomiting, when taken orally. Oral administration can also only be applied to conscious patients, and patients willing and able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzamide
Benzamide is a organic compound with the chemical formula of C6H5C(O)NH2. It is the simplest amide derivative of benzoic acid. In powdered form, it appears as a white solid, while in crystalline form, it appears as colourless crystals. It is slightly soluble in water, and soluble in many organic solvents. It is a natural alkaloid found in the herbs of Berberis pruinosa. Chemical derivatives A number of substituted A substitution reaction (also known as single displacement reaction or single substitution reaction) is a chemical reaction during which one functional group in a chemical compound is replaced by another functional group. Substitution reactions ar ... benzamides are commercial drugs, including: See also * References External links Physical characteristics {{Authority control Phenyl compounds ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hot Flash
Hot flashes (also known as hot flushes) are a form of flushing, often caused by the changing hormone levels that are characteristic of menopause. They are typically experienced as a feeling of intense heat with sweating and rapid heartbeat, and may typically last from two to 30 minutes for each occurrence. Signs and symptoms Hot flashes, a common symptom of menopause and perimenopause, are typically experienced as a feeling of intense heat with sweating and rapid heartbeat, and may typically last from two to thirty minutes for each occurrence, ending just as rapidly as they began. The sensation of heat usually begins in the face or chest, although it may appear elsewhere such as the back of the neck, and it can spread throughout the whole body. Some women feel as if they are going to faint. In addition to being an internal sensation, the surface of the skin, especially on the face, becomes hot to the touch. This is the origin of the alternative term "hot flush", since the sens ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hypoestrogenism
Hypoestrogenism, or estrogen deficiency, refers to a lower than normal level of estrogen. It is an umbrella term used to describe estrogen deficiency in various conditions. Estrogen deficiency is also associated with an increased risk of cardiovascular disease, and has been linked to diseases like urinary tract infections and osteoporosis. In women, low levels of estrogen may cause symptoms such as hot flashes, Sleep disorder, sleeping disturbances, decreased bone health, and changes in the genitourinary system. Hypoestrogenism is most commonly found in women who are postmenopausal, have primary ovarian insufficiency (POI), or are presenting with amenorrhea (absence of menstrual cycle, menstrual periods). Hypoestrogenism includes primarily genitourinary effects, including thinning of the vaginal tissue layers and an increase in Vagina#Infections, diseases, and safe sex, vaginal pH. With normal levels of estrogen, the environment of the vagina is protected against inflammation, in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hyperestrogenism
Hyperestrogenism, hyperestrogenic state, or estrogen excess, is a medical condition characterized by an excessive amount of estrogenic activity in the body. Signs and symptoms Signs of hyperestrogenism may include heightened levels of one or more of the estrogen sex hormones (usually estradiol and/or estrone), lowered levels of follicle-stimulating hormone and/or luteinizing hormone (due to suppression of the hypothalamic–pituitary–gonadal axis by estrogen), and lowered levels of androgens such as testosterone (generally only relevant to males). Symptoms of the condition in women may consist of menstrual irregularities, amenorrhea, abnormal vaginal bleeding, and enlargement of the uterus and breasts. It may also present as isosexual precocity in children and as hypogonadism, gynecomastia, feminization, impotence, and loss of libido in males. If left untreated, hyperestrogenism may increase the risk of estrogen-sensitive cancers such as breast cancer later in life. Causes Hyp ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Side Effect
In medicine, a side effect is an effect, whether therapeutic or adverse, that is secondary to the one intended; although the term is predominantly employed to describe adverse effects, it can also apply to beneficial, but unintended, consequences of the use of a drug. Developing drugs is a complicated process, because no two people are exactly the same, so even drugs that have virtually no side effects, might be difficult for some people. Also, it is difficult to make a drug that targets one part of the body but that does not affect other parts, the fact that increases the risk of side effects in the untargeted parts. Occasionally, drugs are prescribed or procedures performed specifically for their side effects; in that case, said side effect ceases to be a side effect and is now an intended effect. For instance, X-rays were historically (and are currently) used as an imaging technique; the discovery of their oncolytic capability led to their employ in radiotherapy (ablation of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Prostate-specific Antigen
Prostate-specific antigen (PSA), also known as gamma-seminoprotein or kallikrein-3 (KLK3), P-30 antigen, is a glycoprotein enzyme encoded in humans by the ''KLK3'' gene. PSA is a member of the kallikrein-related peptidase family and is secreted by the epithelial cells of the prostate gland. PSA is produced for the ejaculate, where it liquefies semen in the seminal coagulum and allows sperm to swim freely. It is also believed to be instrumental in dissolving cervical mucus, allowing the entry of sperm into the uterus. PSA is present in small quantities in the serum of men with healthy prostates, but is often elevated in the presence of prostate cancer or other prostate disorders. PSA is not uniquely an indicator of prostate cancer, but may also detect prostatitis or benign prostatic hyperplasia. Medical uses Prostate cancer Screening Clinical practice guidelines for prostate cancer screening vary and are controversial, in part due to uncertainty as to whether the benefi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Prostate Gland
The prostate is both an accessory gland of the male reproductive system and a muscle-driven mechanical switch between urination and ejaculation. It is found only in some mammals. It differs between species anatomically, chemically, and physiologically. Anatomically, the prostate is found below the bladder, with the urethra passing through it. It is described in gross anatomy as consisting of lobes and in microanatomy by zone. It is surrounded by an elastic, fibromuscular capsule and contains glandular tissue as well as connective tissue. The prostate glands produce and contain fluid that forms part of semen, the substance emitted during ejaculation as part of the male sexual response. This prostatic fluid is slightly alkaline, milky or white in appearance. The alkalinity of semen helps neutralize the acidity of the vaginal tract, prolonging the lifespan of sperm. The prostatic fluid is expelled in the first part of ejaculate, together with most of the sperm, because of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Castration
Castration is any action, surgical, chemical, or otherwise, by which an individual loses use of the testicles: the male gonad. Surgical castration is bilateral orchiectomy (excision of both testicles), while chemical castration uses pharmaceutical drugs to deactivate the testes. Castration causes sterilization (preventing the castrated person or animal from reproducing); it also greatly reduces the production of hormones, such as testosterone and estrogen. Surgical castration in animals is often called neutering. The term ''castration'' is sometimes also used to refer to the removal of the ovaries in the female, otherwise known as an oophorectomy, or the removal of internal testes, otherwise known as gonadectomy. The equivalent of castration for female animals is spaying. Estrogen levels drop following oophorectomy, and long-term effects of the reduction of sex hormones are significant throughout the body. Castration of animals is intended to favor a desired de ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Testosterone
Testosterone is the primary sex hormone and anabolic steroid in males. In humans, testosterone plays a key role in the development of male reproductive tissues such as testes and prostate, as well as promoting secondary sexual characteristics such as increased muscle and bone mass, and the growth of body hair. In addition, testosterone in both sexes is involved in health and well-being, including moods, behaviour, and in the prevention of osteoporosis. Insufficient levels of testosterone in men may lead to abnormalities including frailty and bone loss. Testosterone is a steroid from the androstane class containing a ketone and a hydroxyl group at positions three and seventeen respectively. It is biosynthesized in several steps from cholesterol and is converted in the liver to inactive metabolites. It exerts its action through binding to and activation of the androgen receptor. In humans and most other vertebrates, testosterone is secreted primarily by the testicles o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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