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Andarine
Andarine (developmental code names GTx-007, S-4) is a selective androgen receptor modulator (SARM) which was developed by GTX, Inc for the treatment of conditions such as muscle wasting, osteoporosis, and benign prostatic hyperplasia (BPH), using the nonsteroidal antiandrogen bicalutamide as a lead compound. Development of andarine for all indications has been discontinued, in favor of the structurally related and improved compound enobosarm (ostarine; GTx-024; S-22). Andarine is an orally active partial agonist of the androgen receptor (AR). In intact male rats, 0.5 mg andarine daily was shown to reduce prostate weight to 79.4%, and non-significantly increased levator ani muscle weight. In castrated male rats, this dose restored only 32.5% prostate weight, but 101% levator ani muscle weight This suggests that andarine is able to competitively block binding of dihydrotestosterone to its receptor targets in the prostate gland, but its partial agonist actions at the androgen re ...
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Enobosarm
Enobosarm, also formerly known as ostarine and by the developmental code names GTx-024, MK-2866, and S-22, is a selective androgen receptor modulator (SARM) which is under development for the treatment of hormone sensitive cancer, androgen receptor-positive breast cancer in women and for improvement of body composition (e.g., prevention of muscle loss) in people taking GLP-1 receptor agonists like semaglutide. It was also under development for a variety of other indications, including treatment of cachexia, Duchenne muscular dystrophy, muscle atrophy or sarcopenia, and stress incontinence, stress urinary incontinence, but development for all other uses has been discontinued. Enobosarm was evaluated for the treatment of muscle wasting related to cancer in Phases of clinical research#Phase III, late-stage clinical trials, and the drug improved lean body mass in these trials, but it was not effective in improving muscle strength. As a result, enobosarm was not approved and developme ...
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Bicalutamide
Bicalutamide, sold under the brand name Casodex among others, is an antiandrogen medication that is primarily used to treat prostate cancer. It is typically used together with a gonadotropin-releasing hormone (GnRH) analogue or surgical removal of the testicles to treat metastatic prostate cancer (mPC). To a lesser extent, it is used at high doses for locally advanced prostate cancer (LAPC) as a monotherapy without castration. Bicalutamide was also previously used as monotherapy to treat localized prostate cancer (LPC), but authorization for this use was withdrawn following unfavorable trial findings. Besides prostate cancer, bicalutamide is limitedly used in the treatment of excessive hair growth and scalp hair loss in women, as a puberty blocker and component of feminizing hormone therapy for transgender girls and women, to treat gonadotropin-independent early puberty in boys, and to prevent overly long-lasting erections in men. It is taken by mouth. Common side ...
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Selective Androgen Receptor Modulator
Selective androgen receptor modulators (SARMs) are a class of drugs that tissue selectivity, selectively activate the androgen receptor in specific tissue (biology), tissues, promoting muscle and bone growth while having less effect on male reproductive system, male reproductive tissues like the prostate gland. Non-selective steroidal drugs, called anabolic androgenic steroids (AAS), have been used for various medical purposes, but their side effects limit their use. In 1998, researchers discovered a new class of non-steroidal compounds, the SARMs. These compounds selectively stimulate the androgen receptor, offering potent effects on bone and muscle to increase bone density and lean body mass while having minimal impact on reproductive tissues. SARMs have been investigated in human studies for the treatment of osteoporosis, cachexia (wasting syndrome), benign prostatic hyperplasia, stress urinary incontinence, and breast cancer. , there are no SARMs which have been approved b ...
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Androgen Receptor
The androgen receptor (AR), also known as NR3C4 (nuclear receptor subfamily 3, group C, member 4), is a type of nuclear receptor that is activated by binding any of the androgenic hormones, including testosterone and dihydrotestosterone, in the cytoplasm and then translocating into the Cell nucleus, nucleus. The androgen receptor is most closely related to the progesterone receptor, and progestins in higher dosages can block the androgen receptor. The main function of the androgen receptor is as a DNA-binding protein, DNA-binding transcription factor that Gene expression regulation, regulates gene expression; however, the androgen receptor has other functions as well. Androgen-regulated genes are critical for the development and maintenance of the male sexual phenotype. Function Effect on development In some cell types, testosterone interacts directly with androgen receptors, whereas, in others, testosterone is converted by 5-alpha reductase, 5-alpha-reductase to dihydrot ...
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Gtx Inc
GTx, Inc. was a pharmaceutical company working on drugs in the selective estrogen receptor modulator (SERM) and selective androgen receptor modulator (SARM) classes. Its drugs in development included 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 Duane D Miller and James T Dalton, who later joined the company and served as Chief Scientific Officer. The company held its IPO in February 2004. In 2006 GTx signed a partnership with Ipsen to develop toremifene, a selective estrogen receptor modulator to prevent prostate cancer and to prevent bone loss in men with prostate canc ...
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Cachexia
Cachexia () is a syndrome that happens when people have certain illnesses, causing muscle loss that cannot be fully reversed with improved nutrition. It is most common in diseases like cancer, Heart failure, congestive heart failure, chronic obstructive pulmonary disease, chronic kidney disease, and AIDS. These conditions change how the body handles inflammation, metabolism, and brain signaling, leading to muscle loss and other harmful changes to body composition over time. Unlike weight loss from not eating enough, cachexia mainly affects muscle and can happen with or without fat loss. Diagnosis of cachexia is difficult because there are no clear guidelines, and its occurrence varies from one affected person to the next. Like malnutrition, cachexia can lead to worse health outcomes and lower quality of life. Definition Cachexia is hard to define because it often happens alongside malnutrition and sarcopenia. Since there are no clear rules separating these conditions, experts ...
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Phenol Ethers
Phenol (also known as carbolic acid, phenolic acid, or benzenol) is an aromatic organic compound with the molecular formula . It is a white crystalline solid that is volatile and can catch fire. The molecule consists of a phenyl group () bonded to a hydroxy group (). Mildly acidic, it requires careful handling because it can cause chemical burns. It is acutely toxic and is considered a health hazard. Phenol was first extracted from coal tar, but today is produced on a large scale (about 7 million tonnes a year) from petroleum-derived feedstocks. It is an important industrial commodity as a precursor to many materials and useful compounds, and is a liquid when manufactured. It is primarily used to synthesize plastics and related materials. Phenol and its chemical derivatives are essential for production of polycarbonates, epoxies, explosives such as picric acid, Bakelite, nylon, detergents, herbicides such as phenoxy herbicides, and numerous pharmaceutical drugs. ...
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Abandoned Drugs
Abandon, abandoned, or abandonment may refer to: Common uses * Abandonment (emotional), a subjective emotional state in which people feel undesired, left behind, insecure, or discarded * Abandonment (legal), a legal term regarding property ** Child abandonment, the extralegal abandonment of children ** Lost, mislaid, and abandoned property, legal status of property after abandonment and rediscovery * Abandonment (mysticism) Art, entertainment, and media Film * ''Abandon'' (film), a 2002 film starring Katie Holmes * ''Abandoned'' (1949 film), starring Dennis O'Keefe * ''Abandoned'' (1955 film), the English language title of the Italian war film ''Gli Sbandati'' * ''Abandoned'' (2001 film), a Hungarian film * ''Abandoned'' (2010 film), starring Brittany Murphy * ''Abandoned'' (2015 film), a television movie about the shipwreck of the ''Rose-Noëlle'' in 1989 * ''Abandoned'' (2022 film), starring Emma Roberts * ''The Abandoned'' (1945 film), a 1945 Mexican film * ''The Aba ...
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GTx-027
GTx-027 is a selective androgen receptor modulator (SARM) which was under development for or of potential interest in the treatment of breast cancer and stress urinary incontinence (SUI) but was never marketed. It is taken by mouth. Description The drug is a nonsteroidal androgen receptor (AR) modulator with mixed agonistic (androgenic) and antagonistic (antiandrogenic) effects. It has been found to reduce the growth of androgen receptor-expressing MDA-MB-231 breast cancer cells ''in vitro''. In addition, it has been found to increase pelvic floor muscle weight in ovariectomized female rodents. The drug has been found to increase body weight, lean body mass, and muscle strength in animals as well. In terms of chemical structure, GTx-027 is a nonsteroidal arylpropionamide SARM and is an analogue of enobosarm (ostarine; GTx-024). GTx-027 was first described in the scientific literature by 2013. It is said to have either not passed preclinical research or to have reached phas ...
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Acetothiolutamide
Acetothiolutamide is a selective androgen receptor modulator (SARM) derived from the nonsteroidal antiandrogen bicalutamide that was described in 2002 and was one of the first SARMs to be discovered and developed. It is a high-affinity, selective ligand of the androgen receptor (AR) (Ki = 2.1–4.9 nM), where it acts as a full agonist ''in vitro'', and has ''in vitro'' potency comparable to that of testosterone. However, ''in vivo'', acetothiolutamide displayed overall negligible androgenic effects, though significant (albeit very low) anabolic effects were observed at high doses. In addition, notable antiandrogen effects were observed in castrated male rats treated with testosterone propionate. The discrepancy between the ''in vitro'' and ''in vivo'' actions of acetothiolutamide was determined to be related to rapid plasma clearance and extensive hepatic metabolism into a variety of metabolites with differing pharmacological activity, including AR partial agonism and antagonism ...
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Visual Disturbances
A vision disorder is an impairment of the sense of vision. Vision disorder is not the same as an eye disease. Although many vision disorders do have their immediate cause in the eye, there are many other causes that may occur at other locations in the optic pathway. Causes There are many eye conditions that can lead to vision disorder. Some of which are as follows: *Age-Related Macular Degeneration (ARMD): ARMD is a retinal degeneration disease specifically associated with macula blood vessels, which can result in central vision impairment. It is strongly linked to advancing age, as well as European ancestry. * Bulging eyes: where the eye (one or both) protrudes or distends out of its orbit. Left untreated, bulging eyes may lead to eye dryness, pain and vision loss * Cytomegalovirus (CMV) Retinitis: This is an inflammation of the retina caused by infection, which can result in blindness. It occurs in people experiencing suppressed immune systems, most commonly by Acquired Immu ...
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