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RAD140 is an investigational selective androgen receptor modulator (SARM) that is developed by Radius Health, Inc. for use in androgen replacement therapy. It was licensed to Ellipses Pharmaceuticals in 2020. Some of the potential benefits under investigation are for the treatment of conditions such as muscle wasting and bone loss. Clinical trials The first-in-human study was initiated in October of 2017 and completed in September 2020 in postmenopausal women with breast cancer. In early 2020 a single case report of drug-induced liver injury following use of RAD 140 was published. Animal studies RAD 140 appears to be safer than testosterone replacement therapy (TRT) in rats. RAD 140 slightly increased lean muscle mass when used in primates, by targeting androgen receptors in skeletal tissue. See also * AC-262,356 * BMS-564,929 * Enobosarm * LGD-2226 * LGD-4033 * S-23 * S-40503 S-40503 is an investigational selective androgen receptor modulator (SARM) developed ...
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Selective Androgen Receptor Modulator
Selective Androgen Receptor Modulators or SARMs are a class of androgen receptor ligands that maintain some of the desirable effects of androgens, such as preventing osteoporosis and muscle loss while reducing risks of developing prostate cancer. In the late 1990s, the first nonsteroidal SARM, an analog of bicalutamide, was discovered. They are intended to have the same kind of effects as androgenic drugs, such as anabolic-androgenic steroids, but be more selective in their action. At present, there are no SARMs which have been approved for therapeutic use by the U.S. Food and Drug Administration. Comparison to testosterone As previously mentioned, the purpose of research in relation to SARMs is to replace testosterone supplementation in disease treatment with selective androgen receptor molecules. This is due to the fact that testosterone supplementation can have adverse effects on patients, which are detailed on the testosterone page. Thinking of testosterone as a model mole ...
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Enobosarm
Enobosarm, also known as ostarine or MK-2866, is an investigational selective androgen receptor modulator (SARM) developed by GTx, Inc. for the treatment of conditions such as muscle wasting and osteoporosis, formerly under development by Merck & Company. Chemistry According to a 2009 paper authored by GTx, "Readers are cautioned to note that the name ostarine is often mistakenly linked to the chemical structure of -4 which is also known as andarine. The chemical structure of ostarine has not been publicly disclosed." A 2009 review stated "Recently, GTx disclosed that compound 5 had advanced into clinical trials. The patent application described detailed data in an initial proof-of-concept Phase IIa clinical trial. It is not explicitly stated that compound 5 is Ostarine (MK-2866). The first quoted sentence is cited tPublished PCT application WO2008127717/ref> As of 2012, the mechanism of action of Enobosarm is still being debated and requires further investigation. History ...
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Designer Drugs
A designer drug is a structural or functional analog of a controlled substance that has been designed to mimic the pharmacological effects of the original drug, while avoiding classification as illegal and/or detection in standard drug tests. Designer drugs include psychoactive substances that have been designated by the European Union as new psychoactive substances (NPS) as well as analogs of performance-enhancing drugs such as designer steroids. Some of these were originally synthesized by academic or industrial researchers in an effort to discover more potent derivatives with fewer side effects, and shorter duration (and possibly also because it is easier to apply for patents for new molecules) and were later co-opted for recreational use. Other designer drugs were prepared for the first time in clandestine laboratories. Because the efficacy and safety of these substances have not been thoroughly evaluated in animal and human trials, the use of some of these drugs may result i ...
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Chloroarenes
In organic chemistry, an aryl halide (also known as haloarene) is an aromatic compound in which one or more hydrogen atoms, directly bonded to an aromatic ring are replaced by a halide. The haloarene are different from haloalkanes because they exhibit many differences in methods of preparation and properties. The most important members are the aryl chlorides, but the class of compounds is so broad that there are many derivatives and applications. Preparation The two main preparatory routes to aryl halides are direct halogenation and via diazonium salts. Direct halogenation In the Friedel-Crafts halogenation, Lewis acids serve as catalysts. Many metal chlorides are used, examples include iron(III) chloride or aluminium chloride. The most important aryl halide, chlorobenzene is produced by this route. Monochlorination of benzene is always accompanied by formation of the dichlorobenzene derivatives. Arenes with electron donating groups react with halogens even in the absence of ...
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S-40503
S-40503 is an investigational selective androgen receptor modulator (SARM) developed by the Japanese company Kaken Pharmaceuticals, which was developed for the treatment of osteoporosis. SARMs are a new class of drugs which produce tissue-specific anabolic effects in some tissues such as muscle and bone, but without stimulating androgen receptors in other tissues such as in the prostate gland, thus avoiding side effects such as benign prostatic hypertrophy which can occur following treatment with unselective androgens like testosterone or anabolic steroids. S-40503 is a SARM that shows good functional selectivity for bone tissue, and has relatively little effect on muscle mass and no observable effect on the prostate gland. In animal studies it was shown to increase both bone mineral density and biomechanical strength of femoral cortical bone, and at low doses showed anabolic effects only on bone tissue, while at higher doses both bone and muscle growth were affected, yet pros ...
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S-23 (drug)
S-23 is an investigational selective androgen receptor modulator (SARM) developed by Gtx inc, GTX, Inc as a potential male contraceptive, male hormonal contraceptive. It binds to the androgen receptor more strongly than older drugs such as andarine with a Dissociation constant#Protein-ligand binding, Ki of 1.7 nM, and in animal studies it showed both a good ratio of anabolic to androgenic effects, and dose-dependent suppression of spermatogenesis with spontaneous recovery after cessation of treatment. References

Anilides Tertiary alcohols Chloroarenes Fluoroarenes Nitriles Phenol ethers Selective androgen receptor modulators Trifluoromethyl compounds {{genito-urinary-drug-stub ...
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LGD-4033
Ligandrol (VK5211, LGD-4033) is a novel nonsteroidal oral selective androgen receptor modulator (SARM) for treatment of conditions such as muscle wasting and osteoporosis, discovered by Ligand Pharmaceuticals and under development by Viking Therapeutics. Ligandrol has been found in World Anti-Doping Agency (WADA) samples and in racehorses too. Like anabolic steroids, it can stimulate muscle growth. "SARMs have shown superior side effect profiles compared with anabolic steroids, which arguably makes them attractive for use by individuals seeking an unfair advantage over their competitors". WADA control At least since June 2015, ligandrol has been available via the internet. In that month, German scientists proposed a new test to detect its metabolites present in human urine, and suggested an expansion of the WADA regime. Misbranded as dietary supplement On 23 October 2017, a nutritional supplement company in Missouri called Infantry Labs was warned by the FDA that the distributio ...
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LGD-2226
LGD-2226 is an investigational selective androgen receptor modulator (SARM), which is being developed for treatment of muscle wasting and osteoporosis. LGD-2226 is an orally active, potent and selective agonist for androgen receptors which was shown to have anabolic effects in both muscle and bone tissue, but with considerably less effects on prostate weight and luteinizing hormone levels than testosterone. Selective androgen receptor modulators may also be used by athletes to assist in training and increase physical stamina and fitness, potentially producing effects similar to anabolic steroids but with significantly less side effects. For this reason, SARMs have already been banned by the World Anti-Doping Agency The World Anti-Doping Agency (WADA; french: Agence mondiale antidopage, AMA) is a foundation initiated by the International Olympic Committee based in Canada to promote, coordinate, and monitor the fight against drugs in sports. The agency's key ... since Janu ...
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BMS-564,929
BMS-564,929 is an investigational selective androgen receptor modulator (SARM) which is being developed by Bristol-Myers Squibb for treatment of the symptoms of age-related decline in androgen levels in men ("andropause"). These symptoms may include Depression (mood), depression, loss of muscle mass and Physical strength, strength, reduction in libido and osteoporosis. Treatment with exogenous testosterone (medication), testosterone is effective in counteracting these symptoms but is associated with a range of side effects, the most serious of which is enlargement of the prostate gland, which can lead to benign prostatic hypertrophy and even prostate cancer. This means there is a clinical need for selective androgen receptor modulators, which produce anabolic effects in some tissues such as muscle and bone, but without stimulating androgen receptors in the prostate. BMS-564,929 is one such compound currently in early human clinical trials, which is an orally active, potent and sel ...
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Androgen Replacement Therapy
Androgen replacement therapy (ART), often referred to as testosterone replacement therapy (TRT) or hormone replacement therapy (HRT), is a form of hormone therapy in which androgens, often testosterone, are supplemented or replaced exogenously. ART is often prescribed to counter the effects of male hypogonadism. It typically involves the administration of testosterone through injections, skin creams, patches, gels, pills, or subcutaneous pellets. ART is also prescribed to lessen the effects or delay the onset of normal male aging. However, this is controversial and is the subject of ongoing clinical trials. As men enter middle age they may notice changes caused by a relative decline in testosterone: fewer erections, fatigue, thinning skin, declining muscle mass and strength, and/or more body fat. Dissatisfaction with these changes causes some middle age men to seek ART. Androgen deficiencies in women have also, as of 2001, been recognized as a medical disorder that can be treat ...
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AC-262,356
AC-262536 is a drug developed by Acadia Pharmaceuticals which acts as a selective androgen receptor modulator (SARM). Chemically it possesses endo-exo isomerism, with the endo form being the active form. It acts as a partial agonist for the androgen receptor with a Ki of 5nM, and no significant affinity for any other receptors tested. In animal studies it produced a maximal effect of around 66% of the anabolic action of testosterone, but only around 27% of its potency as an androgen. See also * ACP-105 * Enobosarm * JNJ-28330835 * Ligandrol Ligandrol (VK5211, LGD-4033) is a novel nonsteroidal oral selective androgen receptor modulator (SARM) for treatment of conditions such as muscle wasting and osteoporosis, discovered by Ligand Pharmaceuticals and under development by Viking T ... References Secondary alcohols Naphthalenes Nitriles Selective androgen receptor modulators Tropanes {{genito-urinary-drug-stub ...
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Drug-induced Liver Injury
Hepatotoxicity (from ''hepatic toxicity'') implies chemical-driven liver damage. Drug-induced liver injury is a cause of acute and chronic liver disease caused specifically by medications and the most common reason for a drug to be withdrawn from the market after approval. The liver plays a central role in transforming and clearing chemicals and is susceptible to the toxicity from these agents. Certain medicinal agents, when taken in overdoses (e.g. paracetamol) and sometimes even when introduced within therapeutic ranges (e.g. halothane), may injure the organ. Other chemical agents, such as those used in laboratories and industries, natural chemicals (e.g., microcystins), and herbal remedies (two prominent examples being kava, mechanism unknown, and comfrey, through its pyrrolizidine alkaloid content) can also induce hepatotoxicity. Chemicals that cause liver injury are called hepatotoxins. More than 900 drugs have been implicated in causing liver injury (see LiverTox, externa ...
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