Description
AC262,536
Liquid: 30mg/ml – 30mlÂ
Application: Selective Androgen Receptor Modulator
CAS: 870888-46-3
Molar Mass: 278.348 g/mol
Synonyms: AC262,536
Peer-Reviewed Studies
Development of selective androgen receptor modulators (SARMs)
Abstract
The Androgen Receptor (AR), a member of the steroid hormone receptor family, plays important roles in the physiology and pathology of diverse tissues. AR ligands, which include circulating testosterone and locally synthesized dihydrotestosterone, bind to and activate the AR to elicit their effects. Ubiquitous expression of the AR, metabolism and cross reactivity with other receptors limit broad therapeutic utilization of steroidal androgens. However, the discovery of selective androgen receptor modulators (SARMs) and other tissue-selective nuclear hormone receptor modulators that activate their cognate receptors in a tissue-selective manner provides an opportunity to promote the beneficial effects of androgens and other hormones in target tissues with greatly reduced unwanted side-effects. In the last two decades, significant resources have been dedicated to the discovery and biological characterization of SARMs in an effort to harness the untapped potential of the AR. SARMs have been proposed as treatments of choice for various diseases, including muscle-wasting, breast cancer, and osteoporosis. This review provides insight into the evolution of SARMs from proof-of-concept agents to the cusp of therapeutic use in less than two decades, while covering contemporary views of their mechanisms of action and therapeutic benefits.
Abstract
Selective androgen receptor modulators (SARMs) are a class of androgen receptor ligands that bind androgen receptors and display tissue selective activation of androgenic signaling. SARMs have selective anabolic effects on muscle and bone, and were originally synthesized for treatment of muscle wasting conditions, osteoporosis, breast cancer. To date, no SARM has been clinically approved and little is known about the beneficial effects and other adverse effects on users. We examined the adverse effects and potential benefits of SARMs amongst users. We performed an internet survey assessing the demographics of users via a 32-question survey. Using reddit as a platform, we distributed the survey through various subreddits that included potential SARMs users. Out of the 520 responses, 343 participants admitted having used SARMs. Most were males (98.5%), between the ages of 18-29 (72.3%). More than 90% of users acquired SARMs via the internet and did not consult with a physician. More than half of SARMs users experienced side effects including mood swings, decreased testicular size, and acne. More than 90% of men reported increased muscle mass and were satisfied with their SARMs usage. Despite having seemingly positive effects, more than 50% of SARMs users report significant adverse effects. Chi square was the main method of statistical analysis. Future studies should focus on comprehensive reproductive evaluation of men using SARMs.
Selective Androgen Receptor Modulators: Current Knowledge and Clinical Applications
Abstract
Introduction: Selective androgen receptor modulators (SARMs) differentially bind to androgen receptors depending on each SARM’s chemical structure. As a result, SARMs result in anabolic cellular activity while avoiding many of the side effects of currently available anabolic steroids. SARMs have been studied in the treatment of breast cancer and cachexia and have also been used as performance-enhancing agents. Here, we evaluate and summarize the current literature on SARMs.
Aim:Â To present the background, mechanisms, current and potential clinical applications, as well as risks and benefits of SARMs.
Methods:Â A literature review was performed in MEDLINE using the terms selective androgen receptor modulator, hypogonadism, cachexia, breast cancer, benign prostatic hyperplasia, libido, and lean muscle mass. Both basic research and clinical studies were included.
Main outcome measure:Â To complete a review of peer-reviewed literature.
Results:Â Although there are currently no U.S. Food and Drug Agency-approved indications for SARMs, investigators are exploring the potential uses for these compounds. Basic research has focused on the pharmacokinetics and pharmacodynamics of these agents, demonstrating good availability with a paucity of drug interactions. Early clinical studies have demonstrated potential uses for SARMs in the treatment of cancer-related cachexia, benign prostatic hyperplasia (BPH), hypogonadism, and breast cancer, with positive results.
Conclusion:Â SARMs have numerous possible clinical applications, with promise for the safe use in the treatment of cachexia, BPH, hypogonadism, breast cancer, and prostate cancer. Solomon ZJ, Mirabal JR, Mazur DJ, et al. Selective Androgen Receptor Modulators: Current Knowledge and Clinical Applications. Sex Med Rev 2019;7:84-94.
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