madman
Super Moderator
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: To present the background, mechanisms, current and potential clinical applications, as well as risks and benefits of SARMs.
Methods: 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: To complete a review of peer-reviewed literature.
Results: 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: SARMs have numerous possible clinical applications, with promise for safe use in the treatment of cachexia, BPH, hypogonadism, breast cancer, and prostate cancer.
CONCLUSION
The AR is a complex signaling apparatus with important effects on tissue development, growth, and maintenance. Although steroid hormones have valuable clinical applications, their widespread activation of AR receptors gives rise to treatment-limiting side effects. Like the SERMs before them, SARMs and their tissue selectivity demonstrate the potential to revolutionize the treatment of many debilitating diseases. Depending on their chemical structure, SARMs can act as agonists, antagonists, partial agonists, or partial antagonists of the AR within different tissues. Results from recent clinical trials have shown mixed but promising results and basic research continues to raise the idea that SARMs could be powerful and effective treatments in a wide variety of conditions, from Alzheimer’s disease and osteoporosis to male contraception and BPH.
Continued investigation and development of these agents is called for given their novel mechanisms of action and potential to address and complement conditions with a lack of effective therapies or therapies with unacceptable side effects. Additionally, to date, SARMs have consistently been shown to be well tolerated, easily administered via an oral route, and overall lacking in significant drug interactions that can only further increase their future applicability. Like the SERMs before them, the next decades could herald the approval and widespread use of SARMs for an array of indications. However, further studies are currently needed to determine the safety and efficacy of these medications before they are approved for clinical use.
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: To present the background, mechanisms, current and potential clinical applications, as well as risks and benefits of SARMs.
Methods: 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: To complete a review of peer-reviewed literature.
Results: 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: SARMs have numerous possible clinical applications, with promise for safe use in the treatment of cachexia, BPH, hypogonadism, breast cancer, and prostate cancer.
CONCLUSION
The AR is a complex signaling apparatus with important effects on tissue development, growth, and maintenance. Although steroid hormones have valuable clinical applications, their widespread activation of AR receptors gives rise to treatment-limiting side effects. Like the SERMs before them, SARMs and their tissue selectivity demonstrate the potential to revolutionize the treatment of many debilitating diseases. Depending on their chemical structure, SARMs can act as agonists, antagonists, partial agonists, or partial antagonists of the AR within different tissues. Results from recent clinical trials have shown mixed but promising results and basic research continues to raise the idea that SARMs could be powerful and effective treatments in a wide variety of conditions, from Alzheimer’s disease and osteoporosis to male contraception and BPH.
Continued investigation and development of these agents is called for given their novel mechanisms of action and potential to address and complement conditions with a lack of effective therapies or therapies with unacceptable side effects. Additionally, to date, SARMs have consistently been shown to be well tolerated, easily administered via an oral route, and overall lacking in significant drug interactions that can only further increase their future applicability. Like the SERMs before them, the next decades could herald the approval and widespread use of SARMs for an array of indications. However, further studies are currently needed to determine the safety and efficacy of these medications before they are approved for clinical use.
