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Heterocyclic Drugs from Plants
Published in Rohit Dutt, Anil K. Sharma, Raj K. Keservani, Vandana Garg, Promising Drug Molecules of Natural Origin, 2020
Debasish Bandyopadhyay, Valeria Garcia, Felipe Gonzalez
Current treatments for osteoporosis include testosterone and dihydrotestosterone; a steroidal approach to treat osteoporosis also known as hormone replacement therapy (HRT). Even though these treatments are beneficial to increasing bone density and muscle mass although some serious and potentially fatal side effects (hepatotoxicity) associated with these drugs (Sechi et al., 2004). To reduce such aftereffects of the steroidal approach, non-steroidal approach of treating osteoporosis known as non-steroidal selective androgen receptor modulator (SARM’s) is necessary (Unwalla et al., 2017). Pyrrole derivatives might be fitted in this role (Micheli et al., 2003). A cyanopyrrole was studied and showed decent activity in promoting muscle growth with minimal prostate toxicity than other steroidal treatments.
Supplements
Published in David Lightsey, The Myths about Nutrition Science, 2019
“We are extremely concerned about unscrupulous companies marketing body-building products with potentially dangerous ingredients. Bodybuilding products that contain selective androgen receptor modulators, or SARMs, have not been approved by the FDA and are associated with serious safety concerns, including potential to increase the risk of heart attack or stroke and life-threatening reactions like liver damage,” said Donald D. Ashley, J.D., director of the Office of Compliance in the FDA’s Center for Drug Evaluation and Research. “We will continue to take action against companies marketing these products to protect the public health.”
Sarcopenia and Androgens: A Link Between Pathology and Treatment
Published in Chad Cox, Clinical Nutrition and Aging, 2017
Carla Basualto-AlarcÓN, Diego Varela, Javier Duran, Rodrigo Maass, Manuel Estrada
Supplementation with selective androgen-receptor modulators (SARMs) has emerged as a means of treating muscle and bone disorders, mainly because of the specificity of SARM action and the relatively few side effects of SARM treatment. Research using experimental models has demonstrated that administration of SARM S-4 exerts potent anabolic effects on skeletal muscle and bone and only minimal effects on the prostate (97). In a recent randomized, double-blind, placebo-controlled study of 170 women aged ≥65 with sarcopenia and moderate physical dysfunction found that 6 months of treatment with MK-0773 significantly improved physical performance measures (98). GTx-024 (enobosarm), a non-steroidal SARM that exerts tissue-selective anabolic effects in muscle and bone while sparing other androgenic tissue related to hair growth in women and prostate effects in men, has demonstrated promising pharmacologic effects in preclinical studies and favorable safety and pharmacokinetic profiles in phase I investigations. Thus GTx-024 supplementation resulted in dose-dependent improvement in total lean body mass and physical function and was well tolerated (99). Treatment with one or more of the numerous other SARMs currently under study may emerge as therapeutic alternatives to androgen agonist therapy. The intense research into pharmacological modulation of androgens and androgen intracellular signaling pathways may lead to the development of effective approaches to restoring and preventing the muscle loss observed in sarcopenia.
Social media may cause emergent SARMs abuse by athletes: a content quality analysis of the most popular YouTube videos
Published in The Physician and Sportsmedicine, 2023
Nikhil Vasireddi, Henrik A. Hahamyan, Yash Kumar, Mitchell K. Ng, James E. Voos, Jacob G. Calcei
Selective Androgen Receptor Modulators (SARMs) are a class of performance enhancing drugs (PEDs) that act as androgen receptor ligands that achieve tissue-selective activation of androgenic signaling. The non-steroidal forms of SARMs were discovered in the late 1990s, originally demonstrating potential to treat muscle wasting in patients with cancer, osteoporosis, advanced age, and other chronic illnesses [1]. The potential to slow the functional decline of older individuals using targeted androgen signaling has led to the development of non-steroidal SARMs from nearly all major pharmaceutical companies [2]. Clinical trials, in vivo, and in vitro studies suggest that SARMs can build muscle mass, much like androgenic-anabolic steroids [3–7]. Athletes and social media influences use this literature to justify SARMs use and promote SARMs on social media. However, SARMs may cause adverse effects, such as liver injury and acute myocarditis, and SARMs abuse should be recognized as a substance use disorder [8–14].
Anabolic-androgenic steroids: procurement and administration practices of doping athletes
Published in The Physician and Sportsmedicine, 2019
Julius Fink, Brad Jon Schoenfeld, Anthony C. Hackney, Masahito Matsumoto, Takahiro Maekawa, Koichi Nakazato, Shigeo Horie
Online sellers also are now offering selective androgen receptor modulators (SARMs), which are believed to have similar effects as AAS without the same degree of negative side effects due to their discriminating targeting of receptors. However, steroid-like side effects such as liver toxicity, increased potential of heart attack and stroke, infertility and mental health problems may also occur with the usage of SARMs. The term ‘selective’ in SARM means they preferentially bind to androgen receptors in muscle tissue without triggering androgenic effects in other tissues such as the prostate [13–15]. The popularity of SARMs has also increased among athletes seeking anabolic effects while minimizing androgenic side effects. The legal status of SARMs allows many websites to legally sell these products as ‘research products not for human consumption’. Popular SARMs include Andarine, Accadine (AC-262,536), Cardarine, Endurobol (GW501516), Mk-677 (Ibutamoren), Ligandrol (LGD-4033), Ostarine (Mk-2866), Trestolone (RAD-140), S-23, Stenabolic (SR-9009) and YK-11. Even though not approved by the Food and Drug Administration (FDA), many individuals on the black market take advantage of the fact that SARMs are not yet listed as banned substances and can therefore be sold as research drugs, despite being banned by the World Anti-Doping Agency. Athletes who do not want to procure AAS via illegal routes might buy SARMs without realizing the long-term side effects of these drugs are still under investigation, even though similar side effects to AAS have been observed.
New and developing pharmacotherapy for osteoporosis in men
Published in Expert Opinion on Pharmacotherapy, 2018
Luigi Gennari, John P. Bilezikian
Likewise, the use of selective androgen receptor modulators (SARMs) that activate androgen receptors in a tissue-selective manner may theoretically provide an opportunity to promote the beneficial effects of androgens on bone and muscle with greatly reduced unwanted side effects at the prostate, heart, and the liver. Since the discovery of the first SARM in 1990s, several SARM scaffolds with diverse biological functions have emerged [111], including some compounds with myo- and osteo-anabolic activity in various preclinical models. However, most, if not all, of these compounds failed to advance to clinical development either due to toxicity or lack of efficacy [112,113]. Moreover, SARMs should be theoretically less effective than testosterone on bone if they cannot be converted into estrogen and act on estrogen receptors as testosterone does.