Keywords selective anabolic receptor mo...

selective anabolic receptor modulator
Alessio Molfino, Maria Ida Amabile, Antonella Giorgi, Massimo Monti, Vito D'Andrea, Maurizio Muscaritoli
Introduction : Cachexia is frequent in chronic diseases and especially during cancer development. Multiple definitions of cachexia have been proposed; it may be considered a multifactorial complex syndrome that presents with progressive unintentional weight loss and wasting of muscle mass and adipose tissue. Area covered : This article covers phase-I and phase-II clinical trials of investigational drugs for cancer cachexia. We performed a search on PubMed with keywords as cancer cachexia, phase-I/phase-II trial, drug, identifying articles relevant to this review...
August 2019: Expert Opinion on Investigational Drugs
Fernanda Regina Ribeiro-Santos, Geyson Galo da Silva, Igor Bassi Ferreira Petean, Maya Fernanda Manfrin Arnez, Léa Assed Bezerra da Silva, Lúcia Helena Faccioli, Francisco Wanderley Garcia Paula-Silva
OBJECTIVES: Infection, inflammation and bone resorption are closely related events in apical periodontitis development. Therefore, we sought to investigate the role of cyclooxygenase (COX) in osteoclastogenesis and bone metabolism signaling in periapical bone tissue after bacterial lipopolysaccharide (LPS) inoculation into root canals. METHODOLOGY: Seventy two C57BL/6 mice had the root canals of the first molars inoculated with a solution containing LPS from E. coli (1...
June 3, 2019: Journal of Applied Oral Science: Revista FOB
Yuichiro Ukon, Takahiro Makino, Joe Kodama, Hiroyuki Tsukazaki, Daisuke Tateiwa, Hideki Yoshikawa, Takashi Kaito
Osteoporosis is an unavoidable public health problem in an aging or aged society. Anti-resorptive agents (calcitonin, estrogen, and selective estrogen-receptor modulators, bisphosphonates, anti-receptor activator of nuclear factor κB ligand antibody along with calcium and vitamin D supplementations) and anabolic agents (parathyroid hormone and related peptide analogs, sclerostin inhibitors) have major roles in current treatment regimens and are used alone or in combination based on the pathological condition...
May 24, 2019: International Journal of Molecular Sciences
Sahar Mohsin, May Myh Baniyas, Reem Smh AlDarmaki, Kornélia Tekes, Huba Kalász, Ernest A Adeghate
Currently, 424 million people aged between 20-79 years worldwide are diabetic. More than 25% of adults aged over 65 years in North America have Type 2 diabetes mellitus (DM). Diabetes-induced osteoporosis (DM-OS) is caused by chronic hyperglycemia, advanced glycated end products and oxidative stress. The increase in the prevalence of DM-OS has prompted researchers to develop new biological therapies for the management of DM-OS. Areas covered: This review covered the current and novel biological agents used in the management of DM-OS...
May 11, 2019: Expert Opinion on Biological Therapy
Oliver Zierau, Annika Kolodziejczyk, Günter Vollmer, David Machalz, Gerhard Wolber, Detlef Thieme, Annekathrin Martina Keiler
Selective androgen receptor modulators comprise compounds that bind as ligands to the androgen receptor and possess tissue-selective activities. Ideally, they show agonistic properties in anabolic target tissues, while inducing antagonistic or only weak agonistic effects in reproductive organs. Due to their myoanabolic effects, selective androgen receptor modulators are included in the list of prohibited substances and methods of the World Anti-Doping Agency. In the current investigation, the androgenic potential of RAD-140, GSK-2881078 and GLPG0492 was comparably investigated in two different in vitro bioassays...
May 2019: Journal of Steroid Biochemistry and Molecular Biology
Yoshimi Muta, Tomoko Tanaka, Yuriko Hamaguchi, Nobuya Hamanoue, Ryoko Motonaga, Makito Tanabe, Takashi Nomiyama, Hajime Nawata, Toshihiko Yanase
We previously identified a novel selective androgen receptor modulator, S42, that does not stimulate prostate growth but has a beneficial effect on lipid metabolism. S42 also increased muscle weight of the levator ani in orchiectomized Sprague-Dawley rats. These findings prompted us to investigate whether S42 has a direct effect on cultured C2C12 myotubes. S42 significantly lowered expression levels of the skeletal muscle ubiquitin ligase (muscle atrophy-related gene), atrogin1 and Muscle RING-Finger Protein 1(MuRF1) in C2C12 myotubes, as determined by real time PCR...
March 2019: Biochemistry and Biophysics Reports
Yuehong Chen, Ronghan Liu, Aubryanna Hettinghouse, Shuya Wang, Gang Liu, Chuan-Ju Liu
BACKGROUND: Teriparatide, a 1-34 fragment of parathyroid hormone (PTH) that maintains most of the biological activities of PTH, has been employed since 2002 as an anabolic agent for osteoporotic individuals who are at high risk of fracture. The purpose of the present review is to provide a systematic summary and timely update on treatment with teriparatide for fracture prevention. METHODS: Electronic databases, including OVID MEDLINE, OVID Embase, and the Cochrane Library, were searched on February 9, 2018, to identify published systematic reviews and meta-analyses addressing treatment with teriparatide for fracture prevention, and A Measurement Tool to Assess Systematic Reviews 2 (AMSTAR 2) was used to assess the quality of included studies...
January 2019: JBJS Reviews
Robert Alexandru Vlad, Gabriel Hancu, Gabriel Cosmin Popescu, Ioana Andreea Lungu
Through doping, we understand the use by athletes of substances prohibited by the antidoping agencies in order to gain a competitive advantage. Since sport plays an important role in physical and mental education and in promoting international understanding and cooperation, the widespread use of doping products and methods has consequences not only on health of the athletes, but also upon the image of sport. Thus, doping in sports is forbidden for both ethical and medical reasons. Narcotics and analgesics, anabolic steroids, hormones, selective androgen receptor modulators are among the most frequently utilized substances...
November 2018: Advanced Pharmaceutical Bulletin
Zachary J Solomon, Jorge Rivera Mirabal, Daniel J Mazur, Taylor P Kohn, Larry I Lipshultz, Alexander W Pastuszak
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...
January 2019: Sexual Medicine Reviews
Anna L Goldman, Harrison G Pope, Shalender Bhasin
CONTEXT: The prevalence of body image disorders and anabolic-androgenic steroid (AAS) use is increasing, despite the evidence of their serious adverse health effects and despite the passage of laws regulating their sales. Here we review the evolution of the dual emerging epidemics of body image disorders and AAS use, adverse health effects of AASs, and the need for an integrated health policy and regulatory response. EVIDENCE ACQUISITION: We searched for studies published prior to June 2018...
April 1, 2019: Journal of Clinical Endocrinology and Metabolism
Anne Tournadre, Gaelle Vial, Frédéric Capel, Martin Soubrier, Yves Boirie
Sarcopenia is defined as a combination of low muscle mass with low muscle function. The term was first used to designate the loss of muscle mass and performance associated with aging. Now, recognized causes of sarcopenia also include chronic disease, a physically inactive lifestyle, loss of mobility, and malnutrition. Sarcopenia should be differentiated from cachexia, which is characterized not only by low muscle mass but also by weight loss and anorexia. Sarcopenia results from complex and interdependent pathophysiological mechanisms that include aging, physical inactivity, neuromuscular compromise, resistance to postprandial anabolism, insulin resistance, lipotoxicity, endocrine factors, oxidative stress, mitochondrial dysfunction, and inflammation...
May 2019: Joint, Bone, Spine: Revue du Rhumatisme
Robert Carrasquillo, Kevin Chu, Ranjith Ramasamy
PURPOSE OF REVIEW: Hypogonadism and the treatment of low testosterone is increasingly a subject of medical inquiry and controversy. The few treatments that are FDA-approved such as testosterone topicals, injections, and pellets create significant demand from patients for treatments with more convenient means of administration, fewer adverse effects, and the ability to maintain male fertility. Off-label drugs are in abundant use for low testosterone, including selective estrogen receptor modulators, gonadotropins, and aromatase inhibitors...
June 9, 2018: Current Urology Reports
Anastasia D Dede, Margaret Callan
Identification of patients at risk for fragility fractures is the first important step in the management of osteoporosis. Bisphosphonates have been the mainstay of treatment for decades, whereas denosumab and selective oestrogen receptor modulators are other available licensed antiresorptive drugs. Currently teriparatide is the only approved anabolic agent in Europe, while abaloparatide and romosozumab are awaiting approval and might be available in the near future. For bisphosphonates, current guidance suggests an initial treatment course of 3-5 years and more prolonged treatment should be pursued in patients with higher fracture risk...
May 2, 2018: British Journal of Hospital Medicine
J-Pablo Salvador, Ester Vila-Roca, Núria Monfort, Rosa Ventura, M-Pilar Marco
Antiestrogenic compounds such as tamoxifen, toremifen and chlomifen are used illegally by athletes to minimize physical impacts such as gynecomastia resulting from the secondary effects of anabolic androgenic steroids, used to increase athletic efficiency unlawfully. The use of these compounds is banned by the World Anti-Doping Agency (WADA) and controls are made through analytical methodologies such as HPLC-MS/MS, which do not fulfil the sample throughput requirements. Moreover, compounds such as tamoxifen are also used to treat hormone receptor-positive breast cancer (ER + )...
July 15, 2018: Journal of Pharmaceutical and Biomedical Analysis
Konstantinos Tsarouhas, Nassia Kioukia-Fougia, Petros Papalexis, Aristidis Tsatsakis, Dimitrios Kouretas, Flora Bacopoulou, Christina Tsitsimpikou
Although the use of nutritional supplements by adult athletes has been extensively studied, information on supplements consumption by adolescent athletes is still limited. The present study reports on the use of nutritional supplements contaminated with banned doping substances among 170 recreational adolescent athletes from eleven, randomly selected, gym centres, in Athens, Greece. Nutritional supplements consumption was reported by almost 60% of the study population, with proteins/amino acids and vitamins being the most popular...
May 2018: Food and Chemical Toxicology
Felicia Cosman
PURPOSE OF REVIEW: Osteoporosis guidelines do not usually provide specific recommendations regarding what medication is most appropriate for individual patients. Generic oral bisphosphonates are often considered first-line treatment for osteoporosis, but treatment duration is limited, based on potential long-term safety concerns, and there is no consensus about what to do after 5 years. There are no recommendations concerning long-term management of osteoporosis over 30 or more years of postmenopausal life...
July 2018: Current Opinion in Rheumatology
Ke-Hong Ding, Michael Cain, Michael Davis, Clare Bergson, Meghan McGee-Lawrence, Crystal Perkins, Trevor Hardigan, Xingming Shi, Qing Zhong, Jianrui Xu, Wendy B Bollag, William Hill, Mohammed Elsalanty, Monte Hunter, Maria C Isales, Patricia Lopez, Mark Hamrick, Carlos M Isales
Except for the essential amino acids (AAs), much of the focus on adequate dietary protein intake has been on total nitrogen and caloric intake rather than AA composition. Recent data, however, demonstrate that "amino-acid sensing" can occur through either intracellular or extracellular nutrient-sensing mechanisms. In particular, members of the class 3 G-protein coupled receptor family, like the calcium-sensing receptor are known to preferentially bind specific AAs, which then modulate receptor activation by calcium ions and thus potentially impact bone turnover...
October 2018: Bone
Tomofumi Yatsu, Taichi Kusakabe, Keisuke Kato, Yoshio Inouye, Kiyomitsu Nemoto, Yuichiro Kanno
Androgens are key regulators that play a critical role in the male reproductive system and have anabolic effects on bone mineral density and skeletal muscle mass. We have previously reported that YK11 is a novel selective androgen receptor modulator (SARM) and induces myogenic differentiation and selective gene regulation. In this study, we show that treatment of YK11 and dihydrotestosterone (DHT) accelerated cell proliferation and mineralization in MC3T3-E1 mouse osteoblast cells. Further, YK11-treated cells increased osteoblast specific differentiation markers, such as osteoprotegerin and osteocalcin, compared to untreated cells...
2018: Biological & Pharmaceutical Bulletin
B Gray, M Viljanto, E Menzies, L Vanhaecke
The detection of drugs in human hair samples has been performed by laboratories around the world for many years and the matrix is popular in disciplines, such as workplace drug testing. To date, however, hair has not become a routinely utilised matrix in sports drug detection. The analysis of hair samples offers several potential advantages to doping control laboratories, not least of which are the greatly extended detection window and the ease of sample collection and storage. This article describes the development, validation, and utilisation of a sensitive ultra-high performance liquid chromatography-triple quadrupole mass spectrometry (UHPLC-MS/MS) method for the detection of 50 compounds...
February 12, 2018: Drug Testing and Analysis
Megumi Morimoto, Katsuji Aikawa, Takahito Hara, Masuo Yamaoka
Cancer cachexia is a syndrome that impairs the quality of life and overall survival of patients, and thus the effectiveness of anticancer agents. There are no effective therapies for cancer cachexia due to the complexity of the syndrome, and insufficient knowledge of its pathogenesis results in difficulty establishing appropriate animal models. Previously, promising results have been obtained in clinical trials using novel agents including the ghrelin receptor agonist anamorelin, and the selective androgen receptor modulator (SARM) enobosarm to treat cachexia in patients with cancer...
December 2017: Oncology Letters
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