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D B Hoffmann, M Komrakova, S Pflug, M von Oertzen, D Saul, L Weiser, T A Walde, M Wassmann, A F Schilling, W Lehmann, S Sehmisch
Selective androgen receptor modulators (SARMs) have shown beneficial effects on muscle wasting, general physical function and bone properties in male mammals. However, data on the effects of SARMs in postmenopausal osteoporotic bone are scarce. We evaluated the effects of the SARM drug ostarine on postmenopausal osteoporotic bone in a rat osteoporosis model. Ovariectomy was performed on 46 of 56 3-month-old female Sprague-Dawley rats. Eight weeks after ovariectomy, ostarine was orally administered daily for 5 weeks in dosages of 0...
May 21, 2018: Journal of Bone and Mineral Metabolism
Ryan M Van Wagoner, Amy Eichner, Shalender Bhasin, Patricia A Deuster, Daniel Eichner
Importance: Recent reports have described the increasing use of nonsteroidal selective androgen receptor modulators, which have not been approved by the US Food and Drug Administration (FDA), to enhance appearance and performance. The composition and purity of such products is not known. Objective: To determine the chemical identity and the amounts of ingredients in dietary supplements and products marketed and sold through the internet as selective androgen receptor modulators and compare the analyzed contents with product labels...
November 28, 2017: JAMA: the Journal of the American Medical Association
Mario Thevis, Wilhelm Schänzer
The class of selective androgen receptor modulators (SARMs) has been the subject of intense and dedicated clinical research over the past two decades. Potential therapeutic applications of SARMs are manifold and focus particularly on the treatment of conditions manifesting in muscle loss such as general sarcopenia, cancer-associated cachexia, muscular dystrophy, etc. Consequently, based on the substantial muscle- and bone-anabolic properties of SARMs, these agents constitute substances with significant potential for misuse in sport and have therefore been added to the Word Anti-Doping Agency's (WADA's) Prohibited List in 2008...
March 15, 2018: Molecular and Cellular Endocrinology
Annelie Hansson, Heather Knych, Scott Stanley, Mario Thevis, Ulf Bondesson, Mikael Hedeland
RATIONALE: Selective androgen receptor modulators (SARMs) are prohibited in sports due to their performance enhancing ability. It is important to investigate the metabolism to determine appropriate targets for doping control. This is the first study where the equine metabolites of SARMs S1, S4 (Andarine) and S22 (Ostarine) have been studied in plasma. METHODS: Each SARM was administered to three horses as an intravenous bolus dose and plasma samples were collected...
April 15, 2016: Rapid Communications in Mass Spectrometry: RCM
James T Dalton, Ryan P Taylor, Michael L Mohler, Mitchell S Steiner
PURPOSE OF REVIEW: This review highlights selective androgen receptor modulators (SARMs) as emerging agents in late-stage clinical development for the prevention and treatment of muscle wasting associated with cancer. RECENT FINDINGS: Muscle wasting, including a loss of skeletal muscle, is a cancer-related symptom that begins early in the progression of cancer and affects a patient's quality of life, ability to tolerate chemotherapy, and survival. SARMs increase muscle mass and improve physical function in healthy and diseased individuals, and potentially may provide a new therapy for muscle wasting and cancer cachexia...
December 2013: Current Opinion in Supportive and Palliative Care
Eva de Rijke, Martien L Essers, Jeroen C W Rijk, Mario Thevis, Toine F H Bovee, Leendert A van Ginkel, Saskia S Sterk
For future targeted screening in National Residue Control Programmes, the metabolism of seven SARMs, from the arylpropionamide and the quinolinone classes, was studied in vitro using S9 bovine liver enzymes. Metabolites were detected and identified with ultra-performance liquid chromatography (UPLC) coupled to time-of-flight mass spectrometry (ToF-MS) and triple quadrupole mass spectrometry (QqQ-MS). Several metabolites were identified and results were compared with literature data on metabolism using a human cell line...
2013: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
Fazlin Mohd Fauzi, Alexios Koutsoukas, Andrew Cunningham, Ana Gallegos, Roumen Sedefov, Andreas Bender
OBJECTIVE: This study exemplifies computer-aided (in silico) approaches in assessing the risks of new psychoactive substances emerging in the European Union. In this work, we (i) consider the potential of Ostarine exhibiting psychoactivity and (ii) anticipate potential activities and toxicities of 4-methylamphetamine. METHOD: The approach, termed in silico target prediction, suggests potential protein targets modulated by compounds given their chemical structure...
July 2013: Human Psychopharmacology
Mihail F Zilbermint, Adrian S Dobs
Cancer cachexia is a complex syndrome, affecting up to 60% of the approximately 1.4 million patients diagnosed with cancer each year in the USA. This condition is characterized by progressive deterioration of a patient's nutritional status, weight loss, anorexia, diminished quality of life and increased mortality and morbidity. Current therapy with progestational, anti-inflammatory and anabolic agents is often ineffective and has a large number of undesirable effects. The newly developed nonsteroidal selective androgen receptor modulator Ostarine has demonstrated promising results in Phase I and II clinical trials, increasing total lean body mass, enhancing functional performance and decreasing total tissue percent fat...
October 2009: Future Oncology
Clelia Madeddu, Giovanni Mantovani
PURPOSE OF REVIEW: There are no published conclusive phase III controlled clinical trials nor general consensus about treatment approaches despite several years of coordinated efforts in basic and clinical research. Consequently, practice guidelines for the prevention and treatment of cancer-related muscle wasting are lacking. The purpose of this review is to supply an update on the promising agents and/or combined approaches for the treatment of cancer cachexia. RECENT FINDINGS: The choice for cancer cachexia treatment in clinical practice is very limited: the only approved drugs in Europe are progestagens...
December 2009: Current Opinion in Supportive and Palliative Care
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