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- | ligandrol (VK5211) / Viking Therap
Journal: Ligandrol Ameliorates High-Fat Diet- and Streptozotocin-Induced Type 2 Diabetes Mellitus and Prevents Pancreatic Islets Degeneration. (Pubmed Central) - Dec 16, 2024
Histopathological staining studies showed that ligandrol prevents pancreatic islet degeneration compared with the HFD and STZ group. Our findings suggest that ligandrol's protective effect on pancreatic islets leading to its antidiabetic effect occurs through the activation of AR.
- | ligandrol (VK5211) / Viking Therap
Journal: LGD-4033 and a Case of Drug-Induced Liver Injury: Exploring the Clinical Implications of Off-Label Selective Androgen Receptor Modulator Use in Healthy Adults. (Pubmed Central) - Oct 18, 2024
A diagnostic workup ruled out other potential causes of liver injury, implicating SARM use as the likely etiology. This case underscores the necessity for heightened clinical vigilance, early diagnosis, and prompt intervention to mitigate serious health outcomes associated with SARM misuse.
- | Ostarine (enobosarm) / Veru Inc, ligandrol (VK5211) / Viking Therap
Journal: The disordering effect of SARMs on a biomembrane model. (Pubmed Central) - Jul 23, 2024
By employing theoretical calculations, we gained insights into the possible electrostatic interactions between SARMs and phospholipid molecules, enhancing our understanding of the driving forces behind the interactions of SARMs with lipid membranes. Overall, this investigation provides relevant knowledge related to the biophysical-chemical effects that SARMs produce in biomembrane models and could be of practical reference for promising applications of SARMs in medicine and sport.
- | Ostarine (enobosarm) / Veru Inc
Journal: A screening method for the quantitative determination of selective androgen receptor modulators (SARMs) in capsules by high resolution 19F- and 1H-NMR spectroscopy. (Pubmed Central) - Mar 22, 2024
The statistical analysis of the results from 19F- and 1H-quantitative NMR showed that both approaches were equally effective, thus expanding the potential use of the methodology to non-fluorinated SARMs. At present, no SARM has been approved for human consumption; however, SARMs are actually used by bodybuilders and recreational athletes, who purchase them even though the risk-benefit ratio of these molecules has not been definitively established.
- | ligandrol (VK5211) / Viking Therap
Preclinical, Journal: Effects of ligandrol as a selective androgen receptor modulator in a rat model for osteoporosis. (Pubmed Central) - Nov 30, 2023
Ligandrol at high dose showed a subtle anabolic effect on structural properties without any improvement in biomechanical properties of osteoporotic bones. Considering side effects of ligandrol at this dose, its further investigation for the therapy of postmenopausal osteoporosis should be reevaluated.
- | vosilasarm (EP0062) / Ellipses Pharma, Ostarine (enobosarm) / Veru Inc, ligandrol (VK5211) / Viking Therap
Journal: Detection of anabolic agents including selective androgen receptor modulators in samples outside of sport. (Pubmed Central) - Nov 21, 2023
Our results indicate that SARM use might be a concern outside of sport. Subsequently, in addition to AAS, the healthcare system should also be informed about SARM abuse and the associated adverse side effects.
- | ligandrol (VK5211) / Viking Therap
Preclinical, Journal: Investigation of in vitro generated metabolites of LGD-4033, a selective androgen receptor modulator, in homogenized camel liver for anti-doping applications. (Pubmed Central) - Oct 15, 2023
Subsequently, in addition to AAS, the healthcare system should also be informed about SARM abuse and the associated adverse side effects. These findings provide valuable insights into the metabolism of LGD-4033 in camels and aid in the development of effective doping control methods for the detection of SARMs in camel racing.
- | ligandrol (VK5211) / Viking Therap
Journal: Variation of Sequential Ligandrol (LGD-4033) Metabolite Levels in Routine Anti-Doping Urine Samples Detected with or without Other Xenobiotics. (Pubmed Central) - Oct 4, 2023
It is also worth noting that dietary supplements may contain ligandrol as an official ingredient or as a contaminant. The described method may be usefully applied by other anti-doping or toxicological laboratories.
- | Ostarine (enobosarm) / Veru Inc, ligandrol (VK5211) / Viking Therap
Preclinical, Journal: Selective Androgen Receptor Modulators Combined with Treadmill Exercise Have No Bone Benefit in Healthy Adult Rats. (Pubmed Central) - Sep 28, 2023
TE represents a safe treatment. Because SARMs are increasingly applied in gyms along with physical activities, attention should be paid to possible side effects.
- | ligandrol (VK5211) / Viking Therap
Journal: Investigations into the concentration and metabolite profiles of stanozolol and LGD-4033 in blood plasma and seminal fluid using liquid chromatography high-resolution mass spectrometry. (Pubmed Central) - Nov 29, 2022
The developed assays proved appropriate for the detection of the target substances in both matrices with detection limits between 10 and 40 pg/mL for the unmetabolized drugs in sf and bp, allowing to estimate the concentration of stanozolol in bp (0.02-0.40 ng/mL) and in sf (0.01-0.25 ng/mL) as well as of LGD-4033 in bp (0.21-2.00 ng/mL) and in sf (0.03-0.68 ng/mL) post-administration. In addition, metabolites resulting from different metabolic pathways were identified in sf and bp, with sf resembling a composite of the metabolic profile of bp and urine.
- | ligandrol (VK5211) / Viking Therap
Journal: Structure revision and chemical synthesis of ligandrol's main bishydroxylated long-term metabolic marker. (Pubmed Central) - Nov 16, 2022
A chemically more robust structure was postulated as an alternative to the one previously established. The NMR spectra of the synthesized material and its LC-HRMS comparison with a relevant metabolic sample support the proposed structural revision.
- | ligandrol (VK5211) / Viking Therap
Journal: Ligandrol-induced liver injury - Case Report (Pubmed Central) - Oct 19, 2022
Ligandrol is misused as a selective androgen receptor modulator to promote muscle building. This case represents a typical case of abuse of anabolic substances in amateur sports.
- vosilasarm (RAD140) / Radius
Severe cholestatic injury following use of RAD-140, a novel, easily accessible body-building supplement () - Oct 4, 2022 - Abstract #AGW2022AGW_363;
SARMs have the potential to cause severe cholestatic injury that is not extensively documented. Given the ease of access of these supplements, clinicians should be aware of severe cholestatic liver injury associated with their use and the prolonged recovery.
- | vosilasarm (RAD140) / Radius, ligandrol (VK5211) / Viking Therap
Journal: Detection of selective androgen receptor modulators (SARMs) in serum using a molecularly imprinted nanoparticle surface plasmon resonance sensor. (Pubmed Central) - Sep 20, 2022
Crucially these levels are below the minimum required performance limit (MRPL) set for these compounds by WADA. This study highlights the power of modern molecular imprinting to rapidly address required molecular recognition for new compounds of interest.
- | ligandrol (VK5211) / Viking Therap
Journal: Investigations into the elimination profiles and metabolite ratios of micro-dosed selective androgen receptor modulator LGD-4033 for doping control purposes. (Pubmed Central) - Feb 24, 2022
The metabolite M1, representing the epimer of LGD-4033, was synthesized and the structure elucidated by NMR spectroscopy. As the M1/LGD-4033 ratio changes over time, the ratio and the approximate LGD-4033 concentration can contribute to estimating the time point of drug intake and dose of LGD-4033 in doping control urine samples, which is particularly relevant in anti-doping result management.
- || bicalutamide / Generic mfg.
Clinical, Journal: Development and validation of SARMs and metabolic modulators screening in hair using UHPLC-MS/MS: Application to a doping case and first identification of S23 in authentic human hair. (Pubmed Central) - Feb 5, 2022
After addition of bicalutamide-D used as internal standard and incubation in phosphate buffer pH = 9.5, 20 mg of hair samples were extracted with liquid/liquid extraction...The application and the interest of SARMs screening was demonstrated in a doping case. Three SARMs were detected namely andarine (120-1644 pg/mg), ostarine (1-9 pg/mg) and S23 (0.6-16 pg/mg) in 6x1 cm segments of the subject.
- | Ostarine (enobosarm) / Veru Inc, ligandrol (VK5211) / Viking Therap
Journal: Perspectives in Evaluating Selective Androgen Receptor Modulators (SARMs) in Human Hair: A Short Communication. (Pubmed Central) - Nov 17, 2021
To enhance performance, SARMs must be used on a long-term basis, which can have serious clinical consequences, including liver damage, myocardial infarction, and blood clots. Hair testing for SARMs has additional benefits versus urine analysis as it can detect the parent compound as well as numerous metabolites.
- | vosilasarm (RAD140) / Radius, Ostarine (enobosarm) / Veru Inc, ligandrol (VK5211) / Viking Therap
Journal: The forensic response after an adverse analytical finding (doping) involving a selective androgen receptor modulator (SARM) in human athlete. (Pubmed Central) - Nov 17, 2021
To date, all methods for SARMs identification in various matrices involve liquid chromatography coupled to tandem mass spectrometry or high-resolution mass spectrometry. The aim of this paper is to review the scientific literature on the analytical possibilities of testing SARMs in dietary supplements, urine and hair or nail clippings after an AAF to document the claims of an athlete or his/her legal team.
- | bicalutamide / Generic mfg.
Journal: Development of a multi-residue high-throughput UHPLC-MS/MS method for routine monitoring of SARM compounds in equine and bovine blood. (Pubmed Central) - Oct 3, 2021
Applicability of the developed assay was demonstrated through the analysis of blood samples from racehorses and cattle. The developed method presents a high-throughput cost-effective tool for routine screening for a range of SARM compounds in sport and livestock animals.
- vosilasarm (RAD140) / Radius, Ostarine (enobosarm) / Veru Inc, ligandrol (VK5211) / Viking Therap
Harm by SARM: A Case of Drug-Induced Liver Injury in an Amateur Bodybuilder (Shoreline Exhibit Hall) - Sep 8, 2021 - Abstract #ACG2021ACG_65;
Review of social history revealed insignificant alcohol or acetaminophen use but a six-month history of SARM use for body building: RAD 140, ligandrol, ostarine...He did not show any complications of liver disease and was discharged with Ursodiol...We presented a case of chronic SARM use and delayed onset of hepatotoxicity in a patient requiring liver transplantation evaluation. Providers should complete a thorough medication reconciliation in amateur body-builders.
- | Journal: Simultaneous detection of different chemical classes of selective androgen receptor modulators in urine by liquid chromatography-mass spectrometry-based techniques. (Pubmed Central) - Jun 22, 2021
Urine samples containing andarine, ostarine, or LGD4033 were used to confirm the actual applicability of the selected analytical strategies. All target compounds (parent drugs and their main metabolites) were detected and correctly identified.
- | Ostarine (enobosarm) / Veru Inc, ligandrol (VK5211) / Viking Therap
Preclinical, Journal: Ostarine and Ligandrol Improve Muscle Tissue in an Ovariectomized Rat Model. (Pubmed Central) - May 27, 2021
LG showed more effect on muscle metabolism. However, a higher muscle weight and intramuscular fat content observed after LG treatment (4 mg) as well as an uterotrophic effect of both SARMs at higher dosages could be considered as an unfavorable side effects and might be a limitation for their application at these dosages.
- RAD140 / Radius
[VIRTUAL] RAD-140: An Emerging Cause of Drug-Induced Liver Injury () - Sep 15, 2020 - Abstract #ACG2020ACG_2719;
This case raises concerns regarding SARMs advertised selectivity and safety. Until further data is available, these agents should be used with caution.
- | VK5211 / Ligand, VikingTherapeutics
Journal: Investigation of the metabolism of the selective androgen receptor modulator LGD-4033 in equine urine, plasma and hair following oral administration. (Pubmed Central) - Sep 2, 2020
In vitro incubation of LGD-4033 with equine liver microsomes was also performed for comparison, yielding 11 phase I metabolites. All of the metabolites observed in vivo were also observed in vitro.
- | Ostarine (enobosarm) / Oncternal Therapeutics, VK5211 / Ligand, VikingTherapeutics
Preclinical, Journal: High-throughput liquid chromatography tandem mass spectrometry assay as initial testing procedure for analysis of total urinary fraction. (Pubmed Central) - Aug 28, 2020
Compounds most often identified were stanozolol, GW1516, ostarine, LGD4033 and clomiphene, with median estimated concentrations in the range of 0.02-0.09 ng/mL (either as parent drug or a metabolite). Our data demonstrate the importance of using a highly sensitive ITP to ensure efficient anti-doping testing.
- | VK5211 / Ligand, VikingTherapeutics
Preclinical, Journal: HUMAN IN-VIVO METABOLISM STUDY OF LGD-4033. (Pubmed Central) - Apr 3, 2019
The gluco-conjugated parent LGD-4033 and its gluco-conjugated metabolites M1 and M2 can be also considered as useful target analytes in non-hydrolyzed samples. The study also presents two trihydroxylated metabolites which are identified for the first time in human urine; one of them was recently reported in LGD-4033 metabolism study in horse urine and plasma.
- |||| ligandrol (VK5211) / Viking Therap
Trial completion: Acute Hip Fracture Study in Patients 65 Years or Greater (clinicaltrials.gov) - Apr 11, 2018
P2, N=108, Completed, Sponsor: Viking Therapeutics, Inc.
The study also presents two trihydroxylated metabolites which are identified for the first time in human urine; one of them was recently reported in LGD-4033 metabolism study in horse urine and plasma. Active, not recruiting --> Completed
- ||| ligandrol (VK5211) / Viking Therap
Enrollment closed, Trial primary completion date: Acute Hip Fracture Study in Patients 65 Years or Greater (clinicaltrials.gov) - Jul 19, 2017
P2, N=120, Active, not recruiting, Sponsor: Viking Therapeutics, Inc.
Active, not recruiting --> Completed Recruiting --> Active, not recruiting | Trial primary completion date: Jun 2017 --> Sep 2017
- || ligandrol (VK5211) / Viking Therap
Trial primary completion date: Acute Hip Fracture Study in Patients 65 Years or Greater (clinicaltrials.gov) - Mar 8, 2017
P2, N=120, Recruiting, Sponsor: Viking Therapeutics, Inc.
Recruiting --> Active, not recruiting | Trial primary completion date: Jun 2017 --> Sep 2017 Trial primary completion date: Dec 2016 --> May 2017
- |||| ligandrol (VK5211) / Viking Therap
Enrollment open: Acute Hip Fracture Study in Patients 65 Years or Greater (clinicaltrials.gov) - Nov 14, 2015
P2, N=120, Recruiting, Sponsor: Viking Therapeutics, Inc.
Trial primary completion date: Dec 2016 --> May 2017 Not yet recruiting --> Recruiting
- ||||| ligandrol (VK5211) / Viking Therap
New P2 trial: Acute Hip Fracture Study in Patients 65 Years or Greater (clinicaltrials.gov) - Oct 22, 2015
P2, N=120, Not yet recruiting, Sponsor: Viking Therapeutics, Inc.