HUMAN IN-VIVO METABOLISM STUDY OF LGD-4033.
Authors of this article are:
Fragkaki AG Sakellariou P Kiousi P Kioukia-Fougia N Tsivou M Petrou M Angelis YS.
A summary of the article is shown below:
Selective Androgen Receptor Modulators (SARMs) is an emerging class of therapeutics targeted to cachexia, sarcopenia and hypogonadism treatment. LGD-4033 is a SARM which has been included in the Prohibited List annually released by the World Anti-Doping Agency (WADA). The aim of the present work was the investigation of the metabolism of LGD-4033 in a human excretion study after administration of an LGD-4033 supplement, the determination of the metabolites’ excretion profiles with special interest in the determination of its long-term metabolites, and the comparison of the excretion time of the phase-I and phase-II metabolites. The results were also compared to those derived from previous LGD-4033 studies concerning both in vitro and in vivo experiments. Supplement containing LGD-4033 was administered to one human male volunteer and urine samples were collected up to almost 21 days. Analysis of the hydrolyzed (with β-glucuronidase) as well as of the non-hydrolyzed samples was performed using Liquid Chromatography-High Resolution Mass Spectrometry (LC-HRMS) in negative ionization mode and revealed that, in both cases, the two isomers of the dihydroxylated metabolite (M5) are preferred target metabolites. 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.
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