Targeting the administration of ecdysterone in doping control samples

Parr, Maria Kristina; Ambrosio, Gabriella; Wuest, Bernhard; Mazzarino, Monica; Torre, Xavier de la; Sibilia, Francesca; Joseph, Jan Felix; Diel, Patrick; Botrè, Francesco

doi:10.1007/s11419-019-00504-y

Cited by 28 publications

(37 citation statements)

References 30 publications

(43 reference statements)

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“…Such experiments paved the way, directly or indirectly, for use as a "doping substance" by sportsmen or bodybuilders based on the consumption of uncontrolled dietary supplements [162]. The recent confirmation of these anabolic results [163] led the authors to propose the inscription of 20E on the list of doping prohibited substances [164].…”

Section: Clinical Studiesmentioning

confidence: 99%

20-Hydroxyecdysone, from Plant Extracts to Clinical Use: Therapeutic Potential for the Treatment of Neuromuscular, Cardio-Metabolic and Respiratory Diseases

et al. 2021

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There is growing interest in the pharmaceutical and medical applications of 20-hydroxyecdysone (20E), a polyhydroxylated steroid which naturally occurs in low but very significant amounts in invertebrates, where it has hormonal roles, and in certain plant species, where it is believed to contribute to the deterrence of invertebrate predators. Studies in vivo and in vitro have revealed beneficial effects in mammals: anabolic, hypolipidemic, anti-diabetic, anti-inflammatory, hepatoprotective, etc. The possible mode of action in mammals has been determined recently, with the main mechanism involving the activation of the Mas1 receptor, a key component of the renin–angiotensin system, which would explain many of the pleiotropic effects observed in the different animal models. Processes have been developed to produce large amounts of pharmaceutical grade 20E, and regulatory preclinical studies have assessed its lack of toxicity. The effects of 20E have been evaluated in early stage clinical trials in healthy volunteers and in patients for the treatment of neuromuscular, cardio-metabolic or respiratory diseases. The prospects and limitations of developing 20E as a drug are discussed, including the requirement for a better evaluation of its safety and pharmacological profile and for developing a production process compliant with pharmaceutical standards.

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Section: Clinical Studiesmentioning

confidence: 99%

20-Hydroxyecdysone, from Plant Extracts to Clinical Use: Therapeutic Potential for the Treatment of Neuromuscular, Cardio-Metabolic and Respiratory Diseases

et al. 2021

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“…Studies on the metabolism of ecdysterone have been conducted mostly in animals and only a few refer to humans [10,[30][31][32][33][34]. While ecdysterone does not seem to undergo phase II metabolism [30,34], studies concur on its biotransformation, leading to the formation of dehydroxylated metabolites. However, structure assignment and information on the excretion profiles differ in some studies.…”

Section: Introductionmentioning

confidence: 99%

“…Recently, in a single dose administration study, 51.5 mg of pure ecdysterone has been administered to one healthy volunteer, and the presence of 14-deoxy-ecdysterone was confirmed in the post-administration urine samples, in comparison to the in-house synthesized reference [34]. Parr et al reported ecdysterone as the most abundant analyte in post-administration urine samples, with a wider detection window than 14-deoxyecdysterone, which was excreted later [34].…”

Section: Introductionmentioning

confidence: 99%

Urinary Elimination of Ecdysterone and Its Metabolites Following a Single-Dose Administration in Humans

et al. 2021

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Ecdysterone is a phytosteroid widely discussed for its various pharmacological, growth-promoting, and anabolic effects, mediated by the activation of estrogen receptor beta (ERbeta). Performance-enhancement in sports was demonstrated recently, and ecdysterone was consequently included in the Monitoring Program, to detect potential patterns of misuse in sport. Only few studies on the pharmacokinetics of ecdysterone in humans have been reported so far. In this study, post-administration urine samples in twelve volunteers (single dose of 50 mg of ecdysterone) were analyzed using dilute-and-inject liquid-chromatography–tandem mass spectrometry. Identification and quantitation of ecdysterone and of two metabolites, 14-deoxy-ecdysterone and 14-deoxy-poststerone, was achieved. Ecdysterone was the most abundant analyte present in post-administration urine samples, detected for more than 2 days, with a maximum concentration (Cmax) in the 2.8–8.5 h urine (Cmax = 4.4–30.0 µg/mL). The metabolites 14-deoxy-ecdysterone and 14-deoxy-poststerone were detected later, reaching the maximum concentrations at 8.5–39.5 h (Cmax = 0.1–6.0 µg/mL) and 23.3–41.3 h (Cmax = 0.1–1.5 µg/mL), respectively. Sex-specific differences were not observed. Cumulative urinary excretion yielded average values of 18%, 2.3%, and 1.5% for ecdysterone, 14-deoxy-ecdysterone, and 14-deoxy-poststerone, respectively. Ecdysterone and 14-deoxy-ecdysterone were excreted following first-order kinetics with half-lives calculated with three hours, while pharmacokinetics of 14-deoxy-poststerone needs further evaluation.

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“…More studies are needed to clarify the exact mode of action. Maral root extract and 20-hydroxyecdysone are currently legal; however, 20-hydroxyecdysone was recently included in the WADA monitoring list [102]. Ashwagandha or Indian ginseng (Withania somnifera; Solanaceae) has recently received attention as a supplement that can increase muscle mass, strength, and overall fitness.…”

Section: Testosterone Boostersmentioning

confidence: 99%

Medicinal Use of Testosterone and Related Steroids Revisited

et al. 2021

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Testosterone derivatives and related compounds (such as anabolic-androgenic steroids—AAS) are frequently misused by athletes (both professional and amateur) wishing to promote muscle development and strength or to cover AAS misuse. Even though these agents are vastly regarded as abusive material, they have important pharmacological activities that cannot be easily replaced by other drugs and have therapeutic potential in a range of conditions (e.g., wasting syndromes, severe burns, muscle and bone injuries, anemia, hereditary angioedema). Testosterone and related steroids have been in some countries treated as controlled substances, which may affect the availability of these agents for patients who need them for therapeutic reasons in a given country. Although these agents are currently regarded as rather older generation drugs and their use may lead to serious side-effects, they still have medicinal value as androgenic, anabolic, and even anti-androgenic agents. This review summarizes and revisits the medicinal use of compounds based on the structure and biological activity of testosterone, with examples of specific compounds. Additionally, some of the newer androgenic-anabolic compounds are discussed such as selective androgen receptor modulators, the efficacy/adverse-effect profiles of which have not been sufficiently established and which may pose a greater risk than conventional androgenic-anabolic agents.

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Targeting the administration of ecdysterone in doping control samples

Cited by 28 publications

References 30 publications

20-Hydroxyecdysone, from Plant Extracts to Clinical Use: Therapeutic Potential for the Treatment of Neuromuscular, Cardio-Metabolic and Respiratory Diseases

20-Hydroxyecdysone, from Plant Extracts to Clinical Use: Therapeutic Potential for the Treatment of Neuromuscular, Cardio-Metabolic and Respiratory Diseases

Urinary Elimination of Ecdysterone and Its Metabolites Following a Single-Dose Administration in Humans

Medicinal Use of Testosterone and Related Steroids Revisited

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