Detection of clostebol in sports: Accidental doping?,Drug Testing and Analysis

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Detection of clostebol in sports: Accidental doping?
Drug Testing and Analysis ( IF 2.6 ) Pub Date : 2020-10-29 , DOI: 10.1002/dta.2951
Xavier de la Torre ₁ , Cristiana Colamonici ₁ , Michele Iannone ₁ , Daniel Jardines ₁ , Francesco Molaioni ₁ , Francesco Botrè _{1,

2}

Affiliation

The detection of clostebol misuse in sports has been growing recently, especially in Italy, due to the ample availability of pharmaceutical formulations containing clostebol acetate (Trofodermin®) and the use of more sensitive instrumentation by the antidoping laboratories. Most of these cases have been claimed to be related to a nonconscious use of the drug or through contact with relatives or teammates using it. We have investigated, through the application of the well‐known and currently used gas chromatographic mass spectrometric procedures, the likelihood of these allegations and have demonstrated that after a single transdermal administration of 5 mg of clostebol acetate and a transient contact with the application area, it is possible to generate adverse analytical findings in antidoping controls. We have reviewed the Phase I and Phase II clostebol metabolism in order to generate evidences that may help the sport authorities reviewing these cases. The main clostebol metabolite (4‐chloro‐androst‐4‐en‐3α‐ol‐17‐one, M1) generally used at the screening level as well as other three metabolites (M2–M4) are mainly excreted as glucuronides, whereas M5 (4ζ‐chloro‐5ζ‐androstan‐3β‐ol‐17‐one) is predominantly excreted as sulfate. Neither the 5α‐reductases activity (impaired by the presence of the chlorine in C4) nor specific sulfotransferases present in the skin allowed a clear distinction of the administration route. Studies with a larger number of volunteers and probably investigating another physiological fluid allowed in antidoping such as blood are needed for a deeper investigation. It is not unreasonable to establish a reporting level for M1, maybe creating some false negatives but excluding nonintentional doping scenarios.

中文翻译：

在运动中检测clostebol：意外服用兴奋剂？

由于含有醋酸克洛斯特波 (Trofodermin®) 的药物制剂的充足供应以及反兴奋剂实验室使用更灵敏的仪器，最近对体育运动中滥用氯甾醇的检测一直在增加，尤其是在意大利。这些案例中的大多数都被声称与无意识地使用该药物或通过与使用该药物的亲戚或队友的接触有关。我们通过应用众所周知的和目前使用的气相色谱质谱分析程序调查了这些指控的可能性，并证明在单次透皮给药 5 毫克醋酸氯甾醇和短暂接触应用区域后，在反兴奋剂控制中可能会产生不利的分析结果。我们已经审查了 I 期和 II 期 clostebol 代谢，以生成可能有助于体育当局审查这些案例的证据。通常用于筛选水平的主要clostebol代谢物（4-chloro-androst-4-en-3α-ol-17-one，M1）以及其他三种代谢物（M2-M4）主要以葡萄糖醛酸苷的形式排出，而M5 (4ζ-chloro-5ζ-androstan-3β-ol-17-one) 主要以硫酸盐的形式排出体外。5α-还原酶活性（因 C4 中氯的存在而减弱）和皮肤中存在的特定磺基转移酶都不能明确区分给药途径。需要对更多志愿者进行研究，并可能调查另一种允许在反兴奋剂中使用的生理液体，例如血液，以进行更深入的调查。为M1设立报告级别并非不合理，

更新日期：2020-12-15

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