In April 2024 the Anti-Doping Agency of Kenya (ADAK) reported 2 anti-doping rule violations against the Kenyan Athlete Josphat Kipkemboi Kemei after his 2 samples tested positive for the prohibited substance Methoxy polyethylene glycol-epoetin beta (CERA).

In May 2024 the Athletics Integrity Unit (AIU), on behalf of World Athletics, also reported two anti-doping rule violations against the Athlete after his 2 other samples tested positive for the substances CERA and Testosterone.

Thereupon in May 2024 ADAK delegated its Results Management to the AIU regarding the two reported anti-doping rule violations. These charges from ADAK and the AIU were based on the samples provided by the Athlete on:

• 16 April 2023 in China;
• 15 February 2024 in Kenya;
• 29 February 2024 in Kenya; and
• 15 March 2024 in Kenya.

Following notification the Athlete timely admitted the violation, waived his right for a hearing, accepted a provisional suspension and the sanction proposed by the AIU.

The AIU deems that the Athlete failed to establish that the violation was not intentional. Because he had signed and submitted the Admission of Anti-Doping Rule Violations and Acceptance of Consequences Form he received a 1 year reduction from the AIU.

Furthermore the AIU finds that there are aggravating circumstances present in this case because the Athlete had committed multiple anti-doping rule violations. Finally these violations are considered together as one first anti-doping rule violation.

Therefore the AIU decides on 16 May 2024 to impose a 5 year period of ineligibility on the Athlete, starting on the date of the provisional suspension, i.e. on 22 April 2024.

In April 2023 an Expert Panel of the Athletics Integrity Unit (AIU) concluded unanimously in their Joint Expert Opinion that the hematological profile of the Kenyan Athlete Rodgers Kwemoi “highly likely” showed that he had used a prohibited substance or a prohibited method: the use of EPO or Blood doping. 

This conclusion of the AIU Expert Panel was based on assessment of blood samples, collected in the period from 18 July 2016 until 1 February 2023 reported in the Athlete’s Biological Passport (ABP). 

Following notification the Athlete submitted an explanation for the abnormal values in his ABP. However after consideration the Expert Panel rejected the Athlete’s explanation in their 2nd Joint Expert Opinion in August 2023.

Consequently in August 2023 the AIU, on behalf of World Athletics, reported an anti-doping rule violation against the Athlete. A provisional suspension was ordered and he was heard for the World Athletics Disciplinary Tribunal. 

The Athlete denied he acted intentionally and he disputed the reliability of the ABP evidence. He asserted that the abnormalities in his ABP could be explained by his regular training at high altitude.

The AIU deems that the abnomalies in the Athlete's ABP were caused by a prohibited substance or a prohibited method and that he failed to demonstrate that the violation was not intentional. Furthermore the AIU contended that the Athlete provided inconsistent evidence in his defence.

The Panel assessed and addressed the Parties' evidence and determines that:

• The ABP is a reliable means that may assist in establishing an anti-doping rule violation;
• The Athlete had used a prohibited substance or a prohibited method between July 2016 and February 2023;
• He committed an anti-doping rule violation;
• He was involved in a deliberate, systematic and sophisticated doping regime;
• The are significant aggravating circumstances present in this case;
• The Athlete's results shall be disqualified from July 2016 until the provisional suspension.

Therefore the Panel decides on 24 April 2024 to impose a 6 year period of ineligibility on the Athlete, starting on the date of the provisional suspension, i.e. on 8 August 2023.

Doping control analysis of trimetazidine and characterization of major metabolites using mass spectrometric approaches / Gerd Sigmund, Anja Koch,  Anne-Katrin Orlovius, Sven Guddat, Andreas Thomas, Wilhelm Schänzer, Mario Thevis

• Drug Testing And Analysis 6 (2014) 11-12 (November-December), p. 1197-1205
• 32nd Cologne workshop: Advances in sports drug testing
• PMID: 24913825 
• DOI: 10.1002/dta.1680

Abstract

Since January 2014, the anti-anginal drug trimetazidine [1-(2,3,4-trimethoxybenzyl)-piperazine] has been classified as prohibited substance by the World Anti-Doping Agency (WADA), necessitating specific and robust detection methods in sports drug testing laboratories. In the present study, the implementation of the intact therapeutic agent into two different initial testing procedures based on gas chromatography-mass spectrometry (GC-MS) and liquid chromatography-tandem mass spectrometry (LC-MS/MS) is reported, along with the characterization of urinary metabolites by electrospray ionization-high resolution/high accuracy (tandem) mass spectrometry. For GC-MS analyses, urine samples were subjected to liquid-liquid extraction sample preparation, while LC-MS/MS analyses were conducted by established 'dilute-and-inject' approaches. Both screening methods were validated for trimetazidine concerning specificity, limits of detection (0.5-50 ng/mL), intra-day and inter-day imprecision (<20%), and recovery (41%) in case of the GC-MS-based method. In addition, major metabolites such as the desmethylated trimetazidine and the corresponding sulfoconjugate, oxo-trimetazidine, and trimetazidine-N-oxide as identified in doping control samples were used to complement the LC-MS/MS-based assay, although intact trimetazidine was found at highest abundance of the relevant trimetazidine-related analytes in all tested sports drug testing samples. Retrospective data mining regarding doping control analyses conducted between 1999 and 2013 at the Cologne Doping Control Laboratory concerning trimetazidine revealed a considerable prevalence of the drug particularly in endurance and strength sports accounting for up to 39 findings per year.

Analytical detection of trimetazidine produced by metabolic conversion of lomerizine in doping control analysis / Masato Okano, Mario Thevis, Mitsuhiko Sato, Shinji Kageyama

• Drug Testing And Analysis 8 (2016) 8 (August), p. 869-874
• PMID: 26560081
• DOI: 10.1002/dta.1893

Abstract

The identification of trimetazidine in urine samples might result from administration of the permitted drug lomerizine. Laboratories are therefore urged to carefully investigate suspicious cases where trimetazidine is detected. Differentiation of abuse of the banned substance trimetazidine from use of the permitted drug lomerizine would be supported by analysis of the intact drug lomerizine and/or specific metabolites.

Trimetazidine attenuates high-altitude fatigue and cardiorespiratory fitness impairment : A randomized double-blinded placebo-controlled clinical trial / Jie Yang, Laiping Zhang, Chuan Liu, Jihang Zhang, Shiyong Yu, Jie Yu, Shizhu Bian, Sanjiu Yu, Chen Zhang, Lan Huang

• Biomedicine & Pharmacotherapy 116 (2019, August), 109003
• PMID: 31125823
• DOI: 10.1016/j.biopha.2019.109003

Abstract

Trimetazidine (TMZ) has been shown to optimize myocardial energy metabolism and is a common anti-ischemic agent. Our trial (ChiCTR-TRC-13003298) aimed to explore whether TMZ has any preventive effect on high-altitude fatigue (HAF), cardiac function and cardiorespiratory fitness upon acute high-altitude exposure and how it works on HAF. Thirty-nine healthy young subjects were enrolled in a randomized double-blinded placebo-controlled trial and were randomized to take oral TMZ (n = 20) or placebo (n = 19), 20 mg tid, 14 days prior to departure until the end of study. The 2018 Lake Louise Score questionnaire, echocardiography, assessments of physical working capacity, circulating markers of myocardial energy metabolism and fatigue were performed both before departure and arrival at highland. At follow-up, TMZ significantly reduced the incidence of HAF (p = 0.038), reversed cardiorespiratory fitness impairment, decreased left ventricular end-systolic volume (LVESV, p = 0.032) and enhanced left ventricular ejection fraction (LVEF, p = 0.015) at highland. Relative to the placebo group, the TMZ group had significantly lower LDH (p = 0.025) and lactate levels before (p < 0.001) and after (p = 0.012) physical exercise after acute high-altitude exposure. Additionally, improved left ventricular systolic function might have contributed to ameliorating HAF during TMZ treatment (LVEF, OR = 0.859, 95% CI = 0.741-0.996, p = 0.044). In conclusion, our results demonstrated that TMZ could prevent HAF, cardiorespiratory fitness impairment and improves left ventricular systolic function during acute high-altitude exposure. This trial provides new insights into the effect of TMZ and novel evidence against HAF and cardiorespiratory fitness impairment at highland.

Anti-Doping Reanalysis Programme (2004-2021) / International Olympic Committee (IOC). - Lausanne : IOC, 2021

Contents:

• Anti-doping rule violations (ADRVs) resulting from the re-analysis programme from 2004 to today
  31 Aug 2021 · 1 pages · xlsx
• Beijing 2008 re-analysis programme
  01 Aug 2021 · 3 pages
• London 2012 re-analysis programme
  01 Dec 2021 · 1 pag

Prolonged occurrence of cocaine in human saliva and urine after chronic use / Edward J. Cone, William W. Weddington, Jr.

• Journal of Analytical Toxicology 13 (1989) 2 (March-April), p. 65-68
• PMID: 2733393
• DOI: 10.1093/jat/13.2.65

Abstract

Cocaine was detected by immunoassay in saliva and urine of chronic cocaine addicts for 5-10 days during abstinence. Confirmation by a less sensitive but highly specific GC/MS assay of unmetabolized cocaine was successful in saliva through the first 24 h of collection and for the initial 4-5 days in urine. Cocaine saliva concentrations and subject scores for cocaine craving and depression declined during this time and correlated significantly. The presence of unmetabolized cocaine in these biofluids long after the last drug administration suggests that multiple dosing and high exposure to cocaine in man leads to accumulation in deep body compartments and subsequent slow release back into circulation and eventual excretion. The prolonged presence of cocaine in saliva and urine may have implications in testing for cocaine use and in treatment of cocaine withdrawal.

Urinary excretion of cocaine and benzoylecgonine following oral ingestion in a single subject / R.C. Baselt, R. Chang

• Journal of Analytical Toxicology 11 (1987) 2 (March-April), p. 81–82
• PMID: 3573730
• DOI: 10.1093/jat/11.2.81

Abstract

A 25 mg oral dose of cocaine HCl given to a single volunteer resulted in a peak urinary cocaine concentration of 269 ng/mL at 1 h, and a peak benzoylecgonine concentration of 7,940 ng/mL at 12 h. Urine benzoylecgonine concentrations remained in excess of 300 ng/mL for 48 h. We conclude that small, oral doses of cocaine, potentially undetectable to the user, may cause positive urine test results for at least 48 h using routine detection methods.

Cocaine and benzoylecgonine excretion in humans / H.E. Hamilton, J.E. Wallace, E.L. Shimek Jr, P. Land, S.C. Harris, J.G. Christenson

• Journal of forensic sciences 22 (1977) 4 (October), p. 697-707
• PMID: 370332University of Texas System (UT System)
  
  

Abstract

Maximal urinary excretion of unchanged cocaine occurred within 2 h of the intranasal absorption of 1.5 mg/kg body weight of cocaine hydrochloride, and diminished rapidly thereafter. Excretion of benzoylecgonine was maximal 4 to 8 h following administration of the drug and diminished slowly over an interval of several days. Peak cocaine and benzoylecgonine concentrations observed were 24 and 75 microgram/ml, respectively. Benzoylecgonine/cocaine ratios were too varied to allow estimation of cocaine concentrations from benzoylecgonine concentration data or vice versa. Benzoylecgonine concentrations generally exceeded the corresponding cocaine values by a wide margin, but excretion of free cocaine in the absence of benzoylecgonine was observed in one subject. Cocaine was generally detected for only approximately 8 h, and for a maximum of 12 h, whereas benzoylecgonine was generally detected by chromatographic or enzyme immunologic assays for 48 to 72 h. Benzoylecgonine was positively identified in urine by raidoimmunoassay for 96 to 144 h after dosing.

In September 2023 the Athletics Integrity Unit (AIU), on behalf on World Athletics, reported an anti-doping rule violation against the Lithuanian Athlete Vilmante Stašauskaitė after her sample tested positive for the prohibited substance Meldonium.

Following notification the Athlete timely admitted the violation, waived her right for a hearing, accepted a provisional suspension and the sanction proposed by the AIU. The Parties went into a Case Resolution Agreement.

The amateur Athlete acknowledged with corroboration evidence that she had had purchased and used Meldonium without a prescription. She asserted that she was unaware that Meldonium was a prohibited substance.

Therefore the AIU decides on 24 April 2024 to impose a 21 month period of ineligibility on the Athlete, starting on the date of the sample collection, i.e. on 10 September 2023.