Detection of bazedoxifene, a selective estrogen receptor modulator, in human urine by liquid chromatography‐tandem mass spectrometry

Okano, Masato; Sato, Mitsuhiko; Kageyama, Shinji

doi:10.1002/dta.3225

Cited by 3 publications

(3 citation statements)

References 15 publications

(23 reference statements)

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“…Bazedoxifene (Figure 1, 7 ), an SERM, was introduced into WADA's Prohibited List in 2020, and the traceability in routine doping controls was assessed by Okano et al by means of an administration study conducted with seven study participants 76 . Upon oral administration of 20 mg of bazedoxifene acetate, urine was sampled up to 78 h and analyzed by LC–HRMS/MS.…”

Section: β2‐agonists Hormone and Metabolic Modulators And Diureticsmentioning

confidence: 99%

Annual banned‐substance review—Analytical approaches in human sports drug testing 2021/2022–

Thevis

Kuuranne

Geyer

2022

Drug Testing and Analysis

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Also in 2021/2022, considerable efforts were invested into advancing human sports drug testing programs, recognizing and taking into account existing as well as emerging challenges in anti-doping, especially with regard to substances and methods of doping specified in the World Anti-Doping Agency's 2022 Prohibited List. In this edition of the annual banned-substance review, literature on recent developments published between October 2021 and September 2022 is summarized and discussed.Focus is put particularly on enhanced analytical approaches and complementary testing options in human doping controls, appreciating the exigence and mission in anti-doping and, equally, the contemporary "new normal" considering, for example, the athlete's exposome versus analytical sensitivity and applicable anti-doping regulations for result interpretation and management.

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Section: β2‐agonists Hormone and Metabolic Modulators And Diureticsmentioning

confidence: 99%

Annual banned‐substance review—Analytical approaches in human sports drug testing 2021/2022–

Thevis

Kuuranne

Geyer

2022

Drug Testing and Analysis

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“…The trace level impurities of Impurity-A and Impurity-B present in the Bazedoxifene drug substance or drug product may cause severe harmful effects on human health. The concentration limit of genotoxic impurities, Impurity-A, and Impurity-B was calculated based on TTC [1][2][3][4][5] and maximum daily dose [1][2][3][4][5][6][7][8] . Impurity-A and Impurity-B each must to be controlled at below 75ppm.…”

mentioning

confidence: 99%

Untitled

2023

IJPSR

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Bazedoxifene acetate represents a promising new treatment for osteoporosis. LC-MS SIR (Selective ion recording) mode, the shortest runtime method, was developed and validated for the trace level quantification of two potential genotoxic impurities, i.e., Impurity-A (1 -Benzyloxy -4 -nitrobenzene) and Impurity -B (4benzyloxy-2-bromopropiophenone) in Bazedoxifene acetate drug substance. The concentration limits of both genotoxic impurities were calculated a limit of 75ppm based on the concept of TTC (threshold of toxicological concern) and MDD (maximum daily dosage, which is 20mg/day for Bazedoxifene acetate drug substance). The mobile phase used for the method was 10mM Ammonium acetate and acetonitrile in the ratio of (30:70) v/v with isocratic mode elution at flow rate 0.6mL/min, stationary phase used as X-Bridge C18 (50x4.6) mm, 3.5µm and run time was 5 minutes. The Impurities were quantified by using MS detector SIR mode (Selective ion recording) at m/z of 230.12 and 319.01 for Impurity-A and Impurity-B, respectively. The detection limit (DL) was 1.4 ppm for both Impurity-A and Impurity-B. The quantification limit (QL) for Impurity-A was 3.0ppm, and Impurity-B was 3.1ppm, respectively. The method was found to be linear, from 3.0 ppm to 111.0 ppm for Impurity-A and 3.1 ppm to 112.4 ppm for Impurity-B. The method was found to be Specific, Precise, Linear, and Accurate. INTRODUCTION:Bazedoxifene acetate Chemical name was 1 -[[4 -[2 -(Hexahydro -1H -azepin -1 -yl) ethoxy] phenyl] methyl] -2 -(4hydroxyphenyl) -3methyl -1H -indol-5-ol monoacetate (salt).

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“…18 Research into the metabolism of the selective estrogen receptor modulator (SERM) bazedoxifene demonstrated that the most suitable target analyte for routine doping controls would be the glucuronic acid conjugated drug, which was traceable for at least 78 h after a single oral dose of the SERM using LC-MS approaches. 19 In order to improve routine ITPs for the SERMs tamoxifen and toremifene, their common metabolic product referred to as carboxy-toremifene was synthesized and fully characterized, thus being available for future anti-doping test methods. 20 Finally, and particularly relevant for result management and in avoiding unintentional anti-doping rule violations, urinary excretion profiles for rectal corticoid administrations were investigated.…”

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confidence: 99%

The 40^th Manfred Donike workshop on doping analysis

Thevis

2022

Drug Testing and Analysis

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The 40 th Manfred Donike workshop on doping analysis It was planned to celebrate the 40th anniversary of the Cologne Workshop on Doping Analysis (from 1996 onwards referred to as the Manfred Donike Workshop), the conference that has been annually hosted in Cologne, Germany, since 1983, in-person in March 2022. Unfortunately, identical to 2021, 1 the developments concerning the COVID-19 crisis generated a situation incompatible with the planned event. Instead, the second time in a row, the Manfred Donike Workshop was conducted as a virtual conference, realized with an overwhelming online attendance of 400 international representatives of World Anti-Doping Agency (WADA)-accredited laboratories plus invited guests, and fantastic presentations and contributions of outstanding breadth and quality. The collection of articles compiled in this special issue of Drug Testing & Analysis reflects a selection of core topics of 2021/2022, including the Games of the XXXII Olympiad, the XVI Paralympic Games, the XXIV Olympic Winter Games, and 2022 Winter Paralympics, issues and solutions, future aspects, and new test methods as well as data on most diverse aspects of sports drug testing, which were thematized at the 2022 conference.Central topics of the 2022 conference can be largely subsumed under analytical aspects concerning steroidal substances and erythropoiesis-stimulating agents as well as blood transfusions, as well as investigations into the detection, characterization, and synthesis of metabolic products of drugs, including, for example, myostatin

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Detection of bazedoxifene, a selective estrogen receptor modulator, in human urine by liquid chromatography‐tandem mass spectrometry

Cited by 3 publications

References 15 publications

Annual banned‐substance review—Analytical approaches in human sports drug testing 2021/2022–

Annual banned‐substance review—Analytical approaches in human sports drug testing 2021/2022–

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The 40^th Manfred Donike workshop on doping analysis

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Detection of bazedoxifene, a selective estrogen receptor modulator, in human urine by liquid chromatography‐tandem mass spectrometry

Cited by 3 publications

References 15 publications

Annual banned‐substance review—Analytical approaches in human sports drug testing 2021/2022–

Annual banned‐substance review—Analytical approaches in human sports drug testing 2021/2022–

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The 40th Manfred Donike workshop on doping analysis

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The 40^th Manfred Donike workshop on doping analysis