Hypoxia-inducible factor stabilizers and other small-molecule erythropoiesis-stimulating agents in current and preventive doping analysis

Drug Testing and Analysis
Simon BeuckMario Thevis

Abstract

Increasing the blood's capacity for oxygen transport by erythropoiesis-stimulating agents (ESAs) constitutes a prohibited procedure of performance enhancement according to the World Anti-Doping Agency (WADA). The advent of orally bio-available small-molecule ESAs such as hypoxia-inducible factor (HIF) stabilizers in the development of novel anti-anaemia therapies expands the list of potential ESA doping techniques. Here, the erythropoiesis-stimulating properties and doping relevance of experimental HIF-stabilizers, such as cobaltous chloride, 3,4-dihydroxybenzoic acid or GSK360A, amongst others, are discussed. The stage of clinical trials is reviewed for the anti-anaemia drug candidates FG-2216, FG-4592, GSK1278863, AKB-6548, and BAY85-3934. Currently available methods and strategies for the determination of selected HIF stabilizers in sports drug testing are based on liquid chromatography-electrospray ionization-tandem mass spectrometry (LC-ESI-MS/MS). For the support of further analytical assay development, patents claiming distinct compounds for the use in HIF-mediated therapies are evaluated and exemplary molecular structures of HIF stabilizers presented. Moreover, data concerning the erythropoiesis-enhancing effects of the...Continue Reading

References

Sep 1, 1990·The American Journal of Clinical Nutrition·R C JohnsonW B Rowe
Sep 1, 1990·Metabolism: Clinical and Experimental·V C DiasH G Parsons
Jan 1, 1989·Critical Reviews in Food Science and Nutrition·K Herrmann
Jan 20, 1995·The Journal of Biological Chemistry·G L Wang, G L Semenza
May 13, 1994·Journal of Chromatography. B, Biomedical Applications·K YoshiokaK Okuda
Nov 1, 1993·Kidney International·P H MaxwellP J Ratcliffe
Nov 11, 1999·Clinica Chimica Acta; International Journal of Clinical Chemistry·E CapristoG Gasbarrini
Mar 29, 2001·The Journal of Pharmacy and Pharmacology·D DimitrijevicA T Florence
Oct 13, 2001·Science·R K Bruick, S L McKnight
Sep 28, 2002·Proceedings of the National Academy of Sciences of the United States of America·Mircea IvanWilliam G Kaelin
Dec 20, 2002·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Michael S WiesenerKai-Uwe Eckardt
Apr 24, 2003·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Christina WarneckeKai-Uwe Eckardt
Jun 6, 2003·The Journal of Biological Chemistry·Maija HirsiläJohanna Myllyharju
Sep 6, 2003·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Shigehiko ImagawaMasayuki Yamamoto
Nov 1, 1958·Proceedings of the Society for Experimental Biology and Medicine·J E DAVIS, J P FIELDS
Jul 13, 2004·The Journal of Biological Chemistry·Rebecca J AppelhoffJonathan M Gleadle
Jul 24, 2004·The Journal of Biological Chemistry·Konstantin SalnikowKazimierz S Kasprzak
Oct 18, 2005·The Journal of Biological Chemistry·Ambreena SiddiqRajiv R Ratan
Oct 26, 2005·British Journal of Sports Medicine·G LippiG C Guidi
Dec 24, 2005·Proceedings of the National Academy of Sciences of the United States of America·Michal SafranWilliam G Kaelin
Jan 13, 2006·Proceedings of the National Academy of Sciences of the United States of America·Melanie J PercyFrank S Lee
Mar 7, 2006·Respiratory Physiology & Neurobiology·José A L CalbetRobert Boushel
Jan 1, 1934·The Biochemical Journal·P E Verkade, J Van Der Lee
Jun 10, 2006·Journal of the American Society of Nephrology : JASN·Wanja M BernhardtKai-Uwe Eckardt
Jun 20, 2006·Proceedings of the National Academy of Sciences of the United States of America·Michael A McDonoughChristopher J Schofield
Jun 29, 2006·Rapid Communications in Mass Spectrometry : RCM·Wilhelm SchänzerMario Thevis
Jul 26, 2006·Journal of Occupational Medicine and Toxicology·Giuseppe LippiGian Cesare Guidi
Aug 16, 2006·Bioorganic & Medicinal Chemistry Letters·Namal C WarshakoonMarlene Mekel
Aug 16, 2006·Bioorganic & Medicinal Chemistry Letters·Namal C WarshakoonStephen East

❮ Previous
Next ❯

Citations

Aug 13, 2013·Analytical and Bioanalytical Chemistry·Torben Pottgiesser, Yorck Olaf Schumacher
Sep 6, 2013·Pediatric Nephrology : Journal of the International Pediatric Nephrology Association·Bradley A Warady, Douglas M Silverstein
Jun 8, 2014·Journal of Pharmaceutical and Biomedical Analysis·Mario Thevis, Wilhelm Schänzer
Dec 19, 2013·Expert Opinion on Emerging Drugs·Jolanta Malyszko
Dec 17, 2015·Annual Review of Physiology·Sadeesh K Ramakrishnan, Yatrik M Shah
Jan 26, 2016·Journal of Pharmaceutical and Biomedical Analysis·C BuissonA Molina
Jul 1, 2015·Proceedings of the National Academy of Sciences of the United States of America·Sadeesh K RamakrishnanYatrik M Shah
Mar 15, 2013·Kidney International·Toshio MiyataCharles van Ypersele de Strihou
Dec 22, 2015·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Hermes Licea PerezChristopher A Evans
Mar 15, 2016·PM & R : the Journal of Injury, Function, and Rehabilitation·Stuart E WillickDaniel Eichner
Jul 22, 2014·Drug Testing and Analysis·Oliver KrugMario Thevis
Sep 17, 2013·Drug Testing and Analysis·Bastian Ebert, Wolfgang Jelkmann
Nov 29, 2013·Drug Testing and Analysis·Mario ThevisWilhelm Schänzer
Dec 29, 2013·Stem Cells Translational Medicine·Catherine E Forristal, Jean-Pierre Levesque
Jan 26, 2017·Molecular and Cellular Endocrinology·Olivier SalaminNicolas Leuenberger
Aug 29, 2016·Angiology·Gordon A A Ferns, Lamia Heikal
May 10, 2018·Toxicological Sciences : an Official Journal of the Society of Toxicology·Sabrina A RoccoJustin A Colacino
Aug 4, 2018·International Urology and Nephrology·Dengpiao XieMingquan Li
Jun 25, 2014·Molecules and Cells·Robin J RuthenborgJung-Whan Kim
Nov 13, 2019·Rapid Communications in Mass Spectrometry : RCM·Andre KnoopMario Thevis
Nov 28, 2019·Tissue Engineering. Part B, Reviews·Dheraj K TaheemEileen Gentleman
May 24, 2020·The FEBS Journal·James W WilsonSonia Rocha
May 22, 2020·Journal of Analytical Toxicology·Monica MazzarinoFrancesco Botrè
Aug 19, 2020·Drug Testing and Analysis·Christian GörgensMario Thevis
Mar 8, 2017·Drug Testing and Analysis·Adam T Cawley, John Keledjian
Oct 31, 2015·Nihon Naika Gakkai zasshi. The Journal of the Japanese Society of Internal Medicine·Norio Komatsu
Mar 21, 2017·Drug Testing and Analysis·Marie-Agnes PopotTerence S M Wan
Aug 26, 2020·Biomedical Chromatography : BMC·Laurie De WildePeter Van Eenoo
Feb 13, 2018·Chemical Science·Tzu-Lan YehChristopher J Schofield
Nov 4, 2020·Drug Testing and Analysis·Andre KnoopMario Thevis
Jun 20, 2015·Circulation Research·Tammie Bishop, Peter J Ratcliffe

❮ Previous
Next ❯

Related Concepts

Related Feeds

Addiction

This feed focuses mechanisms underlying addiction and addictive behaviour including heroin and opium dependence, alcohol intoxication, gambling, and tobacco addiction.

Anemia

Anemia develops when your blood lacks enough healthy red blood cells. Anemia of inflammation (AI, also called anemia of chronic disease) is a common, typically normocytic, normochromic anemia that is caused by an underlying inflammatory disease. Here is the latest research on anemia.