Watch out for a revival of peginesatide in sports.
The erythropoietin-mimetic peptide (EMP) peginesatide belongs to the group of erythropoiesis-stimulating agents (ESAs) that are prohibited when misused in sports. Peginesatide is a synthetic pegylated homodimer of two cyclic 21-amino acid chains. It was approved for the treatment of anaemic patients with chronic kidney disease in the USA in 2012, but recalled in 2013 due to prevalent cases of acute severe anaphylactoid reactions and associated fatalities (0.02%). The drug was considered obsolete for athletes and part of the anti-doping scene lost sight of it. However, recent research indicates that the adverse events were not caused by the drug substance, but by the drug product formulated in multi-use vials. These vials contained comparably high levels of subvisible particles. Phenol was identified as a critical component of the drug formulation, which caused the release of histamine from mast cells. Tricky athletes might consider peginesatide a pharmacologically safe ESA in an appropriate formulation. In addition, other EMPs may get a second wind for therapy including misuse in sports. Therefore, it is very important to proceed in developing electrophoretic, immunological, and mass spectroscopic methods for detecting peginesatide and other EMPs in human urine and blood samples. Copyright © 2016 John Wiley & Sons, Ltd.
Institute of Physiology, University of Lübeck, D-23562, Lübeck, Germany.
Wolfgang
W
Jelkmann
D002986:Clinical Trials as Topic; D004300:Doping in Sports; D055808:Drug Discovery; D006397:Hematinics / Q000009:adverse effects / Q000097:blood* / Q000737:chemistry / Q000652:urine*; D006801:Humans; D006967:Hypersensitivity / Q000209:etiology; D010455:Peptides / Q000009:adverse effects / Q000097:blood* / Q000737:chemistry / Q000652:urine*; D015813:Substance Abuse Detection / Q000379:methods*
D006397:Hematinics; D010455:Peptides; C556270:peginesatide
EMP; doping; drug misuse; erythropoietin; formulation