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 GATA inhibitors K7174 and K11706 as well as the lipidic small‐molecule ESA PBI‐1402 are elucidated the context of doping analysis. Copyright © 2012 John Wiley & Sons, Ltd.