Blood oxygenation and peripheral perfusion are pivotal factors to optimize intensity and length of the muscular activity. Enhancement and optimization of oxygen delivery to peripheral tissues is associated with a substantial improvement of the athletic performances, especially in endurance sports. Remarkable progresses in medical research promoted the introduction and commercialization of novel methods and molecules for the therapy of severe systemic pathologies, characterized by detrimental peripheral oxygenation. Unfortunately, the evident benefits of some promising classes of molecules propitiated the gradual diffusion to some sport disciplines, in form of doping. Aim of this review is to give further insights into new techniques of blood doping, chiefly focusing on blood transfusion, oxygen-carrying blood substitutes, synthetic haemoglobin allosteric modulators and administration of substances promoting synthesis and maturation of erythrocytes.