Roxadustat is a medicinal substance for the treatment of certain types of anemia, is an inhibitor of prolyl hydroxylase HIF and stimulates the endogenous production of erythropoietin and the production of hemoglobin and red blood cells, which led the World Anti-Doping Agency WADA to include it on the list of prohibited substances since 2011, in the category of EPO (which promotes blood oxygenation ).

In reality, we don’t know exactly how or to what extent this substance can help an athlete, and we don’t know what type of athletes will use it.

“The substance has been categorically banned since 2011, it was known, the drug is completely prohibited for administration to athletes because it can lead to an increase in sports performance,” Mihaela Dobranici, vice president of the Sports Medicine Society, told Digi 24. .

Dobranich says that such a drug is available on the Romanian market.

Instead, pharmacist Beatrice Speteanu tells News.ro that there are no medicines in Romania that contain the active substance roxadustat, the one for which Simona Halep was found positive.

The pharmacist explained that roxadustat is a synthetic substance that acts as an enzyme and stimulates the oxygenation of the blood, and at the European level there are medicines that contain this substance, used especially in the case of people with kidney problems, and which are approved, but only available on prescription.

“I have known for a long time that there is erythropietin in our country and there are many athletes who use ampoules to increase endurance during training. 20 years have passed. It’s the equivalent of erythropoietin here, and I even know athletes who use erythropoietin for energy because it increases red blood cell production, and by increasing red blood cell production, you get more oxygen, better oxygenation of the blood, so it literally increases endurance during exercise,” said he is Beatriz Speteanu for News.ro.

What is written in the package insert for this medicine:

• Roxadustat is a hypoxia-inducible factor, prolyl hydroxylase inhibitor (HIF-PHI).
• The activity of HIF-PH enzymes controls the intracellular levels of HIF, a transcription factor that regulates the expression of genes involved in erythropoiesis. Activation of the HIF pathway is important in the adaptive response to hypoxia to increase red blood cell production.
• By reversible inhibition of HIF-PH, roxadustat stimulates a coordinated erythropoietic response that includes an increase in endogenous plasma erythropoietin (EPO), activation of iron transport proteins, and downregulation of hepcidin (an iron-regulating protein that is elevated during BCR inflammation). ).
• This leads to an improvement in the bioavailability of iron, an increase in the production of hemoglobin and an increase in the mass of erythrocytes

Removal from the body

• The mean effective half-life (t1/2) of roxadustat is approximately 15 hours in patients with symptomatic anemia due to chronic kidney disease (CKD).
• The apparent total clearance (CL/F) of roxadustat is 1.1 L/h in BCR patients not on dialysis and 1.4 L/h in BCR patients on dialysis.
• Roxadustat and its metabolites are not significantly removed during hemodialysis.
• After oral administration of radiolabeled roxadustat to healthy volunteers, the average excretion of radioactivity was 96% (50% in faeces, 46% in urine).
• With feces, 28% of the dose was excreted in the form of unchanged roxadustat. Less than 2% of the dose was identified in urine as unchanged roxadustat.