Methoxy Polyethylene Glycol-Epoetin Beta (Mircera)
Mircera is a continuous erythropoietin receptor activator (CERA): epoetin beta conjugated to a large methoxy-PEG polymer, giving a very long half-life and monthly dosing for renal anaemia. Its stability made it a doping target, and it featured in cycling positives at the 2008 Tour de France. Prohibited by WADA at all times.
01 Overview
By attaching a single large PEG chain to epoetin beta, Mircera achieves a half-life of roughly a week, allowing once-monthly administration in chronic kidney disease. It interacts with the EPO receptor differently — slower association and dissociation — which is described as continuous receptor activation.\n\nSeveral riders tested positive for Mircera at the 2008 Tour de France after a detection assay was rapidly developed, demonstrating that even novel ESAs are catchable. The cardiovascular hazard profile is the ESA-class profile: thrombosis, hypertension and, in trials targeting higher haemoglobin, excess cardiovascular events.
02 Mechanism
The PEGylated epoetin beta binds the erythropoietin receptor with slow on/off kinetics, providing prolonged, continuous erythropoietic stimulation from a single infrequent dose.
03 Dosing
| Tier | Dose | Route | Notes |
|---|---|---|---|
| Renal anaemia (medical) | 0.6–1.2 mcg/kg | SubQ | Once every 2-4 weeks; titrated to haemoglobin |
| Maintenance (medical) | 50–360 mcg | IV | Monthly; medical use only |
04 Effects
| Effect | Magnitude | Evidence | |
|---|---|---|---|
| Long-lasting red cell mass expansionA single dose sustains erythropoiesis for weeks, raising haemoglobin and oxygen delivery. | Hb +1-2 g/dL | Clinical | |
| Reduced injection frequencyIts very long half-life allows once-monthly administration, improving convenience over EPO or darbepoetin. | Monthly dosing | Clinical |
05 Side effects
| Effect | Severity | Frequency | Evidence | Countermeasures |
|---|---|---|---|---|
| Thromboembolic eventsESA-class clotting risk: stroke, MI, DVT, PE, worsened by dehydration. | Life-threatening | Dose-dependent | Clinical | |
| HypertensionBlood pressure rise typical of ESAs. | Moderate | Common | Clinical |