MIRCERA.com

MIRCERA® stimulates erythropoiesis by the interaction with the erythropoietin receptor on progenitor cells in the bone marrow. MIRCERA is a continuous erythropoietin receptor activator that shows a different activity at the receptor level compared with other erythropoiesis-stimulating agents (ESAs):

• slower association to the receptor ¹
• slightly faster dissociation from the receptor ²
• lower receptor binding affinity ²
• longer half-life. ²

The reduced affinity of MIRCERA for the erythropoietin receptor allows continuous stimulation which achieves stable Hb levels in the target range.^2,3

MIRCERA has an approximate 50–100-fold lower binding affinity to the erythropoietin receptor than epoetin beta.¹ This lower binding affinity results in a delayed receptor mediated elimination. Consequently, MIRCERA is cleared very slowly from the human body which explains its long half-life.²

MIRCERA has the longest half-life of all ESAs; up to six times longer than darbepoetin alfa IV and up to 27 times longer than epoetin alfa IV (see Figure).^4–8 The extended half-life allows more sustained activation of erythropoietin receptor compared with epoetin beta.² Importantly, the half-life of MIRCERA is comparable following intravenous (IV) or subcutaneous (SC) administration.^5,8

Half-life of erythropoiesis-stimulating agents.^5–9

References:

1. Brandt M, Lanzendorfer M, Frische J, et al. Different receptor binding activity of C.E.R.A. (continuous erythropoietin receptor activator) compared with epoetin beta determined by surface plasmon resonance and competition assay on UT-7 cells. Nephrol Dial Transplant 2006;21(Suppl 4):iv9. Abstract SO018.
2. Jarsch M, Brandt M, Lanzendorfer M, Haselbeck A. Comparative erythropoietin receptor binding kinetics of C.E.R.A. and epoetin-beta determined by surface plasmon resonance and competition binding assay. Pharmacology. 2008;81:63–69.
3. Sulowicz W, Locatelli F, Ryckelynck J-P, et al. Once-monthly subcutaneous C.E.R.A. maintains stable haemoglobin control in patients with chronic kidney disease on dialysis and convert directly from epoetin one to three times weekly. Clin J Am Soc Nephrol. 2007;2:637 –646.
4. Aranesp^® Summary of Product Characteristics. Amgen. 2006
5. MIRCERA^® Summary of Product Characteristics. F. Hoffmann-La Roche Ltd. 2007.