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In vivo studies have shown that MIRCERA® stimulates erythropoiesis with a greater magnitude and duration of response than epoetin beta. The increase in mean reticulocyte count (an early marker of erythropoiesis) in mice after a single subcutaneous (SC) injection was higher with MIRCERA than an equivalent dose of epoetin beta (13% vs 7.8%).¹ The median duration of response was 3 days longer with MIRCERA compared with epoetin beta.¹

 

MIRCERA administered intravenously (IV) or SC is equally effective in stimulating erythropoiesis. In patients with chronic kidney disease (CKD) and anaemia, the reticulocyte count, (an indicator of erythropoietic activity) peaked at a median of 8 days after both IV and SC administration and returned to near-baseline values by day 21, with no difference in the time course for reticulocyte response between the two administration routes.²

 

The low clearance and long half-life of MIRCERA was demonstrated in erythropoiesis-stimulating agent (ESA)-naïve patients with CKD and anaemia who were on peritoneal dialysis: clearance was 0.49 and 0.90 mL/h/Kg and the mean half-life was 134 and 139 hours, after IV and SC administration of MIRCERA, respectively.² The mean half-life observed in this patient study is consistent with the results of a study in healthy volunteers, which demonstrated a half-life of 130 hours after IV and SC administration.³

 

The maximum serum concentrations, bioavailability and terminal elimination half-life of MIRCERA following SC administration in CKD patients is summarised in the table below.⁴

  

 

• MIRCERA has a longer half-life than traditional ESAs. The elimination half-life of MIRCERA after IV administration in patients with chronic kidney disease is (see Figure):
  • 27 times longer than the half-life of epoetin alfa IV ^4,5
  • 6 times longer than the half-life of darbepoetin alfa IV ^4,6

The pharmacokinetic parameters of MIRCERA are not affected by administration site or age of patient.^7,8

 

References:

 

1. Tare N, Pill J, Haselbeck A, et al. Preclinical pharmacodynamics and pharmacokinetics of CERA (continuous erythropoietin receptor activator), a new erythropoietic agent for anaemia management in patients with kidney disease [abstract]. Nephrol Dial Transplant. 2003;18(suppl 4):166. Abstract M526.
2. Macdougall IC, Robson R, Opatrna S, et al. Pharmacokinetics and pharmacodynamics of intravenous and subcutaneous Continuous Erythropoietin Receptor Activator (C.E.R.A.) in patients with chronic kidney disease. Clin J Am Soc Nephrol. 2006 doi:10.2215/CJN.00730306.
3. Dougherty FC, Reigner B, et al. C.E.R.A. (Continuous Erythropoietin Receptor Activator): dose-response, pharmacokinetics and tolerability in phase I multiple ascending dose studies. J Clin Oncol. 2004;22(suppl):603. Abstract 6692.
4. MIRCERA® Summary of Product Characteristics. F. Hoffmann-La Roche Ltd. 2007.
5. Eprex® Summary of Product Characteristics. Janssen-Cilag Ltd. 2006.
6. Aranesp® Summary of Product Characteristics. Amgen. 2006.
7. Fishbane S, Pannier A, Liogier X, et al. Pharmacokinetic (PK) properties of subcutaneous (SC) CERA (Continuous Erythropoietin Receptor Activator) are unaffected by administration site. Poster presentation at 38th Annual meeting of The American Society of Nephrology, Philadelphia, USA, 8–13 November 2005.
8. Chanu P, Gieschke R, Reigner B, Dougherty FC. Pharmacokinetic parameters of C.E.R.A. are not affected by age in patients with chronic kidney disease on dialysis. Poster presentation at European Renal Association – European Dialysis and Transplant Association XLIV Congress, Barcelona, Spain. 21–24 June 2007 (Poster SaP351).