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| Primary information |
|---|
| ID | 10846 |
| Therapeutic ID | Th1209 |
| Protein Name | Methoxy polyethylene glycol-epoetin beta |
| Sequence | NA
|
| Molecular Weight | 60,000 |
| Chemical Formula | NA |
| Isoelectric Point | NA |
| Hydrophobicity | NA |
| Melting point | NA |
| Half-life | In CKD patients on peritoneal dialysis with IV administration: 134 ± 65 hours In CKD patients on peritoneal dialysis with SC administration: 139 ± 67 hours |
| Description | Methoxy polyethylene glycol-epoetin beta is a chemically synthesised Erythropoiesis Stimulating Agent (ESA) with a much longer half-life than erythropoietin. It is produced by recombinant DNA technology in Chinese Hamster Ovary (CHO) cells and differs from erythropoietin through the integration of an amide bond between either the N- terminal amino group or the ε-amino group of lysine, predominantly Lys52 and Lys45 and methoxy polyethylene glycol butanoic acid. This results in a molecular weight of approximately 60 kDa with the polyethylene glycol-moiety having an approximate molecular weight of 30 kDa. The dosage strength in μg indicates the quantity of the protein moiety of the methoxy polyethylene glycol-epoetin beta molecule without consideration of glycosylation. Methoxy polyethylene glycol-epoetin beta was approved (as Mircera) for use in Europe in July 2007 by the European Commission, in September 2007 by the Swissmedic, and in November 2007 by the U.S. Food and Drug Administration for use in the United States. |
| Indication/Disease | For the treatment of patients with anaemia associated with chronic kidney disease. |
| Pharmacodynamics | Following a single-dose of Mircera in CKD patients, the onset of hemoglobin increase (defined as an increase > 0.4 g/dL from baseline) was observed 7 to 15 days following initial dose administration |
| Mechanism of Action | Mircera is an erythropoietin receptor activator with greater activity in vivo as well as increased half-life, in contrast to erythropoietin. A primary growth factor for erythroid development, erythropoietin is produced in the kidney and released into the bloodstream in response to hypoxia. In responding to hypoxia, erythropoietin interacts with erythroid progenitor cells to increase red cell production. Production of endogenous erythropoietin is impaired in patients with CKD and erythropoietin deficiency is the primary cause of their anemia. |
| Toxicity | Overdosage can cause severe hypertension. |
| Metabolism | Not metabolized. |
| Absorption | Administered parenterally (subcutaneous or IV) therefore not absorbed. |
| ~94.74 ml/kg |
| Clearance | In CKD patients on peritoneal dialysis : 0.49 ± 0.18 mL/hr/kg |
| Categories | NA |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | Lenalidomide, Nandrolone phenpropionate, Thalidomide |
| Target | Erythropoietin receptor |
| Brand Name | Mircera |
| Company | Genentech, Inc. |
| Brand Description | Genentech, Inc. |
| Prescribed For | Mircera is indicated for the treatment of anemia associated with chronic kidney disease (CKD) in adult patients on dialysis and patients not on dialysis. |
| Chemical Name | NA |
| Formulation | 30 mcg, 50 mcg, 75 mcg, 100 mcg, 120 mcg, 150 mcg, 200 mcg, or 250 mcg in 0.3 mL |
| Physical Appearance | solution for injection |
| Route of Administration | Intravenous |
| Recommended Dosage | Individualize dosing and use the lowest dose of Mircera sufficient to reduce the need for RBC transfusions |
| Contraindication | Uncontrolled hypertension; Pure red cell aplasia (PRCA) that begins after treatment with Mircera or other erythropoietin protein drugs; History of serious or severe allergic reactions to Mircera (e.g. anaphylactic reactions, angioedema, bronchospasm, skin rash, and urticaria). |
| Side Effects | Increased Mortality, Myocardial Infarction, Stroke, and Thromboembolism; Increased mortality and/or tumor progression in patients with cancer; Hypertension; Seizures; Pure red cell aplasia; Serious allergic reactions. |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |