|
| Primary information |
|---|
| ID | 10071 |
| Therapeutic ID | Th1013 |
| Protein Name | Epoetin alfa |
| Sequence | >Th1013_Epoetin_alfa
APPRLICDSRVLERYLLEAKEAENITTGCAEHCSLNENITVPDTKVNFYAWKRMEVGQQAVEVWQGLALLSEAVLRGQALLVNSSQPWEPLQLHVDKAVSGLRSLTTLLRALGAQKEAISPPDAASAAPLRTITADTFRKLFRVYSNFLRGKLKLYTGEACRTGDR
|
| Molecular Weight | 18396.1 |
| Chemical Formula | C815H1317N233O241S5 |
| Isoelectric Point | 8.75 |
| Hydrophobicity | NA |
| Melting point | 53 |
| Half-life | 4 hours in healthy volunteers receiving an intravenous injection |
| Description | It is recombinant human erythropoietin which is produced by CHO cells. |
| Indication/Disease | For treatment of anemia (from renal transplants or certain HIV treatment). |
| Pharmacodynamics | Used in the treatment of anemia and involved in the regulation of erythrocyte differentiation and maintenance of a physiological level of circulating erythrocyte mass. |
| Mechanism of Action | Binding of erythropoietin to the erythropoietin receptor leads to receptor dimerization which facilitates activation of JAK-STAT signaling pathways within the cytosol. Activated STAT (signal transducers and activators of transcription) proteins are then translocated to the nucleus where they serve as transcription factors which regulate the activation of specific genes involved in cell division or differentiation. |
| Toxicity | Overdose from epoetin alfa include signs and symptoms associated with an excessive and/or rapid increase in hemoglobin concentration, including cardiovascular events. Patients with suspected or known overdose should be monitored closely for cardiovascular events and hematologic abnormalities. |
| Metabolism | Binding of erythropoietin and epoetin alfa to EPO-R leads to cellular internalization, which involves the degradation of the ligand. Erythropoietin and epoetin alfa may also be degraded by the reticuloendothelial scavenging pathway or lymphatic system |
| Absorption | Bioavailability is 20-40% |
| 40–63.80 mL/kg |
| Clearance | 20.2 ± 15.9 mL/h/kg [150 Units/kg SC TIW, Week 1 when anemic cancer patients were receiving chemotherapy] |
| Categories | Amino Acids, Peptides, and Proteins, Antianemic Preparations, Biological Factors, Blood and Blood Forming Organs, Colony-Stimulating Factors, Cytokines, Erythropoiesis-Stimulating Agents, Erythropoietin, genetics, Glycoproteins, Hematinics, Hematologic Agents, Hematopoietic Cell Growth Factors, Increased Erythroid Cell Production, Intercellular Signaling Peptides and Proteins, Peptides, Proteins |
| Patents Number | CA1339047 |
| Date of Issue | 27-May-1997 |
| Date of Expiry | 27-May-2014 |
| Drug Interaction | NA |
| Target | Erythropoietin receptor |
| Brand Name | Binocrit |
| Company | Sandoz |
| Brand Description | Sandoz |
| Prescribed For | Treatment of symptomatic anaemia associated with chronic renal failure (CRF) in adult and paediatric patients |
| Chemical Name | NA |
| Formulation | 1000 IU/0.5 ml means that each ml of solution contains 2000 IU of epoetin alfa corresponding to 16.8 micrograms per ml. One pre-filled syringe of 0.5 ml contains 1000 international units (IU) corresponding to 8.4 micrograms epoetin alfa |
| Physical Appearance | Clear colourless solution |
| Route of Administration | Subcutaneous and Intravenous infusion |
| Recommended Dosage | For less than 10 kg of weight usual maintainence dose is 75-150 (IU/kg given 3x/week). For 10-30 kg weight usual maintainence dose is 60-150 (IU/kg given 3x/week). For more than 30 kg weight usual maintainence dose is 30-100 (IU/kg given 3x/week). |
| Contraindication | Hypersensitivity, uncontrooled hypertension, Patients who develop Pure Red Cell Aplasia (PRCA) following treatment with any erythropoietin should not receive Binocrit, Patients who develop Pure Red Cell Aplasia (PRCA) following treatment with any erythropoetin. |
| Side Effects | The most frequent adverse reaction during treatment with epoetin alfa is a dose-dependent increase in blood pressure or aggravation of existing hypertension in cancer patients and in chronic renal failure patients. |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |