1. Epoetin alfa Drugbank ID : DB00016
Protein chemical formula : C815H1317N233O241S5
Protein average weight :

2. Description : Indication : Pharmacodynamics :
Human erythropoietin (recombinant), produced by CHO cells.
Indication :
For treatment of anemia (from renal transplants or certain HIV treatment)
Pharmacodynamics :
Used in the treatment of anemia. Involved in the regulation of erythrocyte differentiation and the maintenance of a physiological level of circulating erythrocyte mass.

3. 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.

4. Clearance : Targets : Affected organisms :
20.2 +/ mL/h/kg [150 Units/kg SC TIW, Week 1 when anemic cancer patients were receiving chemotherapy]
23.6 +/- 9.5 mL/h/kg [150 Units/kg SC TIW, Week 3 when anemic cancer patients were not receiving chemotherapy]
9.2 +/- 4.7 mL/h/kg [40,000 Units/kg SC TIW, Week 1 when anemic cancer patients were receiving chemotherapy]
13.9 +/- 7.6 mL/h/kg [40,000 Units/kg SC TIW, Week 3 when anemic cancer patients were not receiving chemotherapy] .
Targets :
Erythropoietin receptor
Affected organisms :
Humans and other mammals

5. Categories : Patents : Sequence : Hematinics and Anti-anemic Agents
Country Patent Number Approved Expires
Canada
Sequence :
APPRLICDSRVLERYLLEAKEAENITTGCAEHCSLNENITVPDTKVNFYAWKRMEVGQQAVEVWQGLALLSEAVLRGQALLVNSSQPWEPLQLHVDKAVSGLRSLTTLLRALGAQKEAISPPDAASAAPLRTITADTFRKLFRVYSNFLRGKLKLYTGEACRTGDR

6. Brands : Binocrit
Company : Sandoz
Description : Binocrit is a solution for injection. It is available in pre-filled syringes that contain between 1,000 and 40,000 international units (IU) of the active substance, epoetin alfa
Used for/Prescribed for : Treatment of symptomatic anaemia associated with chronic renal failure (CRF) in adult and paediatric patients
Formulation : 1000 IU/0.5 ml: Each ml of solution contains 2000 IU of epoetin alfa* corresponding to 16.8 micrograms per ml. 1 pre-filled syringe of 0.5 ml contains 1000 international units (IU) corresponding to 8.4 micrograms epoetin alfa
Form : Clear colourless solution
Route of administration : subcutaneous and intravenous injection
Dosage : for less than 10 kg of weight usual maintainence dose is (IU/kg given 3x/week). For kg weight usual maintainence dose is (IU/kg given 3x/week). For more than 30 kg weight usual maintainence dose is (IU/kg given 3x/week)

7. 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 erythropoietin should not receive Binocrit Side effects : in cancer patients and in chronic renal failure patients the most frequent adverse reaction during treatment with epoetin alfa is a dose-dependent increase in blood pressure or aggravation of existing hypertension. Other common adverse reactions observed in clinical trials of epoetin alfa are deep vein thrombosis, pulmonary embolism, seizures, diarrhoea, nausea, headache, influenza like illness, pyrexia, rash, and vomiting. Influenza like illness including headaches, arthralgia, myalgia, and pyrexia may occur especially at the start of treatment. Drug interaction : There is no evidence that treatment with epoetin alfa alters the metabolism of other medicinal products. However, since cyclosporin is bound by red blood cells there is potential for a substance interaction. If epoetin alfa is given concomitantly with cyclosporin, blood levels of cyclosporin should be monitored and the dose of cyclosporin adjusted as the haematocrit rises.

8. References : https://www. medicines. org