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1071 details
Primary information
ThPP IDTh1013
Therapeutic Peptide/Protein NameEpoetin alfa
SequenceAPPRLICDSRVLERYLLEAKEAENITTGCAEHCSLNENITVPDTKVNFYA view full sequnce in fasta
Functional ClassificationIb
Molecular Weight18396.1
Chemical FormulaC815H1317N233O241S5
Isoelectric Point8.75
HydrophobicityN.A.
Melting Point (℃)53
Half LifeN.A.
DescriptionIt is recombinant human erythropoietin which is produced by CHO cells.
Indication/DiseaseFor treatment of anemia (from renal transplants or certain HIV treatment).
PharmacodynamicsUsed 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 ActionBinding 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.
ToxicityN.A.
MetabolismN.A.
AbsorptionN.A.
Volume of DistributionN.A.
Clearance20.2 ± 15.9 mL/h/kg [150 Units/kg SC TIW, Week 1 when anemic cancer patients were receiving chemotherapy]
CategoriesHematinics
Patents NumberCA1339047
Date of Issue27/05/97
Date of Expiry27/05/14
Drug InteractionN.A.
TargetErythropoietin receptor
Information of corresponding available drug in the market
Brand NameBinocrit
CompanySandoz
Brand DiscriptionBinocrit is a solution administered as an injection. It is available in pre-filled syringes that contain 1,000-40,000 international units (IU) of the active substance, epoetin alfa
Prescribed forTreatment of symptomatic anaemia associated with chronic renal failure (CRF) in adult and paediatric patients
Chemical NameN.A.
Formulation1000 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
Physcial AppearnceClear colourless solution
Route of AdministrationSubcutaneous and Intravenous infusion
Recommended DosageFor 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).
ContraindicationHypersensitivity, 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 EffectsThe 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 Linkhttps://www.medicines.org.uk/emc/medicine/21625
PubMed ID20369312, 18208642
3-D StructureTh1013 (View) or (Download)