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Identification
NameDarbepoetin alfa
Accession NumberDB00012  (BTD00032, BIOD00032)
TypeBiotech
GroupsApproved, Investigational
Description

Human erythropoietin with 2 aa substitutions to enhance glycosylation (5 N-linked chains), 165 residues (MW=37 kD). Produced in Chinese hamster ovary (CHO) cells by recombinant DNA technology.

Protein structureDb00012
Related Articles
Protein chemical formulaC815H1317N233O241S5
Protein average weight18396.1 Da
Sequences
>DB00012 sequence
APPRLICDSRVLERYLLEAKEAENITTGCAEHCSLNENITVPDTKVNFYAWKRMEVGQQA
VEVWQGLALLSEAVLRGQALLVNSSQPWEPLQLHVDKAVSGLRSLTTLLRALGAQKEAIS
PPDAASAAPLRTITADTFRKLFRVYSNFLRGKLKLYTGEACRTGDR
Download FASTA Format
Synonyms
Darbepoetin
Darbepoetin alfa,recombinant
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Aranespinjection, solution150 ug/.3mLintravenous; subcutaneousAmgen Inc2006-09-11Not applicableUs
Aranespsolution25 ug/mLintravenous; subcutaneousAmgen Inc2006-09-11Not applicableUs
Aranespinjection, solution300 ug/.6mLintravenous; subcutaneousAmgen Inc2006-08-14Not applicableUs
Aranespinjection, solution100 ug/.5mLintravenous; subcutaneousAmgen Inc2006-08-14Not applicableUs
Aranespsolution300 ug/mLintravenous; subcutaneousAmgen Inc2006-08-14Not applicableUs
Aranespinjection, solution60 ug/.3mLintravenous; subcutaneousAmgen Inc2006-08-14Not applicableUs
Aranespinjection, solution10 ug/.4mLintravenous; subcutaneousAmgen Inc2006-08-26Not applicableUs
Aranespinjection, solution40 ug/.4mLintravenous; subcutaneousAmgen Inc2006-08-14Not applicableUs
Aranespinjection, solution25 ug/.42mLintravenous; subcutaneousAmgen Inc2006-08-26Not applicableUs
Aranespsolution200 ug/mLintravenous; subcutaneousAmgen Inc2006-09-11Not applicableUs
Aranespsolution150 ug/.75mLintravenous; subcutaneousAmgen Inc2006-09-11Not applicableUs
Aranespsolution100 ug/mLintravenous; subcutaneousAmgen Inc2006-09-11Not applicableUs
Aranespinjection, solution500 ug/mLintravenous; subcutaneousAmgen Inc2006-06-07Not applicableUs
Aranespsolution60 ug/mLintravenous; subcutaneousAmgen Inc2006-09-11Not applicableUs
Aranespinjection, solution200 ug/.4mLintravenous; subcutaneousAmgen Inc2006-08-14Not applicableUs
Aranespsolution40 ug/mLintravenous; subcutaneousAmgen Inc2006-09-11Not applicableUs
Aranesp -(hsa-free)solution500 mcgintravenous; subcutaneousAmgen Canada Inc2002-08-132015-08-04Canada
Aranesp -(hsa-free)solution40 mcgintravenous; subcutaneousAmgen Canada Inc2014-03-12Not applicableCanada
Aranesp -(hsa-free)solution100 mcgintravenous; subcutaneousAmgen Canada Inc2014-05-07Not applicableCanada
Aranesp -(hsa-free)solution100 mcgintravenous; subcutaneousAmgen Canada Inc2013-12-11Not applicableCanada
Aranesp -(hsa-free)solution15 mcgintravenous; subcutaneousAmgen Canada IncNot applicableNot applicableCanada
Aranesp -(hsa-free)solution200 mcgintravenous; subcutaneousAmgen Canada Inc2002-08-132015-08-04Canada
Aranesp -(hsa-free)solution25 mcgintravenous; subcutaneousAmgen Canada Inc2013-08-16Not applicableCanada
Aranesp -(hsa-free)solution100 mcgintravenous; subcutaneousAmgen Canada Inc2002-08-202015-08-04Canada
Aranesp -(hsa-free)solution500 mcgintravenous; subcutaneousAmgen Canada Inc2013-11-04Not applicableCanada
Aranesp -(hsa-free)solution500 mcgintravenous; subcutaneousAmgen Canada IncNot applicableNot applicableCanada
Aranesp -(hsa-free)solution40 mcgintravenous; subcutaneousAmgen Canada Inc2002-08-132015-08-04Canada
Aranesp -(hsa-free)solution500 mcgintravenous; subcutaneousAmgen Canada Inc2014-05-05Not applicableCanada
Aranesp -(hsa-free)solution25 mcgintravenous; subcutaneousAmgen Canada Inc2002-08-132015-08-04Canada
Aranesp -(hsa-free)solution500 mcgintravenous; subcutaneousAmgen Canada Inc2014-04-21Not applicableCanada
Aranesp -(hsa-free)solution500 mcgintravenous; subcutaneousAmgen Canada IncNot applicableNot applicableCanada
Aranesp -(hsa-free)solution500 mcgintravenous; subcutaneousAmgen Canada Inc2014-02-24Not applicableCanada
Aranesp -(hsa-free)solution200 mcgintravenous; subcutaneousAmgen Canada Inc2014-02-10Not applicableCanada
Aranesp -(hsa-free)solution40 mcgintravenous; subcutaneousAmgen Canada IncNot applicableNot applicableCanada
Aranesp -(hsa-free)solution200 mcgintravenous; subcutaneousAmgen Canada Inc2014-04-03Not applicableCanada
Aranesp -(hsa-free)solution200 mcgintravenous; subcutaneousAmgen Canada Inc2014-03-26Not applicableCanada
Aranesp -(hsa-free)solution325 mcgintravenous; subcutaneousAmgen Canada IncNot applicableNot applicableCanada
Aranesp -(hsa-free)solution100 mcgintravenous; subcutaneousAmgen Canada Inc2014-03-03Not applicableCanada
Aranesp -(hsa-free)solution200 mcgintravenous; subcutaneousAmgen Canada Inc2014-01-27Not applicableCanada
Aranesp -(hsa-free)solution60 mcgintravenous; subcutaneousAmgen Canada IncNot applicableNot applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII15UQ94PT4P
CAS number209810-58-2
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of anemia (from renal transplants or certain HIV treatment)
PharmacodynamicsDarbepoetin alfa is used in the treatment of anemia. It is involved in the regulation of erythrocyte differentiation and the maintenance of a physiological level of circulating erythrocyte mass.
Mechanism of actionDarbepoetin alfa stimulates erythropoiesis by the same mechanism as endogenous erythropoietin. Erythropoietin interacts with progenitor stem cells to increase red cell production. 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.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
Manufacturers
  • Amgen Inc.
Packagers
Dosage forms
FormRouteStrength
Injection, solutionintravenous; subcutaneous10 ug/.4mL
Injection, solutionintravenous; subcutaneous100 ug/.5mL
Injection, solutionintravenous; subcutaneous150 ug/.3mL
Injection, solutionintravenous; subcutaneous200 ug/.4mL
Injection, solutionintravenous; subcutaneous25 ug/.42mL
Injection, solutionintravenous; subcutaneous300 ug/.6mL
Injection, solutionintravenous; subcutaneous40 ug/.4mL
Injection, solutionintravenous; subcutaneous500 ug/mL
Injection, solutionintravenous; subcutaneous60 ug/.3mL
Solutionintravenous; subcutaneous100 ug/mL
Solutionintravenous; subcutaneous150 ug/.75mL
Solutionintravenous; subcutaneous200 ug/mL
Solutionintravenous; subcutaneous25 ug/mL
Solutionintravenous; subcutaneous300 ug/mL
Solutionintravenous; subcutaneous40 ug/mL
Solutionintravenous; subcutaneous60 ug/mL
Solutionintravenous; subcutaneous100 mcg
Solutionintravenous; subcutaneous15 mcg
Solutionintravenous; subcutaneous200 mcg
Solutionintravenous; subcutaneous25 mcg
Solutionintravenous; subcutaneous325 mcg
Solutionintravenous; subcutaneous40 mcg
Solutionintravenous; subcutaneous500 mcg
Solutionintravenous; subcutaneous60 mcg
Prices
Unit descriptionCostUnit
Aranesp (Albumin Free) 150 mcg/0.75ml Solution (1 Box = Four 0.75ml Vials)3902.75USD box
Aranesp (Albumin Free) 100 mcg/0.5ml Solution (1 Box = Four 0.5ml Syringes)2601.83USD box
Aranesp (Albumin Free) 100 mcg/ml Solution Four 1ml Vials Per Box2601.83USD box
Aranesp (Albumin Free) 300 mcg/ml vial1951.37USD vial
Aranesp 300 mcg/ml vial1876.32USD ml
Aranesp 200 mcg/ml vial1250.88USD ml
Aranesp 100 mcg/ml vial625.44USD ml
Aranesp (Albumin Free) 60 mcg/ml vial390.31USD vial
Aranesp 60 mcg/ml vial375.3USD ml
Aranesp 40 mcg/ml vial250.2USD ml
Aranesp (Albumin Free) 25 mcg/ml vial162.61USD vial
Aranesp 25 mcg/ml vial156.36USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2147124 No2002-11-052014-08-16Canada
CA2165694 No2003-03-182010-10-15Canada
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point53 °CArakawa, T. et al., Biosci. Biotechnol. Biochem. 65:1321-1327 (2001)
hydrophobicity-0.188Not Available
isoelectric point8.75Not Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesB03XA02
AHFS Codes
  • 20:16.00
PDB Entries
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
LenalidomideDarbepoetin alfa may increase the thrombogenic activities of Lenalidomide.
Nandrolone phenpropionateNandrolone phenpropionate may increase the stimulatory activities of Darbepoetin alfa.
ThalidomideDarbepoetin alfa may increase the thrombogenic activities of Thalidomide.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Identical protein binding
Specific Function:
Receptor for erythropoietin. Mediates erythropoietin-induced erythroblast proliferation and differentiation. Upon EPO stimulation, EPOR dimerizes triggering the JAK2/STAT5 signaling cascade. In some cell types, can also activate STAT1 and STAT3. May also activate the LYN tyrosine kinase.Isoform EPOR-T acts as a dominant-negative receptor of EPOR-mediated signaling.
Gene Name:
EPOR
Uniprot ID:
P19235
Molecular Weight:
55064.725 Da
References
  1. LaMontagne KR, Butler J, Marshall DJ, Tullai J, Gechtman Z, Hall C, Meshaw A, Farrell FX: Recombinant epoetins do not stimulate tumor growth in erythropoietin receptor-positive breast carcinoma models. Mol Cancer Ther. 2006 Feb;5(2):347-55. [PubMed:16505108 ]
  2. Kokhaei P, Abdalla AO, Hansson L, Mikaelsson E, Kubbies M, Haselbeck A, Jernberg-Wiklund H, Mellstedt H, Osterborg A: Expression of erythropoietin receptor and in vitro functional effects of epoetins in B-cell malignancies. Clin Cancer Res. 2007 Jun 15;13(12):3536-44. [PubMed:17575216 ]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on April 28, 2016 16:30