Darbepoetin alfa

Identification

Name
Darbepoetin alfa
Accession Number
DB00012
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.

Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Haematopoietic growth factors
Protein Structure
Db00012
Protein Chemical Formula
C815H1317N233O241S5
Protein Average Weight
18396.1 Da
Sequences
>DB00012 sequence
APPRLICDSRVLERYLLEAKEAENITTGCAEHCSLNENITVPDTKVNFYAWKRMEVGQQA
VEVWQGLALLSEAVLRGQALLVNSSQPWEPLQLHVDKAVSGLRSLTTLLRALGAQKEAIS
PPDAASAAPLRTITADTFRKLFRVYSNFLRGKLKLYTGEACRTGDR
Download FASTA Format
Synonyms
  • Darbepoetin
  • Darbepoetin alfa
  • Darbepoetin alfa,recombinant
  • Darbepoetina alfa

Pharmacology

Pharmacology
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Indication

For the treatment of anemia (from renal transplants or certain HIV treatment)

Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
Contraindications & Blackbox Warnings
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Pharmacodynamics

Darbepoetin 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 action

Darbepoetin 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.

TargetActionsOrganism
AErythropoietin receptor
agonist
Humans
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half-life
Not Available
Clearance
Not Available
Adverse Effects
Medicalerrors
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Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbemaciclibThe risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Abemaciclib.
AbirateroneThe risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Abiraterone.
AfatinibThe risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Afatinib.
AldesleukinThe risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Aldesleukin.
AlectinibThe risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Alectinib.
AlemtuzumabThe risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Alemtuzumab.
AlitretinoinThe risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Alitretinoin.
AlpelisibThe risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Alpelisib.
AltretamineThe risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Altretamine.
AminoglutethimideThe risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Aminoglutethimide.
Interactions
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Food Interactions
  • Administer iron supplement. When initiating an erythropoiesis-stimulating agent, evaluate iron stores and start iron supplementation if indicated. Most patients with chronic kidney disease require iron supplementation while taking an erythropoiesis-stimulating agent.

Products

Products
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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AranespInjection, solutionIntravenous; SubcutaneousAmgen Europe B.V.2016-09-08Not applicableEU flag
AranespInjection, solution500 ug/1mLIntravenous; SubcutaneousAMGEN INC2006-06-07Not applicableUS flag
AranespSolution60 ug/1mLIntravenous; SubcutaneousAMGEN INC2006-09-11Not applicableUS flag
AranespInjection, solutionIntravenous; SubcutaneousAmgen Europe B.V.2016-09-08Not applicableEU flag
AranespInjection, solutionSubcutaneousAmgen Europe B.V.2016-09-08Not applicableEU flag
AranespInjection, solutionIntravenous; SubcutaneousAmgen Europe B.V.2016-09-08Not applicableEU flag
AranespInjection, solution150 ug/0.3mLIntravenous; SubcutaneousAMGEN INC2004-06-012010-02-16US flag
AranespSolution15 mcgIntravenous; SubcutaneousAmgenNot applicableNot applicableCanada flag
AranespSolution300 ug/1mLIntravenous; SubcutaneousAMGEN INC2006-08-14Not applicableUS flag
AranespInjection, solutionIntravenous; SubcutaneousAmgen Europe B.V.2016-09-08Not applicableEU flag

Categories

ATC Codes
B03XA02 — Darbepoetin alfa
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available

Chemical Identifiers

UNII
15UQ94PT4P
CAS number
209810-58-2

References

General References
Not Available
UniProt
P01588
Genbank
X02158
PubChem Substance
46504480
RxNav
283838
ChEMBL
CHEMBL1201566
Therapeutic Targets Database
DAP000800
PharmGKB
PA164743138
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Darbepoetin_alfa
AHFS Codes
  • 20:16.00 — Hematopoietic Agents

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedBasic ScienceRenal Anemia1
4CompletedPreventionAnemia / Chronic Renal Failure (CRF)1
4CompletedTreatmentAnemia3
4CompletedTreatmentAnemia of End Stage Renal Disease1
4CompletedTreatmentAnemia / Chemotherapy1
4CompletedTreatmentAnemia / Chronic Kidney Disease (CKD)1
4CompletedTreatmentAnemia / Neoplasms1
4CompletedTreatmentChronic Kidney Disease (CKD) / Kidney Diseases / Pre-Dialysis / Pre-ESRD / Renal Insufficiency,Chronic3
4CompletedTreatmentColorectal Cancers1
4CompletedTreatmentEnd Stage Renal Disease (ESRD)1

Pharmacoeconomics

Manufacturers
  • Amgen Inc.
Packagers
  • Amgen Inc.
  • Physicians Total Care Inc.
Dosage Forms
FormRouteStrength
Injection, solutionIntravenous; Parenteral
Injection, solutionIntravenous; Subcutaneous10 ug/0.4mL
Injection, solutionIntravenous; Subcutaneous100 ug/0.5mL
Injection, solutionIntravenous; Subcutaneous150 ug/0.3mL
Injection, solutionIntravenous; Subcutaneous200 ug/0.4mL
Injection, solutionIntravenous; Subcutaneous25 ug/0.42mL
Injection, solutionIntravenous; Subcutaneous300 ug/0.6mL
Injection, solutionIntravenous; Subcutaneous40 ug/.4mL
Injection, solutionIntravenous; Subcutaneous40 ug/0.4mL
Injection, solutionIntravenous; Subcutaneous500 ug/1mL
Injection, solutionIntravenous; Subcutaneous60 ug/0.3mL
Injection, solutionParenteral; Subcutaneous
SolutionIntravenous; Subcutaneous100 ug/1mL
SolutionIntravenous; Subcutaneous15 mcg
SolutionIntravenous; Subcutaneous150 ug/0.75mL
SolutionIntravenous; Subcutaneous200 ug/1mL
SolutionIntravenous; Subcutaneous200 mcg
SolutionIntravenous; Subcutaneous25 mcg
SolutionIntravenous; Subcutaneous25 ug/1mL
SolutionIntravenous; Subcutaneous300 ug/1mL
SolutionIntravenous; Subcutaneous325 mcg
SolutionIntravenous; Subcutaneous40 ug/1mL
SolutionIntravenous; Subcutaneous40 mcg
SolutionIntravenous; Subcutaneous500 mcg
SolutionIntravenous; Subcutaneous60 ug/1mL
SolutionIntravenous; Subcutaneous60 mcg
InjectionIntravenous; Subcutaneous
Injection, solutionParenteral
SolutionIntravenous; Subcutaneous100 mcg
SolutionIntravenous; Subcutaneous
SolutionIntravenous; Subcutaneous50 mcg
Injection
SolutionIntravenous; Subcutaneous120 mcg/0.5ml
SolutionIntravenous; Subcutaneous180 mcg/0.5ml
SolutionIntravenous; Subcutaneous20 mcg/0.5ml
SolutionIntravenous; Subcutaneous30 mcg/0.5ml
SolutionIntravenous; Subcutaneous40 mcg/0.5ml
SolutionIntravenous; Subcutaneous60 mcg/0.5ml
InjectionIntravenous
Injection, solutionIntravenous
Injection, solutionIntravenous; Subcutaneous
Injection, solutionSubcutaneous
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)Region
CA2165694No2003-03-182010-10-15Canada flag
CA2147124No2002-11-052014-08-16Canada flag

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)53 °CArakawa, T. et al., Biosci. Biotechnol. Biochem. 65:1321-1327 (2001)
hydrophobicity-0.188Not Available
isoelectric point8.75Not Available

Targets

Drugtargets
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Kind
Protein
Organism
Humans
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 som...
Gene Name
EPOR
Uniprot ID
P19235
Uniprot Name
Erythropoietin receptor
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]

Drug created on June 13, 2005 13:24 / Updated on April 23, 2021 04:04