Darbepoetin alfa

Identification

Summary

Darbepoetin alfa is a recombinant form of human erythropoietin used to increase differentiation of progenitor cells to red blood cells in the treatment of anemia.

Brand Names
Aranesp
Generic Name
Darbepoetin alfa
DrugBank Accession Number
DB00012
Background

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

Indication

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

Pharmacology
Reduce drug development failure rates
Build, train, & validate machine-learning models
with evidence-based and structured datasets.
See how
Build, train, & validate predictive machine-learning models with structured datasets.
See how
Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
Avoid life-threatening adverse drug events
Improve clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.
Learn more
Avoid life-threatening adverse drug events & improve clinical decision support.
Learn more
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
Adverseeffects
Improve decision support & research outcomes
With structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.
Learn more
Improve decision support & research outcomes with our structured adverse effects data.
Learn more
Toxicity

Not Available

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
Identify potential medication risks
Easily compare up to 40 drugs with our drug interaction checker.
Get severity rating, description, and management advice.
Learn more
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

Products2
Drug product information from 10+ global regions
Our datasets provide approved product information including:
dosage, form, labeller, route of administration, and marketing period.
Access now
Access drug product information from over 10 global regions.
Access now
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AranespInjection, solution100 μgIntravenous; SubcutaneousAmgen Europe B.V.2016-09-08Not applicableEU flag
AranespInjection, solution300 μgIntravenous; SubcutaneousAmgen Europe B.V.2016-09-08Not applicableEU flag
AranespInjection, solution60 μgIntravenous; SubcutaneousAmgen Europe B.V.2016-09-08Not applicableEU flag
AranespInjection, solution150 μgIntravenous; SubcutaneousAmgen Europe B.V.2016-09-08Not applicableEU flag
AranespInjection, solution30 μgIntravenous; SubcutaneousAmgen Europe B.V.2016-09-08Not applicableEU flag
AranespInjection, solution30 μgIntravenous; SubcutaneousAmgen Europe B.V.2016-09-08Not applicableEU flag
AranespInjection, solution100 ug/0.5mLIntravenous; SubcutaneousAMGEN INC2003-07-232010-02-16US flag
AranespSolution100 mcg / mLIntravenous; SubcutaneousAmgen2014-05-07Not applicableCanada flag
AranespSolution60 ug/1mLIntravenous; SubcutaneousAMGEN INC2006-09-11Not applicableUS flag
AranespInjection, solution300 μgSubcutaneousAmgen 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
Affected organisms
  • Humans and other mammals

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

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedBasic ScienceRenal Anemia1
4CompletedPreventionAnemia / Renal Failure, Chronic Renal Failure1
4CompletedTreatmentAnemia3
4CompletedTreatmentAnemia of Chronic Kidney Disease1
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 Carcinoma (CRC)1

Pharmacoeconomics

Manufacturers
  • Amgen Inc.
Packagers
  • Amgen Inc.
  • Physicians Total Care Inc.
Dosage Forms
FormRouteStrength
Injection, solutionIntravenous; Parenteral10 MCG
Injection, solutionIntravenous; Parenteral100 MCG
Injection, solutionIntravenous; Parenteral130 MCG
Injection, solutionIntravenous; Parenteral15 MCG
Injection, solutionIntravenous; Parenteral150 MCG
Injection, solutionIntravenous; Parenteral20 MCG
Injection, solutionIntravenous; Parenteral25 MCG
Injection, solutionIntravenous; Parenteral30 MCG
Injection, solutionIntravenous; Parenteral300 MCG
Injection, solutionIntravenous; Parenteral40 MCG
Injection, solutionIntravenous; Parenteral50 MCG
Injection, solutionIntravenous; Parenteral500 MCG
Injection, solutionIntravenous; Parenteral60 MCG
Injection, solutionIntravenous; Parenteral80 MCG
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; Subcutaneous200 μg
Injection, solutionIntravenous; Subcutaneous25 ug/0.42mL
Injection, solutionIntravenous; Subcutaneous300 ug/0.6mL
Injection, solutionIntravenous; Subcutaneous40 ug/0.4mL
Injection, solutionIntravenous; Subcutaneous40 ug/.4mL
Injection, solutionIntravenous; Subcutaneous500 ug/1mL
Injection, solutionIntravenous; Subcutaneous60 ug/0.3mL
Injection, solutionParenteral; Subcutaneous10 MCG
Injection, solutionParenteral; Subcutaneous100 MCG
Injection, solutionParenteral; Subcutaneous15 MCG
Injection, solutionParenteral; Subcutaneous150 MCG
Injection, solutionParenteral; Subcutaneous20 MCG
Injection, solutionParenteral; Subcutaneous30 MCG
Injection, solutionParenteral; Subcutaneous300 MCG
Injection, solutionParenteral; Subcutaneous40 MCG
Injection, solutionParenteral; Subcutaneous50 MCG
Injection, solutionParenteral; Subcutaneous500 MCG
Injection, solutionParenteral; Subcutaneous60 MCG
Injection, solutionParenteral; Subcutaneous80 MCG
SolutionIntravenous; Subcutaneous100 mcg / mL
SolutionIntravenous; Subcutaneous100 ug/1mL
SolutionIntravenous; Subcutaneous15 mcg / mL
SolutionIntravenous; Subcutaneous150 ug/0.75mL
SolutionIntravenous; Subcutaneous200 mcg / mL
SolutionIntravenous; Subcutaneous200 ug/1mL
SolutionIntravenous; Subcutaneous25 ug/1mL
SolutionIntravenous; Subcutaneous25 mcg / mL
SolutionIntravenous; Subcutaneous300 ug/1mL
SolutionIntravenous; Subcutaneous325 mcg / mL
SolutionIntravenous; Subcutaneous40 mcg / mL
SolutionIntravenous; Subcutaneous40 ug/1mL
SolutionIntravenous; Subcutaneous500 mcg / mL
SolutionIntravenous; Subcutaneous60 ug/1mL
SolutionIntravenous; Subcutaneous60 mcg / mL
InjectionIntravenous; Subcutaneous
Injection, solutionParenteral10 MIKROGRAMM
Injection, solutionParenteral100 MIKROGRAMM
Injection, solutionParenteral100 UG
Injection, solutionParenteral130 UG
Injection, solutionParenteral150 MIKROGRAMM
Injection, solutionParenteral150 UG
Injection, solutionParenteral15 UG
Injection, solutionParenteral20 MIKROGRAMM
Injection, solutionParenteral20 UG
Injection, solutionParenteral30 MIKROGRAMM
Injection, solutionParenteral300 MIKROGRAMM
Injection, solutionParenteral300 UG
Injection, solutionParenteral30 UG
Injection, solutionParenteral40 MIKROGRAMM
Injection, solutionParenteral40 UG
Injection, solutionParenteral50 MIKROGRAMM
Injection, solutionParenteral500 MIKROGRAMM
Injection, solutionParenteral500 UG
Injection, solutionParenteral50 UG
Injection, solutionParenteral60 MIKROGRAMM
Injection, solutionParenteral60 UG
Injection, solutionParenteral80 MIKROGRAMM
Injection, solutionParenteral80 UG
SolutionIntravenous; Subcutaneous10 mcg
SolutionIntravenous; Subcutaneous100 mcg
SolutionIntravenous; Subcutaneous20 mcg
SolutionIntravenous; Subcutaneous30 mcg
SolutionIntravenous; Subcutaneous300 mcg
SolutionIntravenous; Subcutaneous40 mcg
SolutionIntravenous; Subcutaneous50 mcg
SolutionIntravenous; Subcutaneous
SolutionIntravenous; Subcutaneous60 mcg
SolutionIntravenous; Subcutaneous80 mcg
SolutionIntravenous; Subcutaneous150 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; Subcutaneous10 μg
Injection, solutionIntravenous; Subcutaneous100 μg
Injection, solutionIntravenous; Subcutaneous130 μg
Injection, solutionIntravenous; Subcutaneous15 μg
Injection, solutionIntravenous; Subcutaneous150 μg
Injection, solutionIntravenous; Subcutaneous20 μg
Injection, solutionIntravenous; Subcutaneous25 μg
Injection, solutionIntravenous; Subcutaneous30 μg
Injection, solutionIntravenous; Subcutaneous300 μg
Injection, solutionIntravenous; Subcutaneous40 μg
Injection, solutionIntravenous; Subcutaneous50 μg
Injection, solutionIntravenous; Subcutaneous500 μg
Injection, solutionIntravenous; Subcutaneous60 μg
Injection, solutionIntravenous; Subcutaneous80 μg
Injection, solutionSubcutaneous
Injection, solutionSubcutaneous10 μg
Injection, solutionSubcutaneous100 μg
Injection, solutionSubcutaneous130 μg
Injection, solutionSubcutaneous15 μg
Injection, solutionSubcutaneous150 μg
Injection, solutionSubcutaneous20 μg
Injection, solutionSubcutaneous30 μg
Injection, solutionSubcutaneous300 μg
Injection, solutionSubcutaneous40 μg
Injection, solutionSubcutaneous50 μg
Injection, solutionSubcutaneous500 μg
Injection, solutionSubcutaneous60 μg
Injection, solutionSubcutaneous80 μg
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

Drugtargets2
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.
Learn more
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
Learn more
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. [Article]
  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. [Article]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]

Drug created on June 13, 2005 13:24 / Updated on September 25, 2021 16:29