Identification

Name
Darbepoetin alfa
Accession Number
DB00012  (BTD00032, BIOD00032)
Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Haematopoietic growth factors
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 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,recombinant
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AranespInjection, solution10 μgSubcutaneousAmgen Europe B.V.2001-06-08Not applicableEu
AranespInjection, solution10 μgSubcutaneousAmgen Europe B.V.2001-06-08Not applicableEu
AranespInjection, solution130 μgIntravenous; SubcutaneousAmgen Europe B.V.2001-06-08Not applicableEu
AranespInjection, solution30 μgIntravenous; SubcutaneousAmgen Europe B.V.2001-06-08Not applicableEu
AranespInjection, solution130 μgIntravenous; SubcutaneousAmgen Europe B.V.2001-06-08Not applicableEu
AranespInjection, solution100 μgIntravenous; SubcutaneousAmgen Europe B.V.2001-06-08Not applicableEu
AranespInjection, solution60 μgIntravenous; SubcutaneousAmgen Europe B.V.2001-06-08Not applicableEu
AranespInjection, solution100 μgSubcutaneousAmgen Europe B.V.2001-06-08Not applicableEu
AranespInjection, solution40 ug/.4mLIntravenous; SubcutaneousAmgen2006-08-14Not applicableUs
AranespInjection, solution100 μgSubcutaneousAmgen Europe B.V.2001-06-08Not applicableEu
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
NespoInjection, solution40 μgIntravenous; SubcutaneousDompé Biotec S.P.A.2001-06-08Not applicableEu
NespoInjection, solution40 μgSubcutaneousDompé Biotec S.P.A.2001-06-08Not applicableEu
NespoInjection, solution40 μgSubcutaneousDompé Biotec S.P.A.2001-06-08Not applicableEu
NespoInjection, solution130 μgSubcutaneousDompé Biotec S.P.A.2001-06-08Not applicableEu
NespoInjection, solution10 μgIntravenous; SubcutaneousDompé Biotec S.P.A.2001-06-08Not applicableEu
NespoInjection, solution10 μgSubcutaneousDompé Biotec S.P.A.2001-06-08Not applicableEu
NespoInjection, solution10 μgSubcutaneousDompé Biotec S.P.A.2001-06-08Not applicableEu
NespoInjection, solution10 μgIntravenous; SubcutaneousDompé Biotec S.P.A.2001-06-08Not applicableEu
NespoInjection, solution130 μgIntravenous; SubcutaneousDompé Biotec S.P.A.2001-06-08Not applicableEu
NespoInjection, solution60 μgIntravenous; SubcutaneousDompé Biotec S.P.A.2001-06-08Not applicableEu
Categories
UNII
15UQ94PT4P
CAS number
209810-58-2

Pharmacology

Indication

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

Structured Indications
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
Human
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
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
LenalidomideDarbepoetin alfa may increase the thrombogenic activities of Lenalidomide.Approved
Nandrolone decanoateNandrolone decanoate may increase the stimulatory activities of Darbepoetin alfa.Approved, Illicit
Nandrolone phenpropionateNandrolone phenpropionate may increase the stimulatory activities of Darbepoetin alfa.Approved, Illicit, Investigational
ThalidomideDarbepoetin alfa may increase the thrombogenic activities of Thalidomide.Approved, Investigational, Withdrawn
Food Interactions
Not Available

References

General References
Not Available
External Links
UniProt
P01588
Genbank
X02158
PubChem Substance
46504480
ChEMBL
CHEMBL1201566
Therapeutic Targets Database
DAP000800
PharmGKB
PA164743138
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Darbepoetin_alfa
ATC Codes
B03XA02 — Darbepoetin alfa
AHFS Codes
  • 20:16.00 — Hematopoietic Agents

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentHealthy Volunteers2
1Not Yet RecruitingNot AvailableReticulocyte Count1
1Unknown StatusTreatmentSymptomatic Anemia1
1WithdrawnTreatmentAnemias / Chronic Kidney Disease (CKD)1
1, 2CompletedTreatmentAnemias / Congestive Heart Failure (CHF)1
1, 2CompletedTreatmentBlood Cancers / Myelodysplastic Syndromes / Myelodysplastic Syndromes (MDS)1
1, 2CompletedTreatmentHypoxic Ischemic Encephalopathy (HIE)1
2Active Not RecruitingSupportive CareLymphoma, Large B-Cell, Diffuse (DLBCL)1
2Active Not RecruitingTreatmentMalignant Lymphomas1
2CompletedPreventionAnemias / Prostate Cancer1
2CompletedSupportive CareAnemias / Leukemias / Lymphoproliferative Disorders / Malignant Lymphomas / Multiple Myeloma and Plasma Cell Neoplasm / Precancerous Conditions / Unspecified Adult Solid Tumor, Protocol Specific1
2CompletedSupportive CareAnemias / Non-Myeloid Malignancies1
2CompletedTreatmentAnemias3
2CompletedTreatmentAnemias / Cancer, Breast1
2CompletedTreatmentAnemias / Cancers1
2CompletedTreatmentAnemias / Cancers / Non-Myeloid Malignancies2
2CompletedTreatmentAnemias / Chronic Kidney Disease (CKD)1
2CompletedTreatmentAnemias / Congestive Heart Failure (CHF)1
2CompletedTreatmentAnemias / Drug/Agent Toxicity by Tissue/Organ / Lung Cancers / Neutropenias1
2CompletedTreatmentAnemias / Genital Neoplasms, Female / Gynecological Malignancies1
2CompletedTreatmentAnemias / Heart Failure, Unspecified1
2CompletedTreatmentAnemias / Lung Cancer Non-Small Cell Cancer (NSCLC)1
2CompletedTreatmentAnemias / Neoplasms1
2CompletedTreatmentAnemias / Non-Myeloid Malignancies2
2CompletedTreatmentAnemias / Renal Insufficiency,Chronic2
2CompletedTreatmentCancer, Breast1
2CompletedTreatmentCancer, Breast / Stage I Breast Carcinoma / Stage II Breast Cancer1
2CompletedTreatmentChronic Lymphocytic Leukaemia (CLL) / Malignant Lymphomas / Multiple Myeloma (MM) / Neoplasms, Breast / Neoplasms, Lung1
2CompletedTreatmentDysgerminoma1
2CompletedTreatmentMyelodysplastic Syndrome1
2CompletedTreatmentMyelodysplastic Syndromes1
2CompletedTreatmentMyocardial Infarction (MI)1
2CompletedTreatmentNeuroprotection / Spinal Ischemia / Strokes1
2CompletedTreatmentPre-Dialysis2
2CompletedTreatmentRenal Anemia Associated With Chronic Renal Failure (CRF)1
2CompletedTreatmentTraumatic Brain Injury (TBI)1
2Not Yet RecruitingTreatmentHypoxic-Ischemic Encephalopathy Mild / Neonatal Encephalopathy1
2RecruitingTreatmentNeonatal Stroke / PAIS / Perinatal Stroke1
2TerminatedPreventionAnemias / Neoplasms1
2TerminatedSupportive CareAnemia of Cancer / Anemias / Cancers / Carcinoma NOS / Neoplasms / Non-Myeloid Malignancies1
2TerminatedTreatmentAnemias / Cancers / Neoplasms1
2TerminatedTreatmentAnemias / Chronic Kidney Disease (CKD)1
2TerminatedTreatmentLeukemias1
2TerminatedTreatmentMyelodysplastic Syndrome1
2Unknown StatusTreatmentMyelodysplastic Syndromes1
2Unknown StatusTreatmentNewborn Infants1
2, 3CompletedTreatmentHaematological Malignancies1
2, 3RecruitingTreatmentErythroblastosis Fetalis Due to Isoimmunization / Erythroblastosis Fetalis Due to RH Antibodies / Erythroblastosis Fetalis, Rh Disease / Erythroblastosis, Fetal1
2, 3TerminatedPreventionAcute Kidney Injury (AKI)1
2, 3TerminatedSupportive CareAnemias / Prostatic Neoplasms1
2, 3Unknown StatusTreatmentMyelodysplastic Syndromes1
3Active Not RecruitingTreatmentAnemias1
3Active Not RecruitingTreatmentAnemias / End Stage Renal Disease (ESRD)1
3Active Not RecruitingTreatmentChronic Kidney Disease (CKD) / Diabetes1
3CompletedSupportive CareAnemias / Leukemias / Lymphoproliferative Disorders / Malignant Lymphomas / Multiple Myeloma and Plasma Cell Neoplasm / Precancerous Conditions / Unspecified Adult Solid Tumor, Protocol Specific1
3CompletedSupportive CareAnemias / Leukemias / Lymphoproliferative Disorders / Malignant Lymphomas / Multiple Myeloma and Plasma Cell Neoplasm / Precancerous/Nonmalignant Condition / Unspecified Adult Solid Tumor, Protocol Specific1
3CompletedSupportive CareSmith-Magenis Syndrome1
3CompletedTreatmentAcute Myocardial Infarct1
3CompletedTreatmentAnemia in Chronic Kidney Disease Patients Not on Dialysis / Management of Anemia in Chronic Kidney Disease Patients Not on Dialysis1
3CompletedTreatmentAnemias10
3CompletedTreatmentAnemias / Cancers2
3CompletedTreatmentAnemias / Cardiovascular Disease (CVD) / Congestive Heart Failure (CHF) / Heart Failure, Unspecified / Ventricular Dysfunction1
3CompletedTreatmentAnemias / Chronic Kidney Disease (CKD)1
3CompletedTreatmentAnemias / Chronic Kidney Disease (CKD) / Chronic Renal Failure (CRF)2
3CompletedTreatmentAnemias / Diabetes Mellitus (DM) / Kidney Diseases1
3CompletedTreatmentAnemias / Kidney Diseases1
3CompletedTreatmentAnemias / Neoplasms1
3CompletedTreatmentAnemias / Non-Myeloid Malignancies1
3CompletedTreatmentAnemias / Renal Anemia, Chronic1
3CompletedTreatmentCancers1
3CompletedTreatmentCancers / Non-Myeloid Malignancies1
3CompletedTreatmentChronic Kidney Disease (CKD)1
3CompletedTreatmentChronic Kidney Disease (CKD) / Kidney Diseases2
3CompletedTreatmentDiffuse Large Cell Lymphoma1
3CompletedTreatmentEnd Stage Renal Disease (ESRD) / Pre-Dialysis1
3CompletedTreatmentKidney Diseases3
3CompletedTreatmentKidney Failure,Chronic1
3CompletedTreatmentLung Cancer Small Cell Lung Cancer (SCLC)1
3CompletedTreatmentMyelodysplastic Syndromes (MDS)1
3RecruitingNot AvailableAnemias1
3RecruitingTreatmentAnemia in Chronic Kidney Disease in Non-dialysis Patients1
3RecruitingTreatmentAnemia in Subjects With DD-CKD1
3RecruitingTreatmentAnemia; Non-dialysis Dependent Chronic Kidney Disease1
3RecruitingTreatmentAnemias2
3RecruitingTreatmentAnemias / Chronic Kidney Disease (CKD) / End Stage Renal Failure on Dialysis1
3RecruitingTreatmentAnemias / Dialysis-dependent Chronic Kidney Disease1
3RecruitingTreatmentAnemias / Non-dialysis-dependent Chronic Kidney Disease2
3RecruitingTreatmentNeonatal / Neurocognitive / Neurodevelopmental Impairment / Neuroprotective1
3TerminatedTreatmentAnemias1
3TerminatedTreatmentAnemias / Cardiovascular Disease (CVD) / Congestive Heart Failure (CHF) / Heart Failure, Unspecified / Ventricular Dysfunction1
3TerminatedTreatmentAnemias / Chronic Kidney Disease (CKD)1
3TerminatedTreatmentAnemias / Chronic Kidney Disease (CKD) / Kidney Diseases1
3Unknown StatusNot AvailableMyelodysplastic Syndrome1
3WithdrawnTreatmentAnemias / Chronic Obstructive Pulmonary Disease (COPD)1
4CompletedNot AvailableAnemias / Chronic Kidney Disease (CKD) / Prophylaxis of cardiomyopathy1
4CompletedNot AvailableAnemias / Neoplasms1
4CompletedBasic ScienceRenal Anemia1
4CompletedPreventionAnemias / Chronic Renal Failure (CRF)1
4CompletedTreatmentAnemia of End Stage Renal Disease1
4CompletedTreatmentAnemias3
4CompletedTreatmentAnemias / Chronic Kidney Disease (CKD)1
4CompletedTreatmentAnemias / Chronic Renal Anemia1
4CompletedTreatmentAnemias / Neoplasms1
4CompletedTreatmentAnemias / Cancer treatment1
4CompletedTreatmentChronic Kidney Disease (CKD) / Chronic Renal Insufficiency / Kidney Diseases / Pre-Dialysis / Pre-ESRD3
4CompletedTreatmentColorectal Cancers1
4CompletedTreatmentEnd Stage Renal Disease (ESRD)1
4CompletedTreatmentKidney Diseases2
Not AvailableActive Not RecruitingTreatmentAnemias / Cancers1
Not AvailableCompletedNot AvailableAnemias / Kidney Failure,Chronic1
Not AvailableCompletedPreventionSarcomas1
Not AvailableCompletedTreatmentAnemias / Congestive Heart Failure (CHF)1
Not AvailableCompletedTreatmentAnemias / Kidney Failure,Chronic / Peritoneal Dialysis, Continuous Ambulatory1
Not AvailableCompletedTreatmentMalignancies, Hematologic1
Not AvailableRecruitingNot AvailableCardiovascular Disease (CVD) / Chronic Kidney Disease (CKD)1
Not AvailableTerminatedNot AvailableChronic Kidney Disease, Receiving Dialysis1
Not AvailableTerminatedTreatmentAnemias / Chronic Kidney Disease (CKD) / Diabetes Mellitus (DM)1
Not AvailableUnknown StatusTreatmentCancer, Breast1

Pharmacoeconomics

Manufacturers
  • Amgen Inc.
Packagers
Dosage forms
FormRouteStrength
Injection, solutionIntravenous; Subcutaneous10 ug/.4mL
Injection, solutionIntravenous; Subcutaneous10 μg
Injection, solutionIntravenous; Subcutaneous100 ug/.5mL
Injection, solutionIntravenous; Subcutaneous100 μg
Injection, solutionIntravenous; Subcutaneous130 μg
Injection, solutionIntravenous; Subcutaneous15 μg
Injection, solutionIntravenous; Subcutaneous150 μg
Injection, solutionIntravenous; Subcutaneous150 ug/.3mL
Injection, solutionIntravenous; Subcutaneous20 μg
Injection, solutionIntravenous; Subcutaneous200 ug/.4mL
Injection, solutionIntravenous; Subcutaneous200 μg
Injection, solutionIntravenous; Subcutaneous25 ug/.42mL
Injection, solutionIntravenous; Subcutaneous25 μg
Injection, solutionIntravenous; Subcutaneous30 μg
Injection, solutionIntravenous; Subcutaneous300 μg
Injection, solutionIntravenous; Subcutaneous300 ug/.6mL
Injection, solutionIntravenous; Subcutaneous40 ug/.4mL
Injection, solutionIntravenous; Subcutaneous40 μg
Injection, solutionIntravenous; Subcutaneous50 μg
Injection, solutionIntravenous; Subcutaneous500 μg
Injection, solutionIntravenous; Subcutaneous500 ug/mL
Injection, solutionIntravenous; Subcutaneous60 ug/.3mL
Injection, solutionIntravenous; Subcutaneous60 μg
Injection, solutionIntravenous; Subcutaneous80 μg
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
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)
CA2165694No2003-03-182010-10-15Canada
CA2147124No2002-11-052014-08-16Canada

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

Taxonomy

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

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 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 07:24 / Updated on November 19, 2017 20:33