Darbepoetin alfa

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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

Protein Chemical Formula: C₈₁₅H₁₃₁₇N₂₃₃O₂₄₁S₅
Protein Average Weight: 18396.1 Da

Sequences

>Darbepoetin alfa
MGVHECPAWLWLLLSLLSLPLGLPVLGAPPRLICDSRVLERYLLEAKEAENITTGCNETC
SLNENITVPDTKVNFYAWKRMEVGQQAVEVWQGLALLSEAVLRGQALLVNSSQVNETLQL
HVDKAVSGLRSLTTLLRALGAQKEAISPPDAASAAPLRTITADTFRKLFRVYSNFLRGKL
KLYTGEACRTGDR

Download FASTA Format

Synonyms

Darbepoetin
Darbepoetin alfa
Darbepoetin alfa,recombinant
Darbepoetina alfa

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Pharmacology

Indication

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

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Age Group	Patient Characteristics	Dose Form
Treatment of	Anemia		••••••••••••			•••••••••
Treatment of	Anemia		••••••••••••			•••••••••

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.

Target	Actions	Organism
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

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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.

Drug	Interaction
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Abemaciclib	The risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Abemaciclib.
Abiraterone	The risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Abiraterone.
Adagrasib	The risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Adagrasib.
Afatinib	The risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Afatinib.
Aldesleukin	The risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Aldesleukin.

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

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Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Aranesp	Injection, solution	150 μg	Subcutaneous	Amgen Europe B.V.	2016-09-08	Not applicable
Aranesp	Solution	300 ug/1mL	Intravenous; Subcutaneous	AMGEN INC	2002-08-19	2010-02-16
Aranesp	Injection, solution	40 μg	Intravenous; Subcutaneous	Amgen Europe B.V.	2016-09-08	Not applicable
Aranesp	Injection, solution	100 ug/0.5mL	Intravenous; Subcutaneous	AMGEN INC	2006-09-25	2010-02-16
Aranesp	Injection, solution	80 μg	Intravenous; Subcutaneous	Amgen Europe B.V.	2016-09-08	Not applicable

Chemical Identifiers

UNII: 15UQ94PT4P
CAS number: 209810-58-2

References

General References

Not Available

External Links

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

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Phase	Status	Purpose	Conditions	Count	Start Date	Why Stopped	100+ additional columns
Unlock 175K+ rows when you subscribe.View sample data
Not Available	Completed	Not Available	Anemia / Cardiomyopathy / Chronic Kidney Disease (CKD)	1	somestatus	stop reason	just information to hide
Not Available	Completed	Not Available	Anemia / Neoplasm	1	somestatus	stop reason	just information to hide
Not Available	Completed	Not Available	Anemia / Renal Failure, Chronic Renal Failure	1	somestatus	stop reason	just information to hide
Not Available	Completed	Not Available	Cardiovascular Disease (CVD) / Chronic Kidney Disease (CKD)	1	somestatus	stop reason	just information to hide
Not Available	Completed	Prevention	Sarcomas	1	somestatus	stop reason	just information to hide

Pharmacoeconomics

Manufacturers

Amgen Inc.

Packagers

Amgen Inc.
Physicians Total Care Inc.

Dosage Forms

Form	Route	Strength
Injection, solution	Intravenous; Parenteral	10 MCG
Injection, solution	Intravenous; Parenteral	100 MCG
Injection, solution	Intravenous; Parenteral	130 MCG
Injection, solution	Intravenous; Parenteral	15 MCG
Injection, solution	Intravenous; Parenteral	150 MCG
Injection, solution	Intravenous; Parenteral	20 MCG
Injection, solution	Intravenous; Parenteral	25 MCG
Injection, solution	Intravenous; Parenteral	30 MCG
Injection, solution	Intravenous; Parenteral	300 MCG
Injection, solution	Intravenous; Parenteral	40 MCG
Injection, solution	Intravenous; Parenteral	50 MCG
Injection, solution	Intravenous; Parenteral	500 MCG
Injection, solution	Intravenous; Parenteral	60 MCG
Injection, solution	Intravenous; Parenteral	80 MCG
Injection, solution	Intravenous; Subcutaneous	10 ug/0.4mL
Injection, solution	Intravenous; Subcutaneous	100 ug/0.5mL
Injection, solution	Intravenous; Subcutaneous	150 ug/0.3mL
Injection, solution	Intravenous; Subcutaneous	200 ug/0.4mL
Injection, solution	Intravenous; Subcutaneous	200 μg
Injection, solution	Intravenous; Subcutaneous	25 ug/0.42mL
Injection, solution	Intravenous; Subcutaneous	300 ug/0.6mL
Injection, solution	Intravenous; Subcutaneous	40 ug/.4mL
Injection, solution	Intravenous; Subcutaneous	40 ug/0.4mL
Injection, solution	Intravenous; Subcutaneous	500 ug/1mL
Injection, solution	Intravenous; Subcutaneous	60 ug/0.3mL
Injection, solution	Parenteral; Subcutaneous	10 MCG
Injection, solution	Parenteral; Subcutaneous	100 MCG
Injection, solution	Parenteral; Subcutaneous	15 MCG
Injection, solution	Parenteral; Subcutaneous	150 MCG
Injection, solution	Parenteral; Subcutaneous	20 MCG
Injection, solution	Parenteral; Subcutaneous	30 MCG
Injection, solution	Parenteral; Subcutaneous	300 MCG
Injection, solution	Parenteral; Subcutaneous	40 MCG
Injection, solution	Parenteral; Subcutaneous	50 MCG
Injection, solution	Parenteral; Subcutaneous	500 MCG
Injection, solution	Parenteral; Subcutaneous	60 MCG
Injection, solution	Parenteral; Subcutaneous	80 MCG
Solution	Intravenous; Subcutaneous	100 mcg / mL
Solution	Intravenous; Subcutaneous	100 ug/1mL
Solution	Intravenous; Subcutaneous	15 mcg / mL
Solution	Intravenous; Subcutaneous	150 ug/0.75mL
Solution	Intravenous; Subcutaneous	200 ug/1mL
Solution	Intravenous; Subcutaneous	200 mcg / mL
Solution	Intravenous; Subcutaneous	25 ug/1mL
Solution	Intravenous; Subcutaneous	25 mcg / mL
Solution	Intravenous; Subcutaneous	300 ug/1mL
Solution	Intravenous; Subcutaneous	325 mcg / mL
Solution	Intravenous; Subcutaneous	40 mcg / mL
Solution	Intravenous; Subcutaneous	40 ug/1mL
Solution	Intravenous; Subcutaneous	500 mcg / mL
Solution	Intravenous; Subcutaneous	60 mcg / mL
Solution	Intravenous; Subcutaneous	60 ug/1mL
Solution	Parenteral	10.000 mcg
Injection	Intravenous; Subcutaneous	10 mcg/0.4ml
Injection, solution	Parenteral	10 MIKROGRAMM
Injection	Intravenous; Subcutaneous	100 mcg/0.5ml
Injection, solution	Parenteral	100 MIKROGRAMM
Injection, solution	Parenteral	100 UG
Injection, solution	Parenteral	130 UG
Injection	Intravenous; Subcutaneous	150 mcg/0.3ml
Injection, solution	Parenteral	150 MIKROGRAMM
Injection, solution	Parenteral	150 UG
Injection, solution	Parenteral	15 UG
Injection	Intravenous; Subcutaneous	20 mcg/0.5ml
Injection, solution	Parenteral	20 MIKROGRAMM
Injection, solution	Parenteral	20 UG
Injection	Intravenous; Subcutaneous	30 mcg/0.3ml
Injection, solution	Parenteral	30 MIKROGRAMM
Injection, solution	Parenteral	300 MIKROGRAMM
Injection, solution	Parenteral	300 UG
Injection, solution	Parenteral	30 UG
Injection	Intravenous; Subcutaneous	40 mcg/0.4ml
Injection, solution	Parenteral	40 MIKROGRAMM
Injection, solution	Parenteral	40 UG
Injection	Intravenous; Subcutaneous	50 mcg/0.5ml
Injection, solution	Parenteral	50 MIKROGRAMM
Injection, solution	Parenteral	500 MIKROGRAMM
Injection, solution	Parenteral	500 UG
Injection, solution	Parenteral	50 UG
Injection	Intravenous; Subcutaneous	60 mcg/0.3ml
Injection, solution	Parenteral	60 MIKROGRAMM
Injection, solution	Parenteral	60 UG
Injection	Intravenous; Subcutaneous	80 mcg/0.4ml
Injection, solution	Parenteral	80 MIKROGRAMM
Injection, solution	Parenteral	80 UG
Solution	Intravenous; Subcutaneous	10 mcg
Solution	Intravenous; Subcutaneous	100 mcg
Solution	Intravenous; Subcutaneous	20 mcg
Solution	Intravenous; Subcutaneous	30 mcg
Solution	Intravenous; Subcutaneous	300 mcg
Solution	Intravenous; Subcutaneous	40 mcg
Solution	Intravenous; Subcutaneous	50 mcg
Solution	Intravenous; Subcutaneous	500 cg
Solution	Intravenous; Subcutaneous	60 mcg
Solution	Intravenous; Subcutaneous	80 mcg
Solution	Intravenous; Subcutaneous	150 mcg
Injection		120 mcg/0.5ml
Injection		20 mcg/0.5ml
Injection		30 mcg/0.5ml
Injection		40 mcg/0.5ml
Injection		60 mcg/0.5ml
Injection, solution, concentrate	Intravenous; Subcutaneous	10 mcg/0.5ml
Injection, solution, concentrate	Intravenous; Subcutaneous	120 mcg/0.5ml
Solution	Intravenous; Subcutaneous	120 mcg/0.5ml
Injection, solution, concentrate	Intravenous; Subcutaneous	180 mcg/0.5ml
Solution	Intravenous; Subcutaneous	180 mcg/0.5ml
Injection, solution, concentrate	Intravenous; Subcutaneous	20 mcg/0.5ml
Solution	Intravenous; Subcutaneous	20 mcg/0.5ml
Injection, solution, concentrate	Intravenous; Subcutaneous	30 mcg/0.5ml
Solution	Intravenous; Subcutaneous	30 mcg/0.5ml
Injection, solution, concentrate	Intravenous; Subcutaneous	40 mcg/0.5ml
Solution	Intravenous; Subcutaneous	40 mcg/0.5ml
Injection, solution, concentrate	Intravenous; Subcutaneous	60 mcg/0.5ml
Solution	Intravenous; Subcutaneous	60 mcg/0.5ml
Injection	Intravenous
Injection, solution	Intravenous	10 MCG
Injection, solution	Intravenous	100 MCG
Injection, solution	Intravenous	15 MCG
Injection, solution	Intravenous	150 MCG
Injection, solution	Intravenous	20 MCG
Injection, solution	Intravenous	25 MCG
Injection, solution	Intravenous	30 MCG
Injection, solution	Intravenous	300 MCG
Injection, solution	Intravenous	40 MCG
Injection, solution	Intravenous	50 MCG
Injection, solution	Intravenous	500 MCG
Injection, solution	Intravenous	60 MCG
Injection, solution	Intravenous	80 MCG
Injection, solution	Intravenous; Subcutaneous	10 μg
Injection, solution	Intravenous; Subcutaneous	100 μg
Injection, solution	Intravenous; Subcutaneous	130 μg
Injection, solution	Intravenous; Subcutaneous	15 μg
Injection, solution	Intravenous; Subcutaneous	150 μg
Injection, solution	Intravenous; Subcutaneous	20 μg
Injection, solution	Intravenous; Subcutaneous	25 μg
Injection, solution	Intravenous; Subcutaneous	30 μg
Injection, solution	Intravenous; Subcutaneous	300 μg
Injection, solution	Intravenous; Subcutaneous	40 μg
Injection, solution	Intravenous; Subcutaneous	50 μg
Injection, solution	Intravenous; Subcutaneous	500 μg
Injection, solution	Intravenous; Subcutaneous	60 μg
Injection, solution	Intravenous; Subcutaneous	80 μg
Injection, solution	Subcutaneous	10 MCG
Injection, solution	Subcutaneous	10 μg
Injection, solution	Subcutaneous	100 μg
Injection, solution	Subcutaneous	100 MCG
Injection, solution	Subcutaneous	130 μg
Injection, solution	Subcutaneous	15 MCG
Injection, solution	Subcutaneous	15 μg
Injection, solution	Subcutaneous	150 μg
Injection, solution	Subcutaneous	150 MCG
Injection, solution	Subcutaneous	20 μg
Injection, solution	Subcutaneous	20 MCG
Injection, solution	Subcutaneous	30 MCG
Injection, solution	Subcutaneous	30 μg
Injection, solution	Subcutaneous	300 MCG
Injection, solution	Subcutaneous	300 μg
Injection, solution	Subcutaneous	40 MCG
Injection, solution	Subcutaneous	40 μg
Injection, solution	Subcutaneous	50 μg
Injection, solution	Subcutaneous	50 MCG
Injection, solution	Subcutaneous	500 μg
Injection, solution	Subcutaneous	500 MCG
Injection, solution	Subcutaneous	60 MCG
Injection, solution	Subcutaneous	60 μg
Injection, solution	Subcutaneous	80 μg
Injection, solution	Subcutaneous	80 MCG

Prices

Unit description	Cost	Unit
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 Box	2601.83USD	box
Aranesp (Albumin Free) 300 mcg/ml vial	1951.37USD	vial
Aranesp 300 mcg/ml vial	1876.32USD	ml
Aranesp 200 mcg/ml vial	1250.88USD	ml
Aranesp 100 mcg/ml vial	625.44USD	ml
Aranesp (Albumin Free) 60 mcg/ml vial	390.31USD	vial
Aranesp 60 mcg/ml vial	375.3USD	ml
Aranesp 40 mcg/ml vial	250.2USD	ml
Aranesp (Albumin Free) 25 mcg/ml vial	162.61USD	vial
Aranesp 25 mcg/ml vial	156.36USD	ml

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
CA2165694	No	2003-03-18	2010-10-15
CA2147124	No	2002-11-05	2014-08-16

Properties

State

Liquid

Experimental Properties

Property	Value	Source
melting point (°C)	53 °C	Arakawa, T. et al., Biosci. Biotechnol. Biochem. 65:1321-1327 (2001)
hydrophobicity	-0.188	Not Available
isoelectric point	8.75	Not Available

Targets

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Details1. Erythropoietin receptor

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Agonist

General Function: Receptor for erythropoietin, which mediates erythropoietin-induced erythroblast proliferation and differentiation (PubMed:10388848, PubMed:2163695, PubMed:2163696, PubMed:8662939, PubMed:9774108). Upon EPO stimulation, EPOR dimerizes triggering the JAK2/STAT5 signaling cascade (By similarity). In some cell types, can also activate STAT1 and STAT3 (PubMed:11756159). May also activate the LYN tyrosine kinase (By similarity)
Specific Function: erythropoietin receptor activity
Gene Name: EPOR
Uniprot ID: P19235
Uniprot Name: Erythropoietin receptor
Molecular Weight: 55064.725 Da

References

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]
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]
Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]

Drug created at June 13, 2005 13:24 / Updated at October 07, 2024 13:57

Darbepoetin alfa

Identification

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Clinical Trial & Rare Diseases Add-on Data Package

Pharmacoeconomics

Properties

Targets

References