DrugBank: Darbepoetin alfa (DB00012)

targets (1)

Identification

Name

Darbepoetin alfa

Accession Number

DB00012 (BIOD00032, BTD00032)

Type

biotech

Groups

approved

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

Display: 3D Structure

Protein chemical formula

C₈₁₅H₁₃₁₇N₂₃₃O₂₄₁S₅

Protein average weight

18396.1000

Sequences

>DB00012 sequence
APPRLICDSRVLERYLLEAKEAENITTGCAEHCSLNENITVPDTKVNFYAWKRMEVGQQA
VEVWQGLALLSEAVLRGQALLVNSSQPWEPLQLHVDKAVSGLRSLTTLLRALGAQKEAIS
PPDAASAAPLRTITADTFRKLFRVYSNFLRGKLKLYTGEACRTGDR

FASTA

Synonyms

Epoetin
Erythropoietin precursor

Salts

Not Available

Brand names

Name	Company
Aranesp	Amgen Inc.

Brand mixtures

Not Available

Categories

Antianemic Agents

CAS number

11096-26-7

Taxonomy

Kingdom

Not Available

Classes

Not Available

Substructures

Not Available

Pharmacology

Indication

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

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.

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

Pharmacoeconomics

Manufacturers

Amgen Inc.

Packagers

Dosage forms

Form	Route	Strength
Solution	Intravenous

Prices

Unit description	Cost	Unit
Aranesp (Albumin Free) 150 mcg/0.75ml Solution (1 Box = Four 0.75ml Vials)	3902.75 USD	box
Aranesp (Albumin Free) 100 mcg/0.5ml Solution (1 Box = Four 0.5ml Syringes)	2601.83 USD	box
Aranesp (Albumin Free) 100 mcg/ml Solution Four 1ml Vials Per Box	2601.83 USD	box
Aranesp (Albumin Free) 300 mcg/ml vial	1951.37 USD	vial
Aranesp 300 mcg/ml vial	1876.32 USD	ml
Aranesp 200 mcg/ml vial	1250.88 USD	ml
Aranesp 100 mcg/ml vial	625.44 USD	ml
Aranesp (Albumin Free) 60 mcg/ml vial	390.31 USD	vial
Aranesp 60 mcg/ml vial	375.3 USD	ml
Aranesp 40 mcg/ml vial	250.2 USD	ml
Aranesp (Albumin Free) 25 mcg/ml vial	162.61 USD	vial
Aranesp 25 mcg/ml vial	156.36 USD	ml

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

Patents

Country	Patent Number	Approved	Expires (estimated)
Canada	2165694	2003-03-18	2010-10-15
Canada	2147124	2002-11-05	2014-08-16

Properties

State

liquid

Experimental Properties

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

References

Synthesis Reference

Not Available

General Reference

Not Available

External Links

Resource	Link
UniProt	P01588
Genbank	X02158
PharmGKB	PA164743138
Drug Product Database	2246360
RxList	http://www.rxlist.com/cgi/generic/aranesp.htm
Drugs.com	http://www.drugs.com/cdi/darbepoetin-alfa-albumin.html
Wikipedia	http://en.wikipedia.org/wiki/Darbepoetin_alfa

ATC Codes

B03XA02

AHFS Codes

20:16.00

PDB Entries

1EER

FDA label

Not Available

MSDS

Not Available

Interactions

Drug Interactions

Searched, but no interactions found.

Food Interactions

Not Available

Targets
1. Erythropoietin receptor Pharmacological action: yes Actions: agonist Isoform EPOR-T, missing the cytoplasmic tail, acts as a dominant-negative receptor of EPOR-mediated signaling Organism class: human UniProt ID: P19235 Gene: EPOR Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report 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. Pubmed 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 Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

Targets

1. Erythropoietin receptor

Pharmacological action: yes
Actions: agonist

Isoform EPOR-T, missing the cytoplasmic tail, acts as a dominant-negative receptor of EPOR-mediated signaling

Organism class: human
UniProt ID: P19235 Link_out

Gene: EPOR Link_out

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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

Comments

Drug created on June 13, 2005 07:24 / Updated on September 03, 2011 16:35