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
Pharmacology
- Indication
For the treatment of anemia (from renal transplants or certain HIV treatment)
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- Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- 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 agonistHumans - 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
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- 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 Integrate drug-drug
interactions in your softwareAbemaciclib 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
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Aranesp Injection, solution 25 ug/0.42mL Intravenous; Subcutaneous AMGEN INC 2006-09-25 2010-02-16 US 
Aranesp Injection, solution 300 μg Intravenous; Subcutaneous Amgen Europe B.V. 2016-09-08 Not applicable EU 
Aranesp Solution 500 mcg / mL Intravenous; Subcutaneous Amgen Not applicable Not applicable Canada 
Aranesp Injection, solution 20 μg Intravenous; Subcutaneous Amgen Europe B.V. 2016-09-08 Not applicable EU Aranesp Solution 200 mcg / mL Intravenous; Subcutaneous Amgen 2014-01-27 Not applicable Canada
Categories
- ATC Codes
- B03XA02 — Darbepoetin alfa
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Antianemic Preparations
- Blood and Blood Forming Organs
- Carbohydrates
- Colony-Stimulating Factors
- Erythropoiesis-Stimulating Agents
- Glycoconjugates
- Glycoproteins
- Hematinics
- Hematologic Agents
- Hematopoietic Cell Growth Factors
- Increased Erythroid Cell Production
- Proteins
- 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
- External Links
- UniProt
- P01588
- Genbank
- X02158
- PubChem Substance
- 46504480
- 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
Phase Status Purpose Conditions Count 4 Completed Basic Science Renal Anemia 1 4 Completed Prevention Anemia / Renal Failure, Chronic Renal Failure 1 4 Completed Treatment Anemia 3 4 Completed Treatment Anemia Associated With End Stage Renal Disease (ESRD) 1 4 Completed Treatment Anemia of Chronic Kidney Disease 1
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 μg Injection, solution Intravenous; Subcutaneous 200 ug/0.4mL 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 ug/1mL Solution Intravenous; Subcutaneous 100 mcg / mL 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 mcg / mL Solution Intravenous; Subcutaneous 25 ug/1mL 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 ug/1mL Solution Intravenous; Subcutaneous 60 mcg / mL 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 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 μg Injection, solution Subcutaneous 10 MCG Injection, solution Subcutaneous 100 MCG Injection, solution Subcutaneous 100 μg 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 MCG Injection, solution Subcutaneous 20 μg Injection, solution Subcutaneous 30 μg Injection, solution Subcutaneous 30 MCG Injection, solution Subcutaneous 300 MCG Injection, solution Subcutaneous 300 μg Injection, solution Subcutaneous 40 μg Injection, solution Subcutaneous 40 MCG Injection, solution Subcutaneous 50 μg Injection, solution Subcutaneous 50 MCG Injection, solution Subcutaneous 500 MCG Injection, solution Subcutaneous 500 μg 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 Canada CA2147124 No 2002-11-05 2014-08-16 Canada
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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- 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
- 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 February 20, 2024 23:54