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Accession NumberDB00019  (BTD00094, BIOD00094)
DescriptionPEGylated (at N terminus) form of human G-CSF (Granulocyte colony stimulating factor), 175 residues, produced from E. coli via bacterial fermentation.
Protein structureDb00019
Related Articles
Protein chemical formulaC845H1343N223O243S9
Protein average weight18802.8 Da
> Pegfilgrastim sequence
Download FASTA Format
Granulocyte colony-stimulating factor precursor
N-(3-Hydroxypropyl)Methionylcolony-stimulating Factor (human), 1-Ether with .Alpha.-Methyl-.Omega.-Hydroxypoly(Oxyethylene)
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Neulastasolution10 mgsubcutaneousAmgen Canada Inc2004-03-12Not applicableCanada
Neulastainjection6 mg/.6mLsubcutaneousAmgen Inc2002-04-01Not applicableUs
NeulastakitsubcutaneousAmgen Inc2002-04-01Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
NeupopegSolution for injection6 mgSubcutaneous useDompé Biotec S.P.A.2002-08-22Not applicableEu
NeupopegSolution for injection6 mgSubcutaneous useDompé Biotec S.P.A.2002-08-22Not applicableEu
NeupopegSolution for injection6 mgSubcutaneous useDompé Biotec S.P.A.2002-08-22Not applicableEu
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
CAS number208265-92-3
IndicationIncreases leukocyte production, for treatment in non-myeloid cancer, neutropenia and bone marrow transplant
Structured Indications
PharmacodynamicsUsed in the treatment of chemotherapy-induced neutropenia by enhancing the production of neutrophils. Pegfilgrastim acts on hematopoietic cells by binding to specific cell surface receptors thereby stimulating proliferation, differentiation, commitment, and end cell functional activation. Pegfilgrastim has reduced renal clearance and prolonged persistence in vivo as compared to Filgrastim.
Mechanism of actionPegfilgrastim binds to the G-CSF receptor. As a G-CSF analog, it controls proliferation of committed progenitor cells and influences their maturation into mature neutrophils. Pegfilgrastim also stimulates the release of neutrophils from bone marrow storage pools and reduces their maturation time. Pegfilgrastim acts to increase the phagocytic activity of mature neutrophils. In patients receiving cytotoxic chemotherapy, pegfilgrastim can accelerate neutrophil recovery, leading to a reduction in duration of the neutropenic phase
TargetKindPharmacological actionActionsOrganismUniProt ID
Granulocyte colony-stimulating factor receptorProteinyes
HumanQ99062 details
Neutrophil elastaseProteinunknownNot AvailableHumanP08246 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationFilgrastim is primarily eliminated by the kidney and neutrophils/neutrophil precursors; the latter presumably involves binding of the growth factor to the G-CSF receptor on the cell surface, internalization of the growth factor-receptor complexes via endocytosis, and subsequent degradation inside the cells. Pegylation of filgrastim renders renal clearance insignificant, which was demonstrated in bilaterally nephrectomized rats and confirmed in subjects with renal impairment. As a result, the neutrophil-mediated clearance is the predominant elimination pathway for pegfilgrastim. During chemotherapy-induced neutropenia, the clearance of pegfilgrastim is significantly reduced and the concentration of pegfilgrastim is sustained until onset of neutrophil recovery.
Half life15-80 hrs
ClearanceNot Available
ToxicityNot Available
Affected organismsNot Available
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Drug Interactions
PegloticaseThe therapeutic efficacy of Pegfilgrastim can be decreased when used in combination with Pegloticase.
Food InteractionsNot Available
Synthesis ReferenceNot Available
General References
  1. Yang BB, Kido A: Pharmacokinetics and pharmacodynamics of pegfilgrastim. Clin Pharmacokinet. 2011 May;50(5):295-306. doi: 10.2165/11586040-000000000-00000. [PubMed:21456630 ]
External Links
ATC CodesL03AA13L03AA10
AHFS Codes
  • 20:16.00
PDB Entries
FDA labelDownload (50 KB)
MSDSNot Available
ManufacturersNot Available
Dosage forms
Injectionsubcutaneous6 mg/.6mL
Solutionsubcutaneous10 mg
Solution for injectionSubcutaneous use6 mg
Unit descriptionCostUnit
Neulasta 6 mg/0.6 ml syringe4102.37USD syringe
Neulasta 6 mg/0.6ml Solution 0.6ml Syringe4026.05USD syringe
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1339071 No1997-07-292014-07-29Canada
CA1341537 No2007-07-312024-07-31Canada
Experimental Properties
melting point60 °CLuo, P., Protein Science 11:1218-1226 (2002)
hydrophobicity0.209Not Available
isoelectric point5.65Not Available
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available


Pharmacological action
General Function:
Receptor activity
Specific Function:
Receptor for granulocyte colony-stimulating factor (CSF3), essential for granulocytic maturation. Plays a crucial role in the proliferation, differientation and survival of cells along the neutrophilic lineage. In addition it may function in some adhesion or recognition events at the cell surface.
Gene Name:
Uniprot ID:
Molecular Weight:
92155.615 Da
  1. Erkeland SJ, Aarts LH, Irandoust M, Roovers O, Klomp A, Valkhof M, Gits J, Eyckerman S, Tavernier J, Touw IP: Novel role of WD40 and SOCS box protein-2 in steady-state distribution of granulocyte colony-stimulating factor receptor and G-CSF-controlled proliferation and differentiation signaling. Oncogene. 2007 Mar 29;26(14):1985-94. Epub 2006 Sep 25. [PubMed:17001306 ]
  2. Elsasser A, Franzen M, Kohlmann A, Weisser M, Schnittger S, Schoch C, Reddy VA, Burel S, Zhang DE, Ueffing M, Tenen DG, Hiddemann W, Behre G: The fusion protein AML1-ETO in acute myeloid leukemia with translocation t(8;21) induces c-jun protein expression via the proximal AP-1 site of the c-jun promoter in an indirect, JNK-dependent manner. Oncogene. 2003 Aug 28;22(36):5646-57. [PubMed:12944913 ]
  3. Ward AC: The role of the granulocyte colony-stimulating factor receptor (G-CSF-R) in disease. Front Biosci. 2007 Jan 1;12:608-18. [PubMed:17127322 ]
  4. Zhuang D, Qiu Y, Haque SJ, Dong F: Tyrosine 729 of the G-CSF receptor controls the duration of receptor signaling: involvement of SOCS3 and SOCS1. J Leukoc Biol. 2005 Oct;78(4):1008-15. Epub 2005 Jul 20. [PubMed:16033816 ]
  5. Cao YR, Shao ZH, Liu H, Shi J, Bai J, Tu MF, Wang HQ, Xing LM, Cui ZZ, Sun J, Jia HR, Yang TY: [The response of bone marrow hematopoietic cells to G-CSF in paroxysmal nocturnal hemoglobinuria patients]. Zhonghua Xue Ye Xue Za Zhi. 2005 Apr;26(4):235-8. [PubMed:15949269 ]
  6. Kotto-Kome AC, Fox SE, Lu W, Yang BB, Christensen RD, Calhoun DA: Evidence that the granulocyte colony-stimulating factor (G-CSF) receptor plays a role in the pharmacokinetics of G-CSF and PegG-CSF using a G-CSF-R KO model. Pharmacol Res. 2004 Jul;50(1):55-8. [PubMed:15082029 ]
Pharmacological action
General Function:
Serine-type endopeptidase activity
Specific Function:
Modifies the functions of natural killer cells, monocytes and granulocytes. Inhibits C5a-dependent neutrophil enzyme release and chemotaxis.
Gene Name:
Uniprot ID:
Molecular Weight:
28517.81 Da
  1. Carter CR, Whitmore KM, Thorpe R: The significance of carbohydrates on G-CSF: differential sensitivity of G-CSFs to human neutrophil elastase degradation. J Leukoc Biol. 2004 Mar;75(3):515-22. Epub 2003 Dec 4. [PubMed:14657210 ]
  2. Jian MY, Koizumi T, Tsushima K, Fujimoto K, Kubo K: Effects of granulocyte colony-stimulating factor (G-CSF) and neutrophil elastase inhibitor (ONO-5046) on acid-induced lung injury in rats. Inflammation. 2004 Dec;28(6):327-36. [PubMed:16245075 ]
  3. Pelus LM, Bian H, King AG, Fukuda S: Neutrophil-derived MMP-9 mediates synergistic mobilization of hematopoietic stem and progenitor cells by the combination of G-CSF and the chemokines GRObeta/CXCL2 and GRObetaT/CXCL2delta4. Blood. 2004 Jan 1;103(1):110-9. Epub 2003 Sep 4. [PubMed:12958067 ]
  4. Druhan LJ, Ai J, Massullo P, Kindwall-Keller T, Ranalli MA, Avalos BR: Novel mechanism of G-CSF refractoriness in patients with severe congenital neutropenia. Blood. 2005 Jan 15;105(2):584-91. Epub 2004 Sep 7. [PubMed:15353486 ]
  5. Schepers H, Wierenga AT, van Gosliga D, Eggen BJ, Vellenga E, Schuringa JJ: Reintroduction of C/EBPalpha in leukemic CD34+ stem/progenitor cells impairs self-renewal and partially restores myelopoiesis. Blood. 2007 Aug 15;110(4):1317-25. Epub 2007 May 2. [PubMed:17475913 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23