Accession Number

Pegfilgrastim is a PEGylated form of the recombinant human granulocyte colony-stimulating factor (G-CSF) analogue, filgrastim.2 It is used to decrease the incidence of infection, as manifested by febrile neutropenia, in patients with with non-myeloid cancer receiving myelosuppressive anti-cancer treatment. Some patients with greater risk factors may develop febrile neutropenia from myelosuppressive therapy and are susceptible to an increased risk of developing infections. Although the risk of developing febrile neutropenia is less than 20% in many readily used chemotherapy regimens,9 infections pose risks of hospitalization and mortalities.4 Due to the relatively short circulating half-life of filgrastim, a 20 kDa PEG moiety was covalently conjugated to the N-terminus of filgrastim (at the methionine residue) to develop a longer acting version of the drug.1,3 Due to a longer half-life and slower elimination rate than filgrastim, pegfilgrastim requires less frequent dosing than filgrastim. However, pegfilgrastim retains the same biological activity as filgrastim and binds to the same G-CSF receptor to stimulate the proliferation, differentiation, and activation of neutrophils.3

First developed by Amgen, pegfilgrastim was initially approved by the FDA in 2002 and marketed as Neulasta®. It is typically administered via a subcutaneous injection. There are several pegfilgrastim biosimilars (Fulphila®, Pelgraz® or Lapelga®, Pelmeg®, Udenyca®, Ziextenzo®, and Grasustek®) that are approved for the same therapeutic indication by Health Canada, European Union (EU), and FDA.8,10 These biosimilars are highly similar to the reference product, Neulasta®, in terms of pharmacological and pharmacokinetic profile and condition(s) of use, such as the therapeutic indication(s), dosing regimen(s), strength(s), dosage form(s), and route(s) of administration.11

Biologic Classification
Protein Based Therapies
Haematopoietic growth factors
Protein Structure
Protein Chemical Formula
Protein Average Weight
39000.0 Da (approximate, PEGylated)
> Pegfilgrastim sequence
Download FASTA Format
  • Granulocyte colony-stimulating factor pegfilgrastim
  • peg-filgrastim
  • pegfilgrastim-apgf
  • pegfilgrastim-bmez
  • pegfilgrastim-cbqv
  • pegfilgrastim-jmdb



Pegfilgrastim is indicated to decrease the incidence of infection, as manifested by febrile neutropenia, in patients with non­ myeloid malignancies receiving myelosuppressive anti-cancer drugs associated with a clinically significant incidence of febrile neutropenia.6

It is also indicated to increase survival in patients acutely exposed to myelosuppressive doses of radiation (Hematopoietic Subsyndrome of Acute Radiation Syndrome).6

Associated Conditions
Contraindications & Blackbox Warnings
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Pegfilgrastim is a recombinant human granulocyte colony-stimulating factor (G-CSF) that promotes the production, proliferation, and maturation of neutrophils, which are white blood cells involved in both innate and adaptive immune responses.4,9 The safety and efficacy of pegfilgrastim in reducing the risk of febrile neutropenia and infections have been demonstrated in various tumor types and settings.4

During chemotherapy-induced neutropenia, the clearance of pegfilgrastim is significantly reduced and the concentration of pegfilgrastim is sustained until the onset of neutrophil recovery.1 Serum concentrations of pegfilgrastim decline as the neutrophil count increases as neutrophil and neutrophil precursors are involved in cell-mediated clearance of the drug.2 Due the addition of polyethylene glycol group to its structure, Pegfilgrastim is a long-acting form of filgrastim with an extended serum half-life and reduced renal clearance.3 Although it is more slowly absorbed than filgrastim, self-regulation of pegfilgrastim is more efficient and the drug effects are maintained during one chemotherapy cycle (2-3 weeks).1

Mechanism of action

Neutrophils are short-lived immune cells that are highly susceptible to cell death following myelosuppressive chemotherapy. This marked reduction in neutrophil numbers during chemotherapy increases the risk of hospitalization, infection, and infection-related mortality. It also directly impacts the clinical outcome of patients if cases of febrile neutropenia requires dose reductions or schedule delay of chemotherapy, thus reducing the clinical efficacy of chemotherapy and patient benefit from receiving appropriate treatment.4

G-CSF is an endogenous haematopoietic growth factor that stimulates granulopoietic cells of the neutrophil lineage. Pegfilgrastim mimics its biological actions and binds to the same G-CSF receptor expressed on cells of myeloid lineage, such as granulocytic precursors and mature neutrophils.1 Upon binding of the ligand, G-CSF receptor undergoes a conformational change and activates several downstream signalling pathways including JAK/STAT, PI3K/AKT and MAPK/ERK.5 These pathways work to increase proliferation and differentiation of granulocyte progenitor cells, induce maturation of the progenitor cells, and enhance survival and function of mature neutrophils.1

AGranulocyte colony-stimulating factor receptor

Pegfilgrastim has a lower absolute bioavailability than filgrastim following subcutaneous administration. The absorption of pegfilgrastim is largely dependent on the lymphatic system due to the attached PEG group contributing to the large size of the drug. It is slowly absorbed following subcutaneous administration with a time to peak concentration (Tmax) of about 1-2 days.1

Volume of distribution

Pegfilgrastim appears to have a volume of distribution of approximately 170L.[A33290]

Protein binding

The plasma protein binding of pegfilgrastim is unlikely.12


It is not know whether pegfilgrastim is metabolized into major metabolites.12 Once it binds to the therapeutic target, pegfilgrastim is internalized by the neutrophil and undergoes nonspecific degradation.1

Route of elimination

The polyethylene glycol moiety limits the renal clearance by glomerular filtration of pegfilgrastim, making neutrophil-mediated clearance as the predominant route of elimination.3 This elimination pathway is initiated by the binding of pegfilgrastim to the G-CSF receptor on the neutrophil cell surface, leading to the internalization of the pegfilgrastim-receptor complex via endocytosis and subsequent degradation inside the cell. While hepatic clearance has not been well characterized for pegfilgrastim, its non-PEGylated precursor filgrastim is known to be unaffected by changes in hepatic clearance.1


The serum half-life of Pegfilgrastim is highly variable depending on the absolute neutrophil count, with the range of 15 to 80 hours following subcutaneous administration. The median serum half-life of 42 hours.3,6


Pegfilgrastim has a self-regulating clearance that involves neutrophil-induced clearance.1,4 The clearance is dependent on the number of neutrophils and body weight of the patient: the clearance increases with increasing number of granulocytes and lower body weights.6 Pegfilgrastim is not eliminated from the circulation until neutrophils start to recover following chemotherapy-induced neutropenia and its clearance is increased as neutrophil counts also increase.4 The apparent serum clearance is 14 mL/h/kg.12

Adverse Effects
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The maximum safe dose of pegfilgrastim has not been established; however, the highest dose used in clinical trials was 300 mcg/kg.9 Overdosage of pegfilgrastim may result in leukocytosis and bone pain. Events of edema, dyspnea, and pleural effusion have been reported in a single patient who self-administered pegfilgrastim on 8 consecutive days in error. In the event of overdose, the patient should be monitored for signs and symptoms of toxicity and responded with appropriate general supportive care.6,9

Affected organisms
  • Humans and other mammals
Not Available
Pharmacogenomic Effects/ADRs
Not Available


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.
Antihemophilic Factor (Recombinant), PEGylatedThe therapeutic efficacy of Antihemophilic Factor (Recombinant), PEGylated can be decreased when used in combination with Pegfilgrastim.
Certolizumab pegolThe therapeutic efficacy of Certolizumab pegol can be decreased when used in combination with Pegfilgrastim.
CyclophosphamideThe risk or severity of pulmonary toxicity can be increased when Pegfilgrastim is combined with Cyclophosphamide.
Damoctocog alfa pegolThe therapeutic efficacy of Damoctocog alfa pegol can be decreased when used in combination with Pegfilgrastim.
ElapegademaseThe therapeutic efficacy of Elapegademase can be decreased when used in combination with Pegfilgrastim.
LipegfilgrastimThe therapeutic efficacy of Lipegfilgrastim can be decreased when used in combination with Pegfilgrastim.
Methoxy polyethylene glycol-epoetin betaThe therapeutic efficacy of Methoxy polyethylene glycol-epoetin beta can be decreased when used in combination with Pegfilgrastim.
Nonacog beta pegolThe therapeutic efficacy of Nonacog beta pegol can be decreased when used in combination with Pegfilgrastim.
PegademaseThe therapeutic efficacy of Pegademase can be decreased when used in combination with Pegfilgrastim.
PegaptanibThe therapeutic efficacy of Pegaptanib can be decreased when used in combination with Pegfilgrastim.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

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  • Action

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Food Interactions
No interactions found.


Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
FulphilaInjection6 mg/0.6mLSubcutaneousMylan Institutional LLC2018-07-09Not applicableUS flag
FulphilaSolution10 mgSubcutaneousBgp Pharma Ulc2020-02-07Not applicableCanada flag
LapelgaSolutionSubcutaneousApotex Corporation2019-02-27Not applicableCanada flag
NeulastaInjection6 mg/0.6mLSubcutaneousPhysicians Total Care, Inc.2006-02-232011-12-31US flag
NeulastaInjection6 mg/0.6mLSubcutaneousAMGEN INC2002-04-01Not applicableUS flag
NeulastaSolution10 mgSubcutaneousAmgen2004-03-12Not applicableCanada flag
NeulastaKit6 mg/0.6mLSubcutaneousAMGEN INC2002-04-01Not applicableUS flag
NeupopegInjection, solution6 mgSubcutaneousDompé Biotec S.P.A.2002-08-222008-12-22EU flag
NeupopegInjection, solution6 mgSubcutaneousDompé Biotec S.P.A.2002-08-222008-12-22EU flag
NeupopegInjection, solution6 mgSubcutaneousDompé Biotec S.P.A.2002-08-222008-12-22EU flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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ATC Codes
L03AA13 — Pegfilgrastim
Drug Categories
Chemical TaxonomyProvided by Classyfire
Not Available
Organic Compounds
Super Class
Organic Acids
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Alternative Parents
Not Available
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available

Chemical Identifiers

CAS number


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]
  2. Curran MP, Goa KL: Pegfilgrastim. Drugs. 2002;62(8):1207-13; discussion 1214-5. doi: 10.2165/00003495-200262080-00012. [PubMed:12010086]
  3. Molineux G: The design and development of pegfilgrastim (PEG-rmetHuG-CSF, Neulasta). Curr Pharm Des. 2004;10(11):1235-44. doi: 10.2174/1381612043452613. [PubMed:15078138]
  4. Arvedson T, O'Kelly J, Yang BB: Design Rationale and Development Approach for Pegfilgrastim as a Long-Acting Granulocyte Colony-Stimulating Factor. BioDrugs. 2015 Jun;29(3):185-98. doi: 10.1007/s40259-015-0127-4. [PubMed:25998211]
  5. Dwivedi P, Greis KD: Granulocyte colony-stimulating factor receptor signaling in severe congenital neutropenia, chronic neutrophilic leukemia, and related malignancies. Exp Hematol. 2017 Feb;46:9-20. doi: 10.1016/j.exphem.2016.10.008. Epub 2016 Oct 24. [PubMed:27789332]
  6. Neulasta (pegfilgrastim) - FDA Label [Link]
  7. Neulasta Safety Data Sheet - Amgen [Link]
  8. Biosimilars of pegfilgrastim [Link]
  9. Pegfilgrastim - StatPearls - NCBI Bookshelf [Link]
  10. EMA approval for pegfilgrastim biosimilar Grasustek [Link]
  11. Biosimilar and Interchangeable Products | FDA [Link]
  12. pegfilgrastim | Cancer Care Ontario [Link]
PubChem Substance
Therapeutic Targets Database
RxList Drug Page Drug Page
AHFS Codes
  • 20:16.00 — Hematopoietic Agents

Clinical Trials

Clinical Trials
4CompletedPreventionBreast Cancer2
4CompletedPreventionBreast Cancer / Lung Cancers / Neutropenia / Non-Hodgkin's Lymphoma (NHL) / Ovarian Cancer1
4CompletedPreventionMalignant Lymphomas1
4CompletedPreventionMalignant Solid Tumours1
4CompletedTreatmentBreast Cancer1
4CompletedTreatmentNon-Hodgkin's Lymphoma (NHL)1
4CompletedTreatmentNon-Small Cell Lung Carcinoma (NSCLC)1
4Unknown StatusSupportive CareBreast Cancer / Neutropenia1
3Active Not RecruitingSupportive CareChemotherapy Induced Neutropenia2
3Active Not RecruitingTreatmentBreast Cancer4


Not Available
  • Amgen Inc.
  • Physicians Total Care Inc.
Dosage Forms
InjectionSubcutaneous6 mg/0.6mL
Injection, solutionCutaneous6 MG
KitSubcutaneous6 mg/0.6mL
SolutionCutaneous; Intramuscular6 MG
Injection, solution6 mg/0.6mL
SolutionSubcutaneous6 mg
Injection, solutionSubcutaneous6 mg
SolutionSubcutaneous10 mg
Injection, solution10 mg/1mL
Injection, solutionCutaneous; Intramuscular6 MG
Injection, solutionSubcutaneous6 mg/0.6mL
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)Region
CA1341537No2007-07-312024-07-31Canada flag
CA1339071No1997-07-292014-07-29Canada flag
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

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Experimental Properties
melting point (°C)60 °CLuo, P., Protein Science 11:1218-1226 (2002)


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 neutroph...
Gene Name
Uniprot ID
Uniprot Name
Granulocyte colony-stimulating factor receptor
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
Uniprot Name
Neutrophil elastase
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]
  6. Abdolzade-Bavil A, von Kerczek A, Cooksey BA, Kaufman T, Krasney PA, Pukac L, Gorlach M, Lammerich A, Scheckermann C, Allgaier H, Shen WD, Liu PM: Differential sensitivity of lipegfilgrastim and pegfilgrastim to neutrophil elastase correlates with differences in clinical pharmacokinetic profile. J Clin Pharmacol. 2016 Feb;56(2):186-94. doi: 10.1002/jcph.578. Epub 2015 Sep 1. [PubMed:26105553]

Drug created on June 13, 2005 07:24 / Updated on October 27, 2020 11:13

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