Filgrastim

Identification

Summary

Filgrastim is a form of recombinant human granulocyte colony stimulating factor used to induce the production of granulocytes and lower infection risk after myelosuppressive therapy.

Brand Names

Accofil, Granix, Grastofil, Neupogen, Nivestim, Nivestym, Ratiograstim, Releuko, Zarxio, Zarzio

Generic Name

Filgrastim

DrugBank Accession Number

DB00099

Background

Filgrastim is a short-acting recombinant, non-pegylated human granulocyte colony-stimulating factor (G-CSF) analog produced by recombinant DNA technology. It has an amino acid sequence identical to endogenous G-CSF, but it is non-glycosylated unlike the endogenous G-CSF and has an N-terminal methionine added in the sequence for expression in E. Coli.⁸ Human G-CSF is a glycoprotein that regulates the production and release of neutrophils from the bone marrow. Filgrastim mimics the biological actions of G-CSF to increase the levels of neutrophils in the blood.¹⁰ It has a number of therapeutic uses, including the management and prevention of infections and febrile neutropenia in patients receiving myelosuppressive chemotherapy or radiation therapy. It is also used to manage severe chronic neutropenia and mobilize hematopoietic progenitor cells to the peripheral blood for collection by leukapheresis in patients undergoing peripheral blood progenitor cell collection and therapy.⁸

Filgrastim was approved in the US in 1991 and there are biosimilars available with similar therapeutic indications.³ Tbo-filgrastim was approved by the FDA on August 29, 2012.⁹ Filgrastim-sndz was approved on March 6, 2015 ¹² and filgrastim-ayow was approved on March 2, 2022.¹³ A long-acting, pegylated G-CSF, pegfilgrastim, was made available to increase the duration of action of the drug.

Type

Biotech

Groups

Approved

Biologic Classification

Protein Based Therapies
Haematopoietic growth factors

Protein Structure

Protein Chemical Formula: C₈₄₅H₁₃₃₉N₂₂₃O₂₄₃S₉
Protein Average Weight: 18800.0 Da (approximate)

Sequences

>Protein sequence
MTPLGPASSLPQSFLLKCLEQVRKIQGDGAALQEKLCATYKLCHPEELVLLGHSLGIPWA
PLSSCPSQALQLAGCLSQLHSGLFLYQGLLQALEGISPELGPTLDTLQLDVADFATTIWQ
QMEELGMAPALQPTQGAMPAFASAFQRRAGGVLVASHLQSFLEVSYRVLRHLAQP

References:

KEGG DRUG: Filgrastim [Link]

Download FASTA Format

Synonyms

Filgrastim
Filgrastim-aafi
Filgrastim-sndz
G-CSF
Granulocyte Colony Stimulating Factor
Tbo-filgrastim

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Pharmacology

Indication

Filgrastim is indicated to decrease the incidence of infection‚ as manifested by febrile neutropenia‚ in patients with nonmyeloid malignancies receiving myelosuppressive anti-cancer drugs associated with a significant incidence of severe neutropenia with fever.⁸

Filgrastim is indicated for reducing the time to neutrophil recovery and the duration of fever, following induction or consolidation chemotherapy treatment of patients with acute myeloid leukemia.⁸

Filgrastim is indicated to reduce the duration of neutropenia and neutropenia-related clinical sequelae‚ e.g.‚ febrile neutropenia, in patients with nonmyeloid malignancies undergoing myeloablative chemotherapy followed by bone marrow transplantation.⁸

Filgrastim is indicated for the mobilization of autologous hematopoietic progenitor cells into the peripheral blood for collection by leukapheresis.⁸

Filgrastim is indicated for chronic administration to reduce the incidence and duration of sequelae of neutropenia (e.g.‚ fever‚ infections‚ oropharyngeal ulcers) in symptomatic patients with congenital neutropenia‚ cyclic neutropenia‚ or idiopathic neutropenia.⁸

Filgrastim is indicated to increase survival in patients acutely exposed to myelosuppressive doses of radiation.⁸

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Associated Conditions

Indication Type	Indication	Approval Level	Patient Characteristics
Management of	Congenital neutropenia	••••••••••••
Management of	Cyclic neutropenia	••••••••••••
Prevention of	Febrile neutropenia	••••••••••••	••••••••••• ••••••••••••
Management of	Hematopoietic subsyndrome of acute radiation syndrome	••••••••••••
Prevention of	Infection	••••••••••••	••••••••••• ••••••••••••

Associated Therapies

Mobilization of hematopoietic progenitor cells into peripheral blood for collection by leukapheresis therapy

Contraindications & Blackbox Warnings

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Pharmacodynamics

Filgrastim is used to reduce the incidence, severity and duration of neutropenia and febrile neutropenia in patients undergoing cytotoxic chemotherapy. In clinical trials in patients, filgrastim reduced the duration of febrile neutropenia, antibiotic use, and hospitalization after induction chemotherapy for acute myelogenous leukemia or myeloablative therapy followed by bone marrow transplantation; however, the incidence of fever and documented infections were not reduced in either setting.¹⁰

Filgrastim is also used to mobilize hematopoietic progenitor cells into the peripheral blood in order to reduce the risk for bleeding complications and the need for platelet transfusions. Recipients of allogeneic PBPCs mobilized with filgrastim experienced significantly more rapid hematological recovery, leading to a significant decrease in time to unsupported platelet recovery when compared with allogeneic bone marrow transplantation.¹⁰

Filgrastim causes a dose-dependent increase in circulating neutrophil counts within 24 hours of administration. Filgrastim can also cause a minor increase in monocyte and lymphocyte counts, but the clinical significance of these effects is unknown.⁸ In some patients, filgrastim also caused a minor increase in the number of circulating eosinophils and basophils relative to baseline; however, these patients may already have had elevated eosinophils and basophils prior to filgrastim treatment. Following termination of filgrastim therapy, circulating neutrophil counts decrease by 50% within one to two days, and to normal levels within one to seven days. As with other hematopoietic growth factors, G-CSF has shown in vitro stimulating properties on human endothelial cells.¹⁰

Mechanism of action

Neutrophils are critical granulocytes involved in the acute inflammatory response and host defences against bacterial infections.⁵ They also contribute to long-term adaptive immunity by promoting immediate host immune response and attracting other cells, such as macrophages and dendritic cells. As neutrophils promote both the initiation and the maintenance of inflammation at sites of infection, suppressed neutrophil responses lead to extreme susceptibility to infection.² Low neutrophil levels, or neutropenia, caused by chronic neutropenia, myelosuppressive chemotherapy, and radiation therapy increases the risk of infection and related events.⁴ Neutropenia caused by chemotherapy or radiation therapy can further progress into febrile neutropenia, which is associated with an elevated risk for life-threatening systemic infections and chemotherapy-associated morbidity and mortality.¹

The production and release of functional neutrophils from the bone marrow are normally regulated by granulocyte colony-stimulating factors (G-CSF), which are major cytokine regulators of neutrophilic granulocytes.² G-CSFs act on hematopoietic cells by binding to specific cell surface receptors to stimulate the proliferation‚ differentiation‚ and maturation of neutrophil progenitors. G-CSF also induces some end-cell functional activation of neutrophils, including enhanced phagocytic ability‚ priming of the cellular metabolism associated with respiratory burst‚ antibody-dependent killing, and the increased expression of some cell surface antigens.⁸ Filgrastim is a short-acting recombinant G-CSF that mimics the biological actions of endogenous G-CSF. It also facilitates the release of neutrophils from the bone marrow into the blood to reduce the incidence of infection and manage neutropenia.^3,4

Target	Actions	Organism
AGranulocyte colony-stimulating factor receptor	stimulator	Humans

Absorption

Filgrastim exhibits nonlinear pharmacokinetics. Subcutaneous administration of 3.45 mcg/kg and 11.5 mcg/kg of filgrastim resulted in maximum serum concentrations of 4 and 49 ng/mL‚ respectively‚ within 2 to 8 hours.

Continuous 24-hour intravenous infusions of 20 mcg/kg over an 11 to 20-day period produced steady-state serum concentrations of filgrastim with no evidence of drug accumulation. The absolute bioavailability of filgrastim after subcutaneous administration is 60% to 70%.⁸

Volume of distribution

After intravenous administration, the volume of distribution averaged 150 mL/kg.⁸ There is no evidence of drug accumulation.¹⁰

Protein binding

There is limited information available.

Metabolism

Like other G-CSF compounds, filgrastim is cleared from plasma via neutrophil-mediated clearance involving internalization via G-CSF receptors and degradation within the neutrophil. Filgrastim is also subject to extracellular proteolytic degradation by neutrophil elastase: this enzyme rapidly cleaves filgrastim and renders it inactive.^6,7

Route of elimination

There is limited information available; however, filgrastim is subject to renal elimination.⁷

Half-life

After intravenous administration, the elimination half-life of filgrastim was approximately 3.5 hours in both normal subjects and patients with cancer. Single parenteral doses or daily intravenous doses‚ over a 14-day period‚ resulted in comparable half-lives. The half-lives were similar for intravenous administration (231 minutes‚ following doses of 34.5 mcg/kg) and for subcutaneous administration (210 minutes‚ following filgrastim dosages of 3.45 mcg/kg).⁸

Clearance

Clearance rates of filgrastim were approximately 0.5 to 0.7 mL/minute/kg after intravenous administration.⁸

Adverse Effects

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Toxicity

The oral LD₅₀ in mouse and rat was >3 mg/kg. The intravenous LD₅₀ in rat was also >3 mg/kg.¹¹

There is limited information regarding filgrastim overdose. The maximum tolerated dose of filgrastim has not been determined. In clinical trials of patients with cancer receiving myelosuppressive chemotherapy‚ white blood cell counts greater than 100,000/mm³ have been reported in less than 5% of patients‚ but were not associated with any reported adverse clinical effects. Patients in the bone marrow transplantation studies received up to 138 mcg/kg/day without toxic effects‚ although there was a flattening of the dose response curve above daily doses of greater than 10 mcg/kg/day.⁸

Pathways

Not Available

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Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">

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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Bleomycin	The risk or severity of pulmonary toxicity can be increased when Filgrastim is combined with Bleomycin.
Cyclophosphamide	The risk or severity of pulmonary toxicity can be increased when Filgrastim is combined with Cyclophosphamide.
Topotecan	The risk or severity of neutropenia can be increased when Filgrastim is combined with Topotecan.
Vinblastine	The risk or severity of peripheral neuropathy can be increased when Filgrastim is combined with Vinblastine.
Vincristine	The risk or severity of peripheral neuropathy can be increased when Filgrastim is combined with Vincristine.

Food Interactions

No interactions found.

Products

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International/Other Brands

Biocilin / Biofigran / Biofilgran / Endufil / Filatil / Filgen / Gran / Granulokine / Grimatin / Inmunef / Jiexin / Leucogen / Leucostim / Macroleuco / Neukine / Neutromax / Neutroval (Sicor Biotech) / Recombicyte / SciLocyte / Tevagastrim / White-C / Zarzio

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Accofil	Injection, solution	12000000 U/0.2ml	Intravenous; Subcutaneous	Accord Healthcare S.L.U.	2022-06-08	Not applicable
Accofil	Injection, solution	30000000 U/0.5ml	Intravenous; Subcutaneous	Accord Healthcare S.L.U.	2016-09-07	Not applicable
Accofil	Injection, solution	48000000 U/0.5ml	Intravenous; Subcutaneous	Accord Healthcare S.L.U.	2016-09-07	Not applicable
Accofil	Injection, solution	30000000 U/0.5ml	Intravenous; Subcutaneous	Accord Healthcare S.L.U.	2016-09-07	Not applicable
Accofil	Injection, solution	70000000 U/0.73ml	Intravenous; Subcutaneous	Accord Healthcare S.L.U.	2022-06-09	Not applicable

Chemical Identifiers

UNII: PVI5M0M1GW
CAS number: 121181-53-1

References

Synthesis Reference

Tetsuro Kuga, Hiromasa Miyaji, Moriyuki Sato, Masami Okabe, Makoto Morimoto, Seiga Itoh, Motoo Yamasaki, Yoshiharu Yokoo, Kazuo Yamaguchi, Hajime Yoshida, Yoshinori Komatsu, "Method of producing a polypeptide having human granulocyte colony stimulating factor activity." U.S. Patent US5994518, issued February, 1988.

US5994518

General References

Kamioner D, Fruehauf S, Maloisel F, Cals L, Lepretre S, Berthou C: Study design: two long-term observational studies of the biosimilar filgrastim Nivestim (Hospira filgrastim) in the treatment and prevention of chemotherapy-induced neutropenia. BMC Cancer. 2013 Nov 16;13:547. doi: 10.1186/1471-2407-13-547. [Article]
Panopoulos AD, Watowich SS: Granulocyte colony-stimulating factor: molecular mechanisms of action during steady state and 'emergency' hematopoiesis. Cytokine. 2008 Jun;42(3):277-88. doi: 10.1016/j.cyto.2008.03.002. Epub 2008 Apr 8. [Article]
Aghedo BO, Gupta V: Filgrastim . [Article]
Dale DC, Crawford J, Klippel Z, Reiner M, Osslund T, Fan E, Morrow PK, Allcott K, Lyman GH: A systematic literature review of the efficacy, effectiveness, and safety of filgrastim. Support Care Cancer. 2018 Jan;26(1):7-20. doi: 10.1007/s00520-017-3854-x. Epub 2017 Sep 22. [Article]
Boxer L, Dale DC: Neutropenia: causes and consequences. Semin Hematol. 2002 Apr;39(2):75-81. doi: 10.1053/shem.2002.31911. [Article]
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. [Article]
Scholz M, Ackermann M, Engel C, Emmrich F, Loeffler M, Kamprad M: A pharmacokinetic model of filgrastim and pegfilgrastim application in normal mice and those with cyclophosphamide-induced granulocytopaenia. Cell Prolif. 2009 Dec;42(6):813-22. doi: 10.1111/j.1365-2184.2009.00638.x. Epub 2009 Aug 17. [Article]
DailyMed Label: NEUPOGEN (filgrastim) injection, for subcutaneous or intravenous use [Link]
DailyMed Label; GRANIX (tbo-filgrastim) injection, for subcutaneous use [Link]
EMA Summary of Product Characteristics: HEXAL (filgrastim) subcutaneous or intravenous injection [Link]
Hospira Safety Data Sheet: NIVESTYM (Filgrastim-aafi) [Link]
Drugs@FDA: Zarxio (filgrastim-sndz) [Link]
Business Wire News: Kashiv Biosciences Receives Approval for Its First Biosimilar RELEUKOTM (filgrastim-ayow) [Link]
FDA Approved Drug Products: NEUPOGEN® (filgrastim) injection, for subcutaneous or intravenous use [Link]
FDA Approved Drug Products: NIVESTYM™ (filgrastim-aafi) injection, for subcutaneous or intravenous use [Link]

External Links

UniProt: P09919
Genbank: X03438
KEGG Drug: D03235
PubChem Substance: 46505833
RxNav: 1433764
ChEMBL: CHEMBL1201567
Therapeutic Targets Database: DAP000113
PharmGKB: PA449626
RxList: RxList Drug Page
Drugs.com: Drugs.com Drug Page
Wikipedia: Filgrastim

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">

Phase	Status	Purpose	Conditions	Count
4	Active Not Recruiting	Treatment	Stage I Breast Cancer	1
4	Completed	Diagnostic	Diabetes Mellitus	1
4	Completed	Prevention	Breast Cancer	1
4	Completed	Prevention	Fungal Infections	1
4	Completed	Supportive Care	Breast Cancer	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Amgen Inc.
Physicians Total Care Inc.

Dosage Forms

Form	Route	Strength
Injection, solution	Intravenous; Subcutaneous	12000000 U/0.2ml
Injection, solution	Intravenous; Subcutaneous	30000000 U/0.5ml
Injection, solution	Intravenous; Subcutaneous	48000000 U/0.5ml
Injection, solution	Intravenous; Subcutaneous	70000000 U/0.73ml
Injection, solution	Parenteral; Subcutaneous	12 MU/0.2ml
Injection, solution	Parenteral; Subcutaneous	70 MU/0.73ml
Injection	Parenteral	30 MIO.E./0.5ML
Injection	Parenteral	0.5 ML
Injection, solution	Intravenous; Subcutaneous	300 mcg/0.5mL
Injection	Parenteral	30 MIO E/0.5ML
Injection	Parenteral	48 MIO.E./0.5ML
Injection	Parenteral	48 MIO E/0.5ML
Solution	Intravenous; Subcutaneous	300 mcg
Solution	Intravenous; Subcutaneous	480 mcg
Solution	Parenteral	300.0 mcg
Injection, solution	Intravenous; Subcutaneous	30 MIU
Injection, solution	Intravenous; Subcutaneous	48 MIU
Solution	Subcutaneous	300.000 mg
Solution	Intravenous; Subcutaneous	30000000 mcg
Injection, solution	Intravenous; Subcutaneous	60 MU/ml
Injection, solution	Intravenous; Subcutaneous	96 MU/ml
Injection	Parenteral	0.3 mg
Injection	Parenteral	0.48 mg
Injection	Intravenous
Injection	Intravenous	30 miu/0.5ml
Injection	Intravenous	48 miu/0.5ml
Solution		300 mcg/1ml
Injection, solution	Subcutaneous	300 ug/1mL
Injection, solution	Subcutaneous	480 ug/1.6mL
Injection, solution, concentrate	Intravenous; Subcutaneous	30 MU/ml
Injection, solution, concentrate	Subcutaneous	300 mcg
Injection, solution, concentrate	Subcutaneous	480 mcg
Solution	Subcutaneous	300.00 mcg
Injection, solution	Subcutaneous	48 MU/0.5ml
Solution	Intravenous; Subcutaneous	300 mcg / 0.5 mL
Solution	Intravenous; Subcutaneous	480 mcg / 0.8 mL
Solution	Parenteral	300 mcg
Solution	Subcutaneous	300 mcg
Solution	Subcutaneous	480 mcg
Injection
Injection	Intravenous; Subcutaneous	15 miu
Injection	Intravenous; Subcutaneous
Injection	Intravenous; Subcutaneous	30 miu
Injection, solution		480 mcg/ml
Injection	Intravenous; Subcutaneous	30 miu/ml
Solution	Subcutaneous	300.00 µg
Injection, solution		30 MU
Injection, solution		48 MU
Injection, solution	Intravenous	300 ug/0.5mL
Injection, solution	Intravenous	300 ug/1mL
Injection, solution	Intravenous	480 ug/0.8mL
Solution	Intravenous; Subcutaneous	300 mcg / mL
Solution	Intravenous; Subcutaneous	600 mcg / mL
Solution	Subcutaneous	0.300 mg
Injection	Parenteral	300 µg/0.5ml
Injection	Parenteral	30 MIO.E.
Injection	Parenteral	300 UG/1ML
Injection	Parenteral	480 µg/0.5ml
Injection	Parenteral	48 MIO.E.
Injection	Parenteral	480 UG
Injection	Parenteral	480 UG/0.5ML
Injection	Intravenous; Subcutaneous	300 mcg/ml
Injection	Intravenous; Subcutaneous	480 mcg/1.6ml
Injection	Intravenous; Subcutaneous	30 mu/0.5ml
Injection	Intravenous; Subcutaneous	48 mu/0.5ml
Injection, solution	Intravenous; Subcutaneous	30 MU/0.5ML
Injection; solution	Intravenous; Subcutaneous	30 miu/0.5ml
Injection; solution	Intravenous; Subcutaneous	48 miu/0.5ml
Solution	Intravenous; Subcutaneous	30 millions of units
Injection, solution		480 mcg/1vial
Injection, solution	Intravenous; Subcutaneous	12 MU/0.2ml
Injection, solution	Intravenous; Subcutaneous	12000000 [units of filgrastim]/0.2mL
Injection, solution	Intravenous; Subcutaneous	30000000 [units of filgrastim]/0.5mL
Injection, solution	Intravenous; Subcutaneous	48 MU/0.5ml
Injection, solution	Intravenous; Subcutaneous	48000000 [units of filgrastim]/0.5mL
Injection	Parenteral	12 MIO E/0.2ML
Injection	Parenteral	0.2 ML
Injection, solution	Intravenous; Subcutaneous
Injection, solution	Intravenous drip; Subcutaneous	0.120 mg/0.2ml
Injection, solution	Intravenous
Solution	Intravenous drip; Subcutaneous	0.300 mg/0.5ml
Injection	Parenteral	05 ML
Solution	Intravenous drip; Subcutaneous	0.480 mg/0.5ml
Injection, solution	Intravenous; Subcutaneous	480 mcg/0.5ml
Injection, solution		120 mcg/0.2ml
Injection, solution	Intravenous; Subcutaneous	300 ug/1mL
Injection, solution	Intravenous; Subcutaneous	480 ug/1.6mL
Injection, solution	Subcutaneous	300 ug/0.5mL
Injection, solution	Subcutaneous	480 ug/0.8mL
Solution	Intravenous; Subcutaneous	480 mcg / 1.6 mL
Solution	Intravenous; Subcutaneous	300 cg
Injection, solution	Intravenous; Subcutaneous	30 MIU/0.5ml
Injection, solution	Intravenous; Subcutaneous	48 MIU/0.8ml
Injection	Parenteral	30 M UI/0.5 ml
Injection	Parenteral	48 M UI/0.8 ml
Injection	Parenteral	0.8 ML
Injection, solution	Intravenous; Subcutaneous	30 MUI/0.5ml
Injection, solution	Intravenous; Subcutaneous	300 µg/0.5 ml
Injection, solution	Intravenous; Subcutaneous	48 MUI/0.8ml
Injection, solution	Intravenous; Subcutaneous	480 µg/0.8 ml
Injection, solution	Intravenous; Subcutaneous	300 ug/0.5mL
Injection, solution	Intravenous; Subcutaneous	480 ug/0.8mL
Solution	Subcutaneous	300.000 mcg
Injection, solution		480 mcg/1ml
Injection	Parenteral	30 MIO E./0.5ML
Solution	Intravenous; Subcutaneous	300 mcg/0.5ml
Injection	Parenteral	48 MIO E./0.5ML
Solution	Intravenous; Subcutaneous	480 mcg/0.5ml
Injection, solution	Intravenous; Subcutaneous	0.3 mg/0.5ml
Solution	Intravenous; Subcutaneous	30 million IU
Injection, solution		10000 iu/10ml
Injection, solution		300 mcg/0.5ml
Injection, solution		480 mcg/0.5ml
Solution		300 mcg/1vial
Solution		480 mcg/1vial
Injection, solution		300 mcg/ml
Injection, solution		300 mcg/1ml

Prices

Unit description	Cost	Unit
Neupogen 480 mcg/0.8ml Solution 1 Box Contains Ten 0.8ml Syringes	4998.24USD	box
Neupogen 480 mcg/1.6ml Solution 1 Box Contains Ten 1.6ml Syringes	4554.58USD	box
Neupogen 300 mcg/0.5ml Solution 1 Box Contains Ten 0.5ml Syringes	3138.1USD	box
Neupogen 480 mcg/1.6 ml vial	437.94USD	ml
Neupogen 300 mcg/ml vial	286.04USD	vial

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

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
CA1341537	No	2007-07-31	2024-07-31
CA1339071	No	1997-07-29	2014-07-29

Properties

State

Liquid

Experimental Properties

Property	Value	Source
boiling point (°C)	100	https://www.msds.amgen.com/-/media/Themes/Amgen/msds-amgen-com/msds-amgen-com/documents/neupogen_safety_data_sheet_20130218_rev_3.pdf
isoelectric point	5.65	Not Available

Targets

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Details1. Granulocyte colony-stimulating factor receptor

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

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: CSF3R
Uniprot ID: Q99062
Uniprot Name: Granulocyte colony-stimulating factor receptor
Molecular Weight: 92155.615 Da

References

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. [Article]
Link DC, Kunter G, Kasai Y, Zhao Y, Miner T, McLellan MD, Ries RE, Kapur D, Nagarajan R, Dale DC, Bolyard AA, Boxer LA, Welte K, Zeidler C, Donadieu J, Bellanne-Chantelot C, Vardiman JW, Caligiuri MA, Bloomfield CD, DiPersio JF, Tomasson MH, Graubert TA, Westervelt P, Watson M, Shannon W, Baty J, Mardis ER, Wilson RK, Ley TJ: Distinct patterns of mutations occurring in de novo AML versus AML arising in the setting of severe congenital neutropenia. Blood. 2007 Sep 1;110(5):1648-55. Epub 2007 May 9. [Article]
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. [Article]
Ward AC: The role of the granulocyte colony-stimulating factor receptor (G-CSF-R) in disease. Front Biosci. 2007 Jan 1;12:608-18. [Article]
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. [Article]
EMA label [File]
TBO filgrastim [File]

Enzymes

Details1. Neutrophil elastase

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

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: ELANE
Uniprot ID: P08246
Uniprot Name: Neutrophil elastase
Molecular Weight: 28517.81 Da

References

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. [Article]
Scholz M, Ackermann M, Engel C, Emmrich F, Loeffler M, Kamprad M: A pharmacokinetic model of filgrastim and pegfilgrastim application in normal mice and those with cyclophosphamide-induced granulocytopaenia. Cell Prolif. 2009 Dec;42(6):813-22. doi: 10.1111/j.1365-2184.2009.00638.x. Epub 2009 Aug 17. [Article]

Drug created at June 13, 2005 13:24 / Updated at February 14, 2024 00:55

Filgrastim

Identification

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Pharmacology

Interactions

Products

Categories

Chemical Identifiers

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Clinical Trials

Pharmacoeconomics

Properties

Targets

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Enzymes

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