Filgrastim
Identification
- Name
- Filgrastim
- Accession Number
- DB00099
- Description
Chemotherapy-induced neutropenia (CIN) is a common and serious complication of myelosuppressive chemotherapy. It is associated with significant morbidity and mortality and can increase the cost of cancer therapy. In these cases, colony stimulating factor is necessary to restore important cells for immune function 3.
For over twenty years, granulocyte colony-stimulating factors (G-CSFs; filgrastims) have been a pillar of treatment and prevention of CIN, and have been found to reduce the risk of neutropenia across various patient settings, decrease the incidence of febrile neutropenia, reduce the incidence of infection, reduce the requirement for treatment with antibiotics, and accelerate neutrophil recovery 3.
Filgrastim is a recombinant, non-pegylated human granulocyte colony stimulating factor (G-CSF) analog. It is marketed as the brand name Neupogen by Amgen (initially approved in 1998) and as Nivestym, a biosimilar agent by Pfizer. Nivestym was approved by the FDA on July 20th, 2018 5. Between 1998 and the present, Neupogen/filgrastim has been approved for various indications 8.
Tbo-filgrastim, which is marketed by Sicor Biotech and FDA approved on August 29, 2012, contains the same active ingredient as Neupogen and is biologically similar, but it is formulated to be short-acting 10. On March 6, 2015, the FDA approved the biosimilar Zarxio (filgrastim-sndz) and is indicated for use in the same conditions as Neupogen. Zarxio is marketed by Sandoz 7.
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Haematopoietic growth factors - Protein Structure
- Protein Chemical Formula
- C845H1343N223O243S9
- Protein Average Weight
- 18800.0 Da
- Sequences
>Amino acid sequence for filgrastim MTPLGPASSLPQSFLLKCLEQVRKIQGDGAALQEKLCATYKLCHPEELVLLGHSLGIPWA PLSSCPSQALQLAGCLSQLHSGLFLYQGLLQALEGISPELGPTLDTLQLDVADFATTIWQ QMEELGMAPALQPTQGAMPAFASAFQRRAGGVLVASHLQSFLEVSYRVLRHLAQP
Download FASTA Format- Synonyms
- Filgrastim
- Filgrastim-aafi
- Filgrastim-sndz
- G-CSF
- Granulocyte Colony Stimulating Factor
- Tbo-filgrastim
Pharmacology
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- Indication
This drug is a leucocyte growth factor Label 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 Label.
Reduce the time to neutrophil recovery and the duration of fever, following induction or consolidation chemotherapy treatment in patients with acute myeloid leukemia (AML) Label
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 (BMT) Label
Mobilize autologous hematopoietic progenitor cells into the peripheral blood for collection by leukapheresis Label
Reduce the incidence and duration of sequelae of severe neutropenia (e.g.‚ fever‚ infections‚ oropharyngeal ulcers) in symptomatic patients with congenital neutropenia‚ cyclic neutropenia‚ or idiopathic neutropenia Label.
Neupogen is approved for treatment of patients with radiation-induced myelosuppression following a radiological/nuclear incident 6.
- Associated Conditions
- Associated Therapies
- Contraindications & Blackbox Warnings
- Contraindications & Blackbox WarningsWith our commercial data, access important information on dangerous risks, contraindications, and adverse effects.Our Blackbox Warnings cover Risks, Contraindications, and Adverse Effects
- Pharmacodynamics
Filgrastim binds to the G-CSF receptor and stimulates the production of neutrophils in the bone marrow Label. Colony-stimulating factors are glycoproteins which act on hematopoietic cells by binding to specific cell surface receptors, in turn, stimulating proliferation and differentiation 9.
G-CSF and its receptor are necessary for basal and stress-induced granulopoiesis, which forms neutrophils. Mice deficient in G-CSF or G-CSFR have severe neutropenia and reduced levels (~50%) of late-stage neutrophil precursors in the bone marrow under normal, resting conditions 4.
Endogenous G-CSF is a lineage-specific colony-stimulating factor that is produced by monocytes‚ fibroblasts, and endothelial cells. G-CSF regulates the production of neutrophils within the bone marrow and enhances neutrophil progenitor proliferation‚ differentiation, and selected end-cell functions (including enhanced phagocytic ability‚ priming of the cellular metabolism associated with respiratory burst‚ antibody-dependent killing, and enhanced expression of certain cell surface antigens). G-CSF is not species-specific and has demonstrated to have negligible direct in vivo or in vitro effects on the production or action of hematopoietic cell types other than the neutrophil and its lineage9.
- Mechanism of action
As a G-CSF analog, this drug controls the proliferation of committed progenitor cells and influences their maturation into mature neutrophils. Filgrastim also stimulates the release of neutrophils from bone marrow storage pools and decreases their time to maturation. Filgrastim acts to increase the phagocytic activity of mature neutrophils, thus allowing them to prevent infection. In patients receiving cytotoxic chemotherapy, filgrastim may accelerate neutrophil recovery, leading to a reduction in the duration of the neutropenic phase post chemotherapy Label.
Used in the treatment of chemotherapy-induced neutropenia by enhancing the production of neutrophils, filgrastim acts on hematopoietic cells by binding to specific cell surface receptors, thereby stimulating proliferation, differentiation, commitment, and end cell functional activation. In one efficacy study, levels of neutrophils returned to baseline by 21 days following completion of chemotherapy and the administration of tbo-filgrastim (fast-acting) 10.
In phase 1 studies involving 96 patients with various non-myeloid malignancies‚ filgrastim administration resulted in a dose-dependent increase in circulating neutrophil counts over the dose range of 1 to 70 mcg/kg/day.
This increase in neutrophil counts was seen whether filgrastim was administered intravenous (1 to 70 mcg/kg twice daily)‚ subcutaneous (1 to 3 mcg/kg once daily)‚ or by continuous subcutaneous (SC) infusion (3 to 11 mcg/kg/day). After the discontinuation of filgrastim therapy‚ neutrophil counts returned to baseline in most cases within only 4 days after Nevistym was used Label.
Target Actions Organism AGranulocyte colony-stimulating factor receptor stimulatorHumans UNeutrophil elastase other/unknownHumans - Absorption
Absorption and clearance of Neupogen follows first-order pharmacokinetics without concentration dependence. 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 2-8 hours Label. Filgrastim does not accumulate. It is estimated that when filgrastim is subcutaneously administered, the absolute bioavailability is approximately 62% and 71% for 375 mcg and 750 mcg doses respectively. When 5 mcg/kg tbo-filgrastim is subcutaneously administered, the absolute bioavailability is 33%. It takes 4-6 hours for tho-filgrastim to reach maximum concentration 10.
- Volume of distribution
150 mL/kg Label
- Protein binding
- Not Available
- Metabolism
- Not Available
- Route of elimination
Filgrastim products demonstrate nonlinear pharmacokinetics. The clearance is dependent on filgrastim product concentration in addition to neutrophil count. G-CSF receptor-mediated clearance is saturated by a high concentration of filgrastim products and is diminished by neutropenia. In addition, filgrastim products are cleared by the kidney 9.
- Half-life
Elimination half-life was approximately 3.5 hours in both normal subjects and cancer subjects Label
- Clearance
0.5 - 0.7 mL/minute/kg after SC administration of 3.45 mcg/kg and 11.5 mcg/kg in both normal subjects and cancer patients Label
- Adverse Effects
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- Toxicity
There are numerous adverse effects associated with Filgastrim. They are organized by organ system as follows:
Generalized effects
Serious allergic reactions, including anaphylaxis: Permanently discontinue NIVESTYM in patients with serious allergic reactions. With non-myeloid malignancies receiving myelosuppressive anti-cancer drugs (≥ 5% difference in incidence compared to placebo) are pyrexia, pain, rash, cough, and dyspnea Label. With AML (≥ 2% difference in incidence) are pain, epistaxis and rash Label. With severe chronic neutropenia (SCN) (≥ 5% difference in incidence) are pain, anemia, epistaxis, diarrhea, hypoesthesia, and alopecia Label.
Musculoskeletal system
Exacerbation of arthritic symptoms has been uncommonly observed 9.
Spleen
Fatal splenic rupture: Evaluate patients who report left upper abdominal or shoulder pain for an enlarged spleen or splenic rupture. Cases of splenomegaly and splenic rupture have been reported uncommonly following administration of filgrastim. Some cases of splenic rupture were fatal Label.
Respiratory system
Acute respiratory distress syndrome (ARDS): Evaluate patients who develop fever and lung infiltrates or respiratory distress for ARDS. Discontinue filgrastim in patients with ARDS Label. Pulmonary adverse effects, in particular interstitial lung disease, have been reported after G-CSF administration. Patients with a recent history of lung infiltrates or pneumonia may be at higher risk. The onset of pulmonary signs, such as cough, fever and dyspnea in association with radiological signs of pulmonary infiltrates and deterioration in pulmonary function may be preliminary signs of acute respiratory distress syndrome (ARDS). Filgrastim should be discontinued and appropriate treatment should be given 9.
Hematological system
Fatal sickle cell crises have occurred.
The granulocyte-colony stimulating factor can promote the malignant growth of myeloid cells in vitro and the same effects may be seen on some non-myeloid cells in vitro. The safety and efficacy of filgrastim administration in patients with myelodysplastic syndrome, or chronic myelogenous leukemia have not been established. Filgrastim is not indicated for use in these conditions. Particular care should be taken to distinguish the diagnosis of blast transformation of chronic myeloid leukemia from acute myeloid leukemia 9.
Capillary leak syndrome has been reported after granulocyte colony-stimulating factor administration, and is characterised by hypotension, hypoalbuminaemia, edema and hemoconcentration. Patients who show symptoms of capillary leak syndrome must be closely monitored and receive standard symptomatic treatment, which may include a need for intensive care 9.
Leukocytosis (white blood cell (WBC) > 50 x 109/l) was seen in 41% of donors and transient thrombocytopenia (platelets < 100 x 109/l) following filgrastim and leukapheresis was observed in 35% of donors 9.
Renal system
This drug increases the risk of glomerulonephritis. Evaluate and consider dose-reduction or interruption of filgrastim if causality is likely Label.
- Affected organisms
- Humans and other mammals
- 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 softwareBleomycin 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. Vindesine The risk or severity of peripheral neuropathy can be increased when Filgrastim is combined with Vindesine. Vinflunine The risk or severity of peripheral neuropathy can be increased when Filgrastim is combined with Vinflunine. Vinorelbine The risk or severity of peripheral neuropathy can be increased when Filgrastim is combined with Vinorelbine. Improve patient outcomesBuild effective decision support tools with the industry’s most comprehensive drug-drug interaction checker.Learn more - Food Interactions
- No interactions found.
Products
- Comprehensive & structured drug product infoFrom application numbers to product codes, connect different identifiers through our commercial datasets.Easily connect various identifiers back to our datasets
- 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 Region Image Accofil Injection, solution 48000000 U/0.5ml Intravenous; Subcutaneous Accord Healthcare S.L.U. 2016-09-07 Not applicable EU Accofil Injection, solution 30000000 U/0.5ml Intravenous; Subcutaneous Accord Healthcare S.L.U. 2016-09-07 Not applicable EU Accofil Injection, solution 30000000 U/0.5ml Intravenous; Subcutaneous Accord Healthcare S.L.U. 2016-09-07 Not applicable EU Accofil Injection, solution 48000000 U/0.5ml Intravenous; Subcutaneous Accord Healthcare S.L.U. 2016-09-07 Not applicable EU Accofil Injection, solution 30000000 U/0.5ml Intravenous; Subcutaneous Accord Healthcare S.L.U. 2016-09-07 Not applicable EU Accofil Injection, solution 48000000 U/0.5ml Intravenous; Subcutaneous Accord Healthcare S.L.U. 2016-09-07 Not applicable EU Accofil Injection, solution 48000000 U/0.5ml Intravenous; Subcutaneous Accord Healthcare S.L.U. 2016-09-07 Not applicable EU Accofil Injection, solution 30000000 U/0.5ml Intravenous; Subcutaneous Accord Healthcare S.L.U. 2016-09-07 Not applicable EU Accofil Injection, solution 30000000 U/0.5ml Intravenous; Subcutaneous Accord Healthcare S.L.U. 2016-09-07 Not applicable EU Accofil Injection, solution 48000000 U/0.5ml Intravenous; Subcutaneous Accord Healthcare S.L.U. 2016-09-07 Not applicable EU
Categories
- ATC Codes
- L03AA02 — Filgrastim
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Antineoplastic and Immunomodulating Agents
- Biological Factors
- Colony-Stimulating Factors
- Glycoconjugates
- Glycoproteins
- Granulocyte Colony-Stimulating Factors
- Hematologic Agents
- Hematopoietic Cell Growth Factors
- Increased Myeloid Cell Production
- Leukocyte Growth Factor
- Peptides
- 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
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
- Wang B, Ludden TM, Cheung EN, Schwab GG, Roskos LK: Population pharmacokinetic-pharmacodynamic modeling of filgrastim (r-metHuG-CSF) in healthy volunteers. J Pharmacokinet Pharmacodyn. 2001 Aug;28(4):321-42. [PubMed:11677930]
- Krzyzanski W, Wiczling P, Lowe P, Pigeolet E, Fink M, Berghout A, Balser S: Population modeling of filgrastim PK-PD in healthy adults following intravenous and subcutaneous administrations. J Clin Pharmacol. 2010 Sep;50(9 Suppl):101S-112S. doi: 10.1177/0091270010376966. [PubMed:20881223]
- 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. [PubMed:24237790]
- 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. [PubMed:18400509]
- FDA Approves Second Neupogen Biosimilar, Nivestym [Link]
- FDA Approves Radiation Medical Countermeasure [Link]
- Zarxio [Link]
- Drugs Approved by the FDA document [Link]
- EMA label [File]
- TBO filgrastim [File]
- External Links
- UniProt
- P09919
- Genbank
- X03438
- KEGG Drug
- D03235
- PubChem Substance
- 46505833
- 1433764
- ChEMBL
- CHEMBL1201567
- Therapeutic Targets Database
- DAP000113
- PharmGKB
- PA449626
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Filgrastim
- AHFS Codes
- 20:16.00 — Hematopoietic Agents
- FDA label
- Download (2.27 MB)
- MSDS
- Download (125 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Diagnostic Diabetes Mellitus 1 4 Completed Prevention Breast Cancer 1 4 Completed Prevention Mycoses 1 4 Completed Supportive Care Breast Cancer 1 4 Completed Treatment Acute Myeloblastic Leukemia / Myelodysplastic Syndrome 1 4 Completed Treatment Adult Acute Lymphocytic Leukemia 2 4 Completed Treatment Anemia / Graft Versus Host Disease (GVHD) / Leukemias / Malignant Lymphomas / Multiple Myeloma and Plasma Cell Neoplasm / Myelodysplastic Syndromes (MDS) 1 4 Completed Treatment Asherman's Syndrome / Endometrium; Atrophy, Cervix 1 4 Completed Treatment Burkitt's Lymphoma / Large Cell Anaplastic Lymphoma / Lymphoma, Lymphoblastic / Mediastinal Neoplasms 1 4 Completed Treatment Early Breast Cancer 2
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Amgen Inc.
- Physicians Total Care Inc.
- Dosage Forms
Form Route Strength Injection, solution Intravenous; Subcutaneous 30000000 U/0.5ml Injection, solution Intravenous; Subcutaneous 48000000 U/0.5ml Injection Parenteral 30 MIO.E./0.5ML Injection Parenteral 0.5 ML 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 Injection, solution Intravenous; Subcutaneous 30 MIU Injection, solution Intravenous; Subcutaneous 48 MIU 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 30 miu/0.5ml Solution 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 Injection, solution Subcutaneous 48 MU/0.5ml Solution Intravenous; Subcutaneous Solution Subcutaneous 300 mcg Solution Subcutaneous 480 mcg Injection 300 MCG/ML Injection Intravenous; Subcutaneous 15 miu Injection Intravenous; Subcutaneous 30 miu Injection Intravenous; Subcutaneous 30 miu/ml 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 600 mcg Injection, solution Intravenous; Subcutaneous 0.3 MG/ML Injection Parenteral 300 µg/0.5ml Injection Parenteral Injection, solution Intravenous; Subcutaneous 300 mcg/0.5ml Injection Parenteral 480 µg/0.5ml Injection Parenteral 480 UG Injection, solution Intravenous; Subcutaneous 480 mcg/0.5ml Injection Parenteral 480 UG/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 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, solution Intravenous; Subcutaneous 120 mcg/0.2ml Injection, solution Intravenous 30 MU/0.5ml Injection Parenteral 05 ML Injection, solution Intravenous 48 MU/0.5ml 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 300 cg 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 30 MIU/0.5mL Injection, solution Intravenous; Subcutaneous 48 MIU/0.8mL Injection, solution Intravenous; Subcutaneous 300 ug/0.5mL Injection, solution Intravenous; Subcutaneous 480 ug/0.8mL Injection, solution Intravenous; Subcutaneous 30 MU Injection, solution Intravenous; Subcutaneous 48 MU 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 Solution Intravenous; Subcutaneous 30 million IU Injection, solution - 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 Canada CA1339071 No 1997-07-29 2014-07-29 Canada
Properties
- State
- Liquid
- Experimental Properties
Property Value Source melting point (°C) 4 MSDS boiling point (°C) 100 MSDS hydrophobicity 0.209 Not Available isoelectric point 5.65 Not Available
Targets

- 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. [PubMed:17001306]
- 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. [PubMed:17494858]
- 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]
- 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]
- 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]
- EMA label [File]
- TBO filgrastim [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Other/unknown
- 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
- 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]
- 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]
- Donini M, Fontana S, Savoldi G, Vermi W, Tassone L, Gentili F, Zenaro E, Ferrari D, Notarangelo LD, Porta F, Facchetti F, Notarangelo LD, Dusi S, Badolato R: G-CSF treatment of severe congenital neutropenia reverses neutropenia but does not correct the underlying functional deficiency of the neutrophil in defending against microorganisms. Blood. 2007 Jun 1;109(11):4716-23. Epub 2007 Feb 20. [PubMed:17311988]
- 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]
- 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]
- El Ouriaghli F, Fujiwara H, Melenhorst JJ, Sconocchia G, Hensel N, Barrett AJ: Neutrophil elastase enzymatically antagonizes the in vitro action of G-CSF: implications for the regulation of granulopoiesis. Blood. 2003 Mar 1;101(5):1752-8. Epub 2002 Oct 17. [PubMed:12393522]
Drug created on June 13, 2005 13:24 / Updated on February 24, 2021 19:34