Identification
- Summary
Sargramostim is a modified form of recombinant human granulocyte-macrophage colony stimulating factor used to increase immune cell production after myelosuppressive therapy or bone marrow transplant.
- Brand Names
- Leukine
- Generic Name
- Sargramostim
- DrugBank Accession Number
- DB00020
- Background
Sargramostim is a human recombinant granulocyte macrophage colony-stimulating factor (GM-CSF) expressed in yeast. It is a glycoprotein that is 127 residues. Substitution of Leu23 leads to a difference from native protein.
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Haematopoietic growth factors - Protein Structure
- Protein Chemical Formula
- C639H1006N168O196S8
- Protein Average Weight
- 14434.5 Da
- Sequences
>DB00020 sequence APARSPSPSTQPWEHVNAIQEALRLLNLSRDTAAEMNETVEVISEMFDLQEPTCLQTRLE LYKQGLRGSLTKLKGPLTMMASHYKQHCPPTPETSCATQIITFESFKENLKDFLLVIPFD CWEPVQE
Download FASTA Format- Synonyms
- Recombinant human granulocyte-macrophage colony stimulating factor
- rGM-CSF
- rHu GM-CSF
- Sargramostim
- External IDs
- B1 61.012
- B1-61012
Pharmacology
- Indication
For the treatment of cancer and bone marrow transplant
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- Associated Therapies
- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- Pharmacodynamics
Sargramostim is used in the treatment of bone marrow transplant recipients or those exposed to chemotherapy an recovering from acut myelogenous leukemia, Leukine or GM-CSF is a hematopoietic growth factor which stimulates the survival, clonal expansion (proliferation) and differentiation of hematopoietic progenitor cells. GM-CSF is also capable of activating mature granulocytes and macrophages. After a bone marrow transplant or chemotherapy, patients have a reduced capacity to produce red and white blood cells. Supplementing them with external sources of GM-CSF helps bring the level of neutrophils back to normal so that they can better fight infections.
- Mechanism of action
Sargramostim binds to the Granulocyte-macrophage colony stimulating factor receptor (GM-CSF-R-alpha or CSF2R) which stimulates a JAK2 STAT1/STAT3 signal transduction pathway. This leads to the production of hemopoietic cells and neutrophils
Target Actions Organism AGranulocyte-macrophage colony-stimulating factor receptor subunit alpha agonistHumans AInterleukin-3 receptor subunit alpha agonistHumans ACytokine receptor common subunit beta agonistHumans USyndecan-2 agonistHumans UBone marrow proteoglycan Not Available Humans - 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
- 420 mL/min/m2 [Normal people with liquid LEUKINE (IV)]
- 431 mL/min/m2 [Normal people with lyophilized LEUKINE (IV)]
- 549 mL/min/m2 [Normal people with liquid LEUKINE (SC)]
- 529 mL/min/m2 [Normal people with lyophilized LEUKINE (SC)]
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.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 softwareBleomycin The risk or severity of adverse effects can be increased when Sargramostim is combined with Bleomycin. Cyclophosphamide The risk or severity of adverse effects can be increased when Cyclophosphamide is combined with Sargramostim. Vinblastine The risk or severity of peripheral neuropathy can be increased when Sargramostim is combined with Vinblastine. Vincristine The risk or severity of peripheral neuropathy can be increased when Sargramostim is combined with Vincristine. Vindesine The risk or severity of peripheral neuropathy can be increased when Sargramostim is combined with Vindesine. Vinflunine The risk or severity of peripheral neuropathy can be increased when Sargramostim is combined with Vinflunine. Vinorelbine The risk or severity of peripheral neuropathy can be increased when Sargramostim is combined with Vinorelbine. 
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- No interactions found.
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.- International/Other Brands
- Leucomax (Novartis)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Leukine Liquid 500 ug/1mL Intravenous; Subcutaneous Physicians Total Care, Inc. 1996-12-01 2012-06-30 US 
Leukine Liquid 500 ug/1mL Subcutaneous Berlex 2007-12-06 2007-12-06 US Leukine Injection, powder, for solution 250 ug/1mL Subcutaneous Bayer 1991-09-05 2012-09-21 US Leukine Injection, powder, for solution 250 ug/1mL Intravenous; Subcutaneous Genzyme Corporation 2010-03-15 2016-06-30 US Leukine Injection, solution 500 ug/1mL Intravenous; Subcutaneous Partner Therapeutics, Inc 1991-03-05 2012-05-08 US Leukine Injection, powder, for solution 250 ug/1mL Intravenous; Subcutaneous Sanofi Aventis 1991-05-01 2021-12-30 US Leukine Liquid 500 ug/1mL Subcutaneous Bayer 1991-03-05 2012-09-21 US Leukine Liquid 500 ug/1mL Intravenous; Subcutaneous Genzyme Corporation 2010-03-15 2013-12-31 US Leukine Injection, powder, lyophilized, for solution 250 ug/1mL Intravenous; Subcutaneous Partner Therapeutics, Inc 1991-03-05 Not applicable US Leukine Liquid 500 ug/1mL Intravenous; Subcutaneous Sanofi Aventis 1996-12-01 2021-12-30 US
Categories
- ATC Codes
- L03AA09 — Sargramostim
- Drug Categories
- Adjuvants, Immunologic
- Amino Acids, Peptides, and Proteins
- Antineoplastic and Immunomodulating Agents
- Biological Factors
- Colony-Stimulating Factors
- Cytokines
- Glycoproteins
- Granulocyte-Macrophage Colony-Stimulating Factor
- Hematopoietic Cell Growth Factors
- Immunologic Factors
- Increased Myeloid Cell Production
- Intercellular Signaling Peptides and Proteins
- 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
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 5TAA004E22
- CAS number
- 123774-72-1
References
- Synthesis Reference
Kaname Sugimoto, "Process for the production of human colony-stimulating factor." U.S. Patent US4621050, issued May, 1983.
US4621050- General References
- Not Available
- External Links
- UniProt
- P04141
- Genbank
- M13207
- PubChem Substance
- 46507000
- 69634
- ChEMBL
- CHEMBL1201670
- Therapeutic Targets Database
- DAP001053
- PharmGKB
- PA164748631
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Sargramostim
Clinical Trials
- Clinical Trials
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Bayer Healthcare
- Genzyme Inc.
- Hospira Inc.
- Kramer-Novis
- Physicians Total Care Inc.
- Wyeth Pharmaceuticals
- Dosage Forms
Form Route Strength Injection, powder, for solution Intravenous; Subcutaneous 250 ug/1mL Injection, powder, for solution Subcutaneous 250 ug/1mL Injection, powder, lyophilized, for solution Intravenous; Subcutaneous 250 ug/1mL Injection, solution Intravenous; Subcutaneous 500 ug/1mL Liquid Intravenous; Subcutaneous 500 ug/1mL Liquid Subcutaneous 500 ug/1mL - Prices
Unit description Cost Unit Leukine 250 mcg vial 204.79USD vial Bio-immunex capsule 0.42USD capsule DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA1341150 No 2000-12-05 2017-12-05 Canada 
Properties
- State
- Liquid
- Experimental Properties
Property Value Source isoelectric point 5.05 Not Available
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Receptor activity
- Specific Function
- Low affinity receptor for granulocyte-macrophage colony-stimulating factor. Transduces a signal that results in the proliferation, differentiation, and functional activation of hematopoietic cells.
- Gene Name
- CSF2RA
- Uniprot ID
- P15509
- Uniprot Name
- Granulocyte-macrophage colony-stimulating factor receptor subunit alpha
- Molecular Weight
- 46206.185 Da
References
- Wang Y, Cai D, Brendel C, Barett C, Erben P, Manley PW, Hochhaus A, Neubauer A, Burchert A: Adaptive secretion of granulocyte-macrophage colony-stimulating factor (GM-CSF) mediates imatinib and nilotinib resistance in BCR/ABL+ progenitors via JAK-2/STAT-5 pathway activation. Blood. 2007 Mar 1;109(5):2147-55. Epub 2006 Nov 7. [Article]
- Chen J, Carcamo JM, Golde DW: The alpha subunit of the granulocyte-macrophage colony-stimulating factor receptor interacts with c-Kit and inhibits c-Kit signaling. J Biol Chem. 2006 Aug 4;281(31):22421-6. Epub 2006 Jun 7. [Article]
- Lencz T, Morgan TV, Athanasiou M, Dain B, Reed CR, Kane JM, Kucherlapati R, Malhotra AK: Converging evidence for a pseudoautosomal cytokine receptor gene locus in schizophrenia. Mol Psychiatry. 2007 Jun;12(6):572-80. Epub 2007 Mar 20. [Article]
- Xiao R, Zhang R, Wang YL, Zhu ZL, Chen T, Yang JH: [Expression of soluble GM-CSF-Ralpha in patients with acute myeloid leukemia]. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2006 Apr;14(2):225-7. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Interleukin-3 receptor activity
- Specific Function
- This is a receptor for interleukin-3.
- Gene Name
- IL3RA
- Uniprot ID
- P26951
- Uniprot Name
- Interleukin-3 receptor subunit alpha
- Molecular Weight
- 43329.585 Da
References
- Eksioglu EA, Mahmood SS, Chang M, Reddy V: GM-CSF promotes differentiation of human dendritic cells and T lymphocytes toward a predominantly type 1 proinflammatory response. Exp Hematol. 2007 Aug;35(8):1163-71. Epub 2007 Jun 11. [Article]
- Sakhno LV, Leplina OIu, Tikhonova MA, Raspai ZhM, Gileva IP, Nikonov SD, Zhdanov OA, Ostanin AA, Chernykh ER: [Characteristics of A-interferon-generated dendritic cells in patients with pulmonary tuberculosis]. Probl Tuberk Bolezn Legk. 2007;(3):42-6. [Article]
- Ward KA, Stewart LA, Schwarer AP: CD34+-derived CD11c+ + + BDCA-1+ + CD123+ + DC: expansion of a phenotypically undescribed myeloid DC1 population for use in adoptive immunotherapy. Cytotherapy. 2006;8(2):130-40. [Article]
- Lencz T, Morgan TV, Athanasiou M, Dain B, Reed CR, Kane JM, Kucherlapati R, Malhotra AK: Converging evidence for a pseudoautosomal cytokine receptor gene locus in schizophrenia. Mol Psychiatry. 2007 Jun;12(6):572-80. Epub 2007 Mar 20. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Receptor activity
- Specific Function
- High affinity receptor for interleukin-3, interleukin-5 and granulocyte-macrophage colony-stimulating factor.
- Gene Name
- CSF2RB
- Uniprot ID
- P32927
- Uniprot Name
- Cytokine receptor common subunit beta
- Molecular Weight
- 97334.89 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Shen Y, Baker E, Callen DF, Sutherland GR, Willson TA, Rakar S, Gough NM: Localization of the human GM-CSF receptor beta chain gene (CSF2RB) to chromosome 22q12.2-->q13.1. Cytogenet Cell Genet. 1992;61(3):175-7. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Pdz domain binding
- Specific Function
- Cell surface proteoglycan that bears heparan sulfate. Regulates dendritic arbor morphogenesis (By similarity).
- Gene Name
- SDC2
- Uniprot ID
- P34741
- Uniprot Name
- Syndecan-2
- Molecular Weight
- 22159.62 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Modrowski D, Basle M, Lomri A, Marie PJ: Syndecan-2 is involved in the mitogenic activity and signaling of granulocyte-macrophage colony-stimulating factor in osteoblasts. J Biol Chem. 2000 Mar 31;275(13):9178-85. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Heparin binding
- Specific Function
- Cytotoxin and helminthotoxin. Also induces non-cytolytic histamine release from human basophils. Involved in antiparasitic defense mechanisms and immune hypersensitivity reactions. The proform acts...
- Gene Name
- PRG2
- Uniprot ID
- P13727
- Uniprot Name
- Bone marrow proteoglycan
- Molecular Weight
- 25205.345 Da
References
- Menon K, Wu Y, Haas J, Sahu SK, Yang B, Zaheer A: Diminished degradation of myelin basic protein by anti-sulfatide antibody and interferon-gamma in myelin from glia maturation factor-deficient mice. Neurosci Res. 2007 Jun;58(2):156-63. Epub 2007 Feb 22. [Article]
- Letuve S, Lajoie-Kadoch S, Audusseau S, Rothenberg ME, Fiset PO, Ludwig MS, Hamid Q: IL-17E upregulates the expression of proinflammatory cytokines in lung fibroblasts. J Allergy Clin Immunol. 2006 Mar;117(3):590-6. Epub 2006 Feb 8. [Article]
- Kang JH, Lee da H, Seo H, Park JS, Nam KH, Shin SY, Park CS, Chung IY: Regulation of functional phenotypes of cord blood derived eosinophils by gamma-secretase inhibitor. Am J Respir Cell Mol Biol. 2007 Nov;37(5):571-7. Epub 2007 Jun 28. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 03, 2022 21:04