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Identification
NameSargramostim
Accession NumberDB00020  (BTD00035, BIOD00035)
TypeBiotech
GroupsApproved, Investigational
DescriptionSargramostim 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.
Protein structureDb00020
Related Articles
Protein chemical formulaC639H1006N168O196S8
Protein average weight14434.5 Da
Sequences
>DB00020 sequence
APARSPSPSTQPWEHVNAIQEALRLLNLSRDTAAEMNETVEVISEMFDLQEPTCLQTRLE
LYKQGLRGSLTKLKGPLTMMASHYKQHCPPTPETSCATQIITFESFKENLKDFLLVIPFD
CWEPVQE
Download FASTA Format
Synonyms
GM-CSF
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
LeukineInjection, powder, for solution250 ug/mLIntravenous; SubcutaneousSanofi Aventis U.S. Llc1991-05-01Not applicableUs
LeukineLiquid500 ug/mLIntravenous; SubcutaneousSanofi Aventis U.S. Llc1996-12-01Not applicableUs
LeukineInjection, powder, for solution250 ug/mLIntravenous; SubcutaneousGenzyme Corporation2010-03-152016-06-30Us
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
LeucomaxNovartis
Brand mixturesNot Available
SaltsNot Available
Categories
UNII5TAA004E22
CAS number123774-72-1
Pharmacology
IndicationFor the treatment of cancer and bone marrow transplant
Structured Indications
PharmacodynamicsSargramostim 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 actionSargramostim 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
TargetKindPharmacological actionActionsOrganismUniProt ID
Granulocyte-macrophage colony-stimulating factor receptor subunit alphaProteinyes
agonist
HumanP15509 details
Interleukin-3 receptor subunit alphaProteinyes
agonist
HumanP26951 details
Cytokine receptor common subunit betaProteinyes
agonist
HumanP32927 details
Syndecan-2Proteinunknown
agonist
HumanP34741 details
Bone marrow proteoglycanProteinunknownNot AvailableHumanP13727 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot 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)]
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
BleomycinThe risk or severity of adverse effects can be increased when Sargramostim is combined with Bleomycin.Approved
CyclophosphamideThe risk or severity of adverse effects can be increased when Cyclophosphamide is combined with Sargramostim.Approved, Investigational
Food InteractionsNot Available
References
Synthesis Reference

Kaname Sugimoto, “Process for the production of human colony-stimulating factor.” U.S. Patent US4621050, issued May, 1983.

US4621050
General ReferencesNot Available
External Links
ATC CodesL03AA09
AHFS CodesNot Available
PDB Entries
FDA labelNot Available
MSDSNot Available
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Injection, powder, for solutionIntravenous; Subcutaneous250 ug/mL
LiquidIntravenous; Subcutaneous500 ug/mL
Prices
Unit descriptionCostUnit
Leukine 250 mcg vial204.79USD vial
Bio-immunex capsule0.42USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1341150 No2000-12-052017-12-05Canada
Properties
StateLiquid
Experimental Properties
PropertyValueSource
isoelectric point5.05Not Available
Taxonomy
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

Targets

Kind
Protein
Organism
Human
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
Molecular Weight:
46206.185 Da
References
  1. 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. [PubMed:17090651 ]
  2. 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. [PubMed:16760463 ]
  3. 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. [PubMed:17522711 ]
  4. 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. [PubMed:16638185 ]
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
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
Molecular Weight:
43329.585 Da
References
  1. 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. [PubMed:17562355 ]
  2. 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. [PubMed:17500228 ]
  3. 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. [PubMed:16698686 ]
  4. 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. [PubMed:17522711 ]
Kind
Protein
Organism
Human
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
Molecular Weight:
97334.89 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. 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. [PubMed:17016423 ]
  3. 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. [PubMed:1424804 ]
Kind
Protein
Organism
Human
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
Molecular Weight:
22159.62 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. 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. [PubMed:17016423 ]
  3. 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. [PubMed:10734053 ]
Kind
Protein
Organism
Human
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 as a proteinase inhibitor, reducing the activity of PAPPA.
Gene Name:
PRG2
Uniprot ID:
P13727
Molecular Weight:
25205.345 Da
References
  1. 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. [PubMed:17383764 ]
  2. 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. [PubMed:16522458 ]
  3. 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. [PubMed:17600316 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23