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Identification
NameSargramostim
Accession NumberDB00020  (BIOD00035, BTD00035)
Typebiotech
Groupsapproved, investigational
Description

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.

Protein structureDb00020
Protein chemical formulaC639H1006N168O196S8
Protein average weight14434.5000
Sequences
>DB00020 sequence
APARSPSPSTQPWEHVNAIQEALRLLNLSRDTAAEMNETVEVISEMFDLQEPTCLQTRLE
LYKQGLRGSLTKLKGPLTMMASHYKQHCPPTPETSCATQIITFESFKENLKDFLLVIPFD
CWEPVQE
Download FASTA Format
Synonyms
SynonymLanguageCode
GM-CSFNot AvailableNot Available
SaltsNot Available
Brand names
NameCompany
LeucomaxNovartis
LeukineBerlex Laboratories Inc
Brand mixturesNot Available
Categories
CAS number83869-56-1
Taxonomy
KingdomOrganic Compounds
SuperclassOrganic Acids
ClassCarboxylic Acids and Derivatives
SubclassAmino Acids, Peptides, and Analogues
Direct parentPeptides
Alternative parentsNot Available
SubstituentsNot Available
Classification descriptionNot Available
Pharmacology
IndicationFor the treatment of cancer and bone marrow transplant
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
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
Metabolism
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
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Injection, powder, for solutionIntravenous drip
Injection, powder, for solutionSubcutaneous
Injection, solutionIntravenous drip
Injection, solutionSubcutaneous
Prices
Unit descriptionCostUnit
Leukine 250 mcg vial204.79USDvial
Bio-immunex capsule0.42USDcapsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
CountryPatent NumberApprovedExpires (estimated)
Canada13411502000-12-052017-12-05
Properties
Stateliquid
Experimental Properties
PropertyValueSource
isoelectric point5.05Not Available
References
Synthesis Reference

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

US4621050
General ReferenceNot Available
External Links
ResourceLink
UniProtP04141
GenbankM13207
PharmGKBPA164748631
RxListhttp://www.rxlist.com/cgi/generic/sargramostim.htm
Drugs.comhttp://www.drugs.com/cdi/sargramostim.html
WikipediaSargramostim
ATC CodesL03AA09
AHFS CodesNot Available
PDB Entries
FDA labelNot Available
MSDSNot Available
Interactions
Drug InteractionsNot Available
Food InteractionsNot Available

Targets

1. Granulocyte-macrophage colony-stimulating factor receptor subunit alpha

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: agonist

Components

Name UniProt ID Details
Granulocyte-macrophage colony-stimulating factor receptor subunit alpha P15509 Details

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
  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
  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
  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
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

2. Interleukin-3 receptor subunit alpha

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: agonist

Components

Name UniProt ID Details
Interleukin-3 receptor subunit alpha P26951 Details

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
  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
  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
  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

3. Cytokine receptor common subunit beta

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: agonist

Components

Name UniProt ID Details
Cytokine receptor common subunit beta P32927 Details

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
  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
  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

4. Syndecan-2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: agonist

Components

Name UniProt ID Details
Syndecan-2 P34741 Details

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
  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
  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

5. Bone marrow proteoglycan

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Bone marrow proteoglycan P13727 Details

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
  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
  3. Kang JH, Lee DH, Seo HM, 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 Jun 28;. Pubmed

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Drug created on June 13, 2005 07:24 / Updated on October 03, 2013 20:55