Sargramostim

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 Conditions

• Acute Lymphoblastic Leukemia (ALL)
• Hematopoietic Subsyndrome of Acute Radiation Syndrome
• Lymphoma, Hodgkins
• Neutropenia
• Non-Hodgkin's Lymphoma (NHL)
• Severe Infection

Associated Therapies

• Allogenic bone marrow transplantation therapy
• Autologous bone marrow transplantation therapy
• Autologous peripheral hematopoietic stem cell transplant

Contraindications & Blackbox Warnings

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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	agonist	Humans
AInterleukin-3 receptor subunit alpha	agonist	Humans
ACytokine receptor common subunit beta	agonist	Humans
USyndecan-2	agonist	Humans
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

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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.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
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Bleomycin	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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Food Interactions

No interactions found.

Products

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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	Subcutaneous	Berlex	2007-12-06	2007-12-06
Leukine	Injection, powder, for solution	250 ug/1mL	Subcutaneous	Bayer	1991-09-05	2012-09-21
Leukine	Injection, powder, for solution	250 ug/1mL	Intravenous; Subcutaneous	Genzyme Corporation	2010-03-15	2016-06-30
Leukine	Injection, solution	500 ug/1mL	Intravenous; Subcutaneous	Partner Therapeutics, Inc	1991-03-05	2012-05-08
Leukine	Injection, powder, for solution	250 ug/1mL	Intravenous; Subcutaneous	Sanofi Aventis	1991-05-01	2021-12-30
Leukine	Liquid	500 ug/1mL	Subcutaneous	Bayer	1991-03-05	2012-09-21
Leukine	Liquid	500 ug/1mL	Intravenous; Subcutaneous	Genzyme Corporation	2010-03-15	2013-12-31
Leukine	Injection, powder, lyophilized, for solution	250 ug/1mL	Intravenous; Subcutaneous	Partner Therapeutics, Inc	1991-03-05	Not applicable
Leukine	Liquid	500 ug/1mL	Intravenous; Subcutaneous	Sanofi Aventis	1996-12-01	2021-12-30
Leukine	Liquid	500 ug/1mL	Intravenous; Subcutaneous	Physicians Total Care, Inc.	1996-12-01	2012-06-30

Categories

ATC Codes

L03AA09 — Sargramostim

• L03AA — Colony stimulating factors
• L03A — IMMUNOSTIMULANTS
• L03 — IMMUNOSTIMULANTS
• L — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Drug Categories

• Adjuvants, Immunologic
• Amino Acids, Peptides, and Proteins
• Antineoplastic and Immunomodulating Agents
• Biological Factors
• Carbohydrates
• Colony-Stimulating Factors
• Cytokines
• Glycoconjugates
• 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

RxNav

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

Phase	Status	Purpose	Conditions	Count
4	Active Not Recruiting	Treatment	Critical Injury (Trauma) in Children	1
4	Completed	Treatment	Coronavirus Disease 2019 (COVID‑19)	1
4	Completed	Treatment	Leukemia, Myeloblastic, Acute	1
4	Completed	Treatment	Malignant Melanoma of Skin	1
4	Recruiting	Treatment	Pediatric Sepsis-induced MODS	1
3	Active Not Recruiting	Treatment	Localized Resectable Neuroblastoma / Localized Unresectable Neuroblastoma / Recurrent Neuroblastoma / Regional Neuroblastoma / Stage 4 Neuroblastoma / Stage 4S Neuroblastoma	1
3	Completed	Prevention	Breast Cancer With Low to Intermediate HER2 Expression	1
3	Completed	Prevention	Iris Melanoma / Medium/Large Size Posterior Uveal Melanoma / Mucosal Melanoma / Ocular Melanoma With Extraocular Extension / Recurrent Melanoma / Recurrent Uveal Melanoma / Small Size Posterior Uveal Melanoma / Stage IIA Cutaneous Melanoma AJCC v6 and v7 / Stage IIA Uveal Melanoma AJCC v7 / Stage IIB Cutaneous Melanoma AJCC v6 and v7 / Stage IIB Uveal Melanoma AJCC v7 / Stage IIC Cutaneous Melanoma AJCC v6 and v7 / Stage IIIA Cutaneous Melanoma AJCC v7 / Stage IIIA Uveal Melanoma AJCC v7 / Stage IIIB Cutaneous Melanoma AJCC v7 / Stage IIIB Uveal Melanoma AJCC v7 / Stage IIIC Cutaneous Melanoma AJCC v7 / Stage IIIC Uveal Melanoma AJCC v7 / Stage IV Cutaneous Melanoma AJCC v6 and v7 / Stage IV Uveal Melanoma AJCC v7	1
3	Completed	Supportive Care	Head and Neck Carcinoma / Oral Complications / Radiation Toxicity	1
3	Completed	Supportive Care	Head and Neck Carcinoma / Oral Mucositis / Radiation Toxicity / Tongue Cancers	1

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

Properties

State

Liquid

Experimental Properties

Property	Value	Source
isoelectric point	5.05	Not Available

Targets

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Details1. Granulocyte-macrophage colony-stimulating factor receptor subunit alpha

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

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

Details2. Interleukin-3 receptor subunit alpha

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

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. [Article]
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. [Article]
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. [Article]
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. [Article]

Details3. Cytokine receptor common subunit beta

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

1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
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. [Article]
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. [Article]

Details4. Syndecan-2

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

1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
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. [Article]
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. [Article]

Details5. Bone marrow proteoglycan

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

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. [Article]
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. [Article]
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. [Article]

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Drug created on June 13, 2005 13:24 / Updated on May 21, 2021 10:20