==== Reference: Usmani SS, Bedi G, Samuel JS, Singh S, Kalra S, Kumar P, et al. (2017) THPdb: Database of FDA-approved peptide and protein therapeutics. PLoS ONE 12(7) e0181748.====

Detailed description page of THPdb

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1117 details
Primary information
ThPP IDTh1016
Therapeutic Peptide/Protein NamePegfilgrastim
SequenceMTPLGPASSLPQSFLLKCLEQVRKIQGDGAALQEKLCATYKLCHPEELVL view full sequnce in fasta
Functional ClassificationIb
Molecular Weight18802.8
Chemical FormulaC845H1343N223O243S9
Isoelectric Point5.65
Hydrophobicity0.209
Melting Point (℃)60
Half Life15-80 hours
DescriptionPEGylated(at N terminus) form of human G-CSF (Granulocyte colony stimulating factor), 175 residues, produced from E. coli via bacterial fermentation.
Indication/DiseaseIncreases leukocyte production, for treatment in non-myeloid cancer, neutropenia and bone marrow transplant
PharmacodynamicsUsed in the treatment of chemotherapy-induced neutropenia by enhancing the production of neutrophils. Pegfilgrastim acts on hematopoietic cells by binding to specific cell surface receptors thereby stimulating proliferation, differentiation, commitment and end cell functional activation. Pegfilgrastim has reduced renal clearance and prolonged persistence in vivo as compared to Filgrastim.
Mechanism of ActionPegfilgrastim binds to the G-CSF receptor. As a G-CSF analog, it controls proliferation of committed progenitor cells and influences their maturation into mature neutrophils. Pegfilgrastim also stimulates the release of neutrophils from bone marrowstorage pools and reduces their maturation time. Pegfilgrastim acts to increase the phagocytic activity of mature neutrophils. In patients receiving cytotoxic chemotherapy, pegfilgrastim can accelerate neutrophil recovery, leading to a reduction in duration of the neutropenic phase
ToxicityN.A.
MetabolismN.A.
AbsorptionN.A.
Volume of DistributionN.A.
ClearanceFilgrastim is primarily eliminated by the kidney and neutrophils/neutrophil precursors; the latter presumably involves binding of the growth factor to the G-CSF receptor on the cell surface, internalization of the growth factor-receptor complexes via endo
CategoriesImmunosuppressive Agents
Patents NumberCA1341537
Date of Issue31/07/07
Date of Expiry31/07/24
Drug InteractionN.A.
TargetGranulocyte colony-stimulating factor receptor,Neutrophil elastase
Information of corresponding available drug in the market
Brand NameNeulasta
CompanyAmgen Inc.
Brand DiscriptionNeulasta is a covalent conjugate of recombinant methionyl human G-CSF/Filgrastim and monomethoxypolyethylene glycol. Filgrastim (175 amino acid, 19 kilodaltons (kD)) is a water-soluble protein. Filgrastim is obtained from the bacterial fermentation of a s
Prescribed forNeulasta is used to prevent neutropenia(lack of certain white blood cells caused by receiving chemotherapy).
Chemical NameN.A.
FormulationSupplied in 0.6 mL prefilled syringes. Each syringe contains 6 mg pegfilgrastim (based on protein weight) in a sterile, clear, colorless, preservative-free solution (pH 4.0) containing acetate (0.35 mg), polysorbate 20 (0.02 mg), sodium (0.02 mg), and sor
Physcial AppearnceSolution
Route of AdministrationSubcutaneous Injection
Recommended DosageSingle subcutaneous injection of 6 mg administered once per chemotherapy cycle in adults. Do not administer Neulasta between 14 days before and 24 hours after administration of cytotoxic chemotherapy.
ContraindicationAllergy, or having sickle cell disorder; chronic myeloid leukemia; myelodysplasia (also called preleukemia); or if you are allergic to latex.
Side EffectsBone pain; pain in your arms or legs; or bruising, swelling, pain, redness, or a hard lump where the injection was given.
Useful Linkhttp://www.drugs.com/neulasta.html
PubMed ID21456630, 25594147, 25581410, 25524005
3-D StructureTh1016 (View) or (Download)