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| Primary information |
|---|
| ID | 10117 |
| Therapeutic ID | Th1016 |
| Protein Name | Pegfilgrastim |
| Sequence | >Th1016_Pegfilgrastim
MTPLGPASSLPQSFLLKCLEQVRKIQGDGAALQEKLCATYKLCHPEELVLLGHSLGIPWAPLSSCPSQALQLAGCLSQLHSGLFLYQGLLQALEGISPELGPTLDTLQLDVADFATTIWQQMEELGMAPALQPTQGAMPAFASAFQRRAGGVLVASHLQSFLEVSYRVLRHLAQP
|
| Molecular Weight | 39000 |
| Chemical Formula | C845H1343N223O243S9 |
| Isoelectric Point | 5.65 |
| Hydrophobicity | 0.209 |
| Melting point | 60 |
| Half-life | 15-80 hours |
| Description | PEGylated(at N terminus) form of human G-CSF (Granulocyte colony stimulating factor), 175 residues, produced from E. coli via bacterial fermentation. |
| Indication/Disease | Increases leukocyte production, for treatment in non-myeloid cancer, neutropenia and bone marrow transplant |
| Pharmacodynamics | Used 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 Action | Pegfilgrastim 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 |
| Toxicity | Overdosage of pegfilgrastim may result in leukocytosis and bone pain. Events of edema, dyspnea, and pleural effusion have been reported in a single patient who self-administered pegfilgrastim on 8 consecutive days in error. |
| Metabolism | It is not know whether pegfilgrastim is metabolized into major metabolites.13 Once it binds to the therapeutic target, pegfilgrastim is internalized by the neutrophil and undergoes nonspecific degradation |
| Absorption | lower absolute bioavailability |
| approximately 170L |
| Clearance | 14 mL/h/kg |
| Categories | Adjuvants, Immunologic, Alcohols, Amino Acids, Peptides, and Proteins, Antineoplastic and Immunomodulating Agents, Biological Factors, Carbohydrates, Colony-Stimulating Factors, Compounds used in a research, industrial, or household setting, Cytokines, Ethylene Glycols, Glycoconjugates, Glycols, Glycoproteins, Granulocyte Colony-Stimulating Factors, Hematinics, Hematopoietic Cell Growth Factors, Increased Myeloid Cell Production, Intercellular Signaling Peptides and Proteins, Leukocyte Growth Factor, Macromolecular Substances, Pegylated agents, Peptides, Polymers, Proteins |
| Patents Number | CA1341537 |
| Date of Issue | 31-Jul-2007 |
| Date of Expiry | 31-Jul-2024 |
| Drug Interaction | NA |
| Target | Granulocyte colony-stimulating factor receptor,Neutrophil elastase |
| Brand Name | Neulasta |
| Company | Amgen Inc. |
| Brand Description | Amgen Inc. |
| Prescribed For | Neulasta is used to prevent neutropenia(lack of certain white blood cells caused by receiving chemotherapy). |
| Chemical Name | NA |
| Formulation | Supplied 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 |
| Physical Appearance | Solution |
| Route of Administration | Subcutaneous Injection |
| Recommended Dosage | Single 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. |
| Contraindication | Allergy, or having sickle cell disorder; chronic myeloid leukemia; myelodysplasia (also called preleukemia); or if you are allergic to latex. |
| Side Effects | Bone pain; pain in your arms or legs; or bruising, swelling, pain, redness, or a hard lump where the injection was given. |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |