Lipegfilgrastim, Pegylated GCSF

Specification

• Cat#: THP-0083
• Product Name: Lipegfilgrastim, Pegylated GCSF
• Description: The product is a pegylated, recombinant granulocyte colony-stimulating factor (G-CSF) that was synthetized using a highly site-specific glycoPEGylation technology. The product is a covalent conjugate of Filgrastim with a single methoxy polyethylene glycol (PEG) molecule via a carbohydrate linker consisting of glycine, N-acetylneuraminic acid and N-acetylgalactosamine. The average molecular mass of the product comprises 18,798 Da for Filgrastim, 203 Da for GalNAc, 338 Da for glycylsialic acid and approximately 20,000 Da for PEG.
• Sequences: MTPLGPASSLPQSFLLKCLEQVRKIQGDGAALQEKLCATYKLCHPEELVLLGHSLGIPWAPLSSCPSQALQLAGCLSQLHSGLFLYQGLLQALEGISPELGPTLDTLQLDVADFATTIWQQMEELGMAPALQPTQGAMPAFASAFQRRAGGVLVASHLQSFLEVSYRVLRHLAQP
• Species: Human
• Molecular Weight: 39000.0 Da (glycoPEGylated, approximate)
• Purity: >99% by SDS-Page and HPLC analysis
• Cas No: 1117844-87-7
• Formula: C866H1372N226O258S9*(C2H4O)n
• Endotoxin Level: <0.001 EU per 1 μg by the LAL method
• Biological Activity: 6mg/vial

Pharmaceutical Information

• Pharmaceutical Application: Pegylated GCSF
• Applications: Indicated for the reduction in the duration of neutropenia and the incidence of febrile neutropenia in adult patients treated with cytotoxic chemotherapy for malignancy (with the exception of chronic myeloid leukaemia and myelodysplastic syndromes).
• Examples of Clinical Use: Reduction in the duration of neutropenia and the incidence of febrile neutropenia
• Pharmacodynamics: Mimicking endogenous granulocyte colony-stimulating factors, the product enhances the number and function of circulating neutrophils by binding to endogenous G-CSF receptors. A small increase in monocyte and/or lymphocyte counts may also be observed. Following a single subcutaneous dose administration of 100 μg/kg, the product resulted in a significant increase in neutrophilic granulocyte and large unstained cell counts. G-CSF also increases the antibacterial activities of neutrophils including the phagocytosis. Due to structural similarity between the product and pegfilgrastim, G-CSF receptor binding was equivalent between two molecules. However, the product showed greater time-dependent resistance to neutrophil elastase degradation and greater retention of activity than pegfilgrastim.
• Mechanism of action: Endogenous granulocyte colony-stimulating factor (G-CSF) is a glycoprotein that stimulates neutrophil progenitors. It is produced mainly by monocytes, fibroblasts and endothelial cells to promote the development of neutrophils and increase their proliferation and maturation. Subsequently, G-SCF stimulates the release of matured neutrophils from the bone marrow storage pools into the peripheral blood to enhance their function. Via binding to to the human G-CSF receptors, Pegylated GCSF activates the receptor signalling pathway as a growth factor to stimulate proliferation of haematopoietic progenitor cells and their differentiation into mature cells, and promote subsequent release into the peripheral blood. This stimulatory effect of Pegylated GCSF may extend to other single lineage and multilineage progenitors and pluripotent haematopoietic stem cells. The presence of the PEG moiety in Pegylated GCSF decreases the plasma clearance and extends the drug's terminal elimination half-life, allowing for less frequent dosing.
• Affected organisms: Not Available
• Targets: Target 1. Granulocyte colony-stimulating factor receptor

Related Reading

A basic introduction to Lipegfilgrastim, Pegylated GCSF

Lipegfilgrastim, also known as pegylated granulocyte colony-stimulating factor (GCSF), is a medication used to stimulate the production of white blood cells in the body. It is a pegylated form of GCSF, which means it has been modified with polyethylene glycol to prolong its effects in the body. Lipegfilgrastim is primarily used to prevent or reduce the severity of neutropenia, a condition characterized by a low level of neutrophils, a type of white blood cell that helps the body fight infection. Neutropenia is a common side effect of certain cancer treatments, such as chemotherapy, and can increase the risk of infection in patients undergoing these treatments.
By stimulating the production of white blood cells, lipegfilgrastim can help improve the body's ability to fight off infections and reduce the likelihood of developing febrile neutropenia, a potentially serious complication of chemotherapy. Lipegfilgrastim is typically administered by injection and is available by prescription. It is important to follow the dosing and administration instructions provided by a healthcare professional when using this medication. Like all medications, lipegfilgrastim may cause side effects, so it's essential to discuss any concerns with a healthcare provider.

Lipegfilgrastim, Pegylated GCSF function and mechanism

GCSF is a medication used to stimulate the production of white blood cells in the body. It is often used in cancer patients undergoing chemotherapy, as chemotherapy can suppress the bone marrow's ability to produce white blood cells, leading to an increased risk of infection.
Pegylated G-CSF works by stimulating the bone marrow to produce more white blood cells, particularly neutrophils, which are important for fighting off infections. The pegylation of G-CSF prolongs its activity in the body, reducing the frequency of injections required compared to non-pegylated forms.
Overall, Lipegfilgrastim helps to reduce the risk of infection in cancer patients undergoing chemotherapy by boosting their white blood cell count. This can be crucial in maintaining their overall health and ability to continue their cancer treatment.
Lipegfilgrastim is a pegylated form of granulocyte colony-stimulating factor (G-CSF). Pegylation is a process in which polyethylene glycol (PEG) molecules are attached to a protein or peptide, which can enhance the protein's half-life in the body and reduce its clearance.
In the case of Lipegfilgrastim, pegylation extends the half-life of G-CSF, allowing for a longer duration of action. G-CSF is a natural growth factor that stimulates the bone marrow to produce and release neutrophils, a type of white blood cell important for fighting infection. By prolonging the presence of G-CSF in the body, Lipegfilgrastim can enhance the production and function of neutrophils, which can be beneficial in certain medical situations, such as during chemotherapy or bone marrow transplantation.

Lipegfilgrastim, Pegylated GCSF produces results in the medical field

GSCF is a medication used in the medical field to stimulate the production of white blood cells in patients undergoing chemotherapy. Chemotherapy often leads to a decrease in white blood cell count, which can increase the risk of infection. Lipegfilgrastim works by stimulating the bone marrow to produce more white blood cells, helping to prevent infections in these vulnerable patients.
Lipegfilgrastim is administered as an injection and has a longer duration of action compared to non-pegylated GCSF, allowing for less frequent dosing. This can improve patient adherence to the treatment regimen and reduce the burden of frequent injections.
Overall, the use of lipegfilgrastim in the medical field is valuable for reducing the risk of infections in patients undergoing chemotherapy and supporting their immune system during cancer treatment.