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Pegfilgrastim
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DB00019 |
[Pegfilgrastim is a PEGylated form of the recombinant human granulocyte colony-stimulating factor (G-CSF) analogue, [filgrastim].[A187601] It is used to decrease the incidence of infection, as manifested by febrile neutropenia, in patients with with non-myeloid cancer receiving myelosuppressive anti-cancer treatment. Some patients with greater risk factors may develop febrile neutropenia from myelosuppressive therapy and are susceptible to an increased risk of developing infections. Although the risk of developing febrile neutropenia is less than 20% in many readily used chemotherapy regimens,[L9782] infections pose risks of hospitalization and mortalities.[A187631] Due to the relatively short circulating half-life of filgrastim, a 20 kDa PEG moiety was covalently conjugated to the N-terminus of filgrastim (at the methionine residue) to develop a longer acting version of the drug.[A29, A187607] Due to a longer half-life and slower elimination rate than filgrastim, pegfilgrastim requires less frequent dosing than filgrastim. However, pegfilgrastim retains the same biological activity as filgrastim and binds to the same G-CSF receptor to stimulate the proliferation, differentiation, and activation of neutrophils.[A187607]
First developed by Amgen, pegfilgrastim was initially approved by the FDA in 2002 and marketed as Neulasta®. It is typically administered via a subcutaneous injection. There are several pegfilgrastim biosimilars (Fulphila®, Pelgraz® or Lapelga®, Pelmeg®, Udenyca®, Ziextenzo®, and Grasustek®) that are approved for the same therapeutic indication by Health Canada, European Union (EU), and FDA.[L9779,L9785] These biosimilars are highly similar to the reference product, Neulasta®, in terms of pharmacological and pharmacokinetic profile and condition(s) of use, such as the therapeutic indication(s), dosing regimen(s), strength(s), dosage form(s), and route(s) of administration.[L9974]] |
