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Product Details:

  • CAS No: 121181-53-1
  • AHFC code: 20:16.0
  • Synonyms: Biograstim, DRG-0086, Filgrastim, Filgrastim Hexal, Filgrastim ratiopharm, Filgrastim-sndz, Filgrastime, Filgrastime [INN-French], Filgrastimum, Filgrastimum [INN-Latin], Granulocyte colony stimulating factor, recombinant, Granulokine, hrG-CSF, HSDB 8159, KRN 8601, Leucostim, MBRI 9901, N-L-Methionylcolony-stimulating factor (human clone 1034), Neukine, Neupogen, Nivestim, Nufile-Safe, r-metHug-C-SF, r-metHug-CSF, Ratiograstim, Recombinant methionyl granulocyte colony stimulating factor, Recombinant methionyl human G-CSF, rG-CSF, rHG-CSF, Tevagrastim, UNII-PVI5M0M1GW, XM 02, Zarxio, Zarzio
  • ATC Code: L03AA02
  • Chemical Formula: C845-H1339-N223-O243-S9
  • Molecular Weight: 18798.7851
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB00099 (BIOD00072, BTD00072)
  • SMILES:
  • InChl:
  • PubChem:
  • IUPAC: Colony-stimulating factor (human clone 1034), N-L-methionyl-

Additional Details

Indication:
Filgrastim is used in patients with acute myeloid leukemia receiving induction or consolidation chemotherapy. It is also used in cancer patients receiving bone marrow transplant. In general, filgrastim increases neutrophil counts in order to decrease the risk of infection or duration of neutropenia in the aforementioned patient populations. Infection and neutropenia are adverse events associated with chemotherapy. Furthermore, filgrastim is also indicated for patients with severe chronic neutropenia. It mobilizes hematopoietic progenitor cells into the peripheral blood for collection by leukapheresis to allow for a more rapid engraftment. Tbo-filgrastim has a narrower indication profile than Neupogen – it is a leukocyte growth factor indicated for the reduction in the duration of severe neutropenia in patients with non-myeloid malignancies.
Pharmacodynamics:
Used in the treatment of chemotherapy-induced neutropenia by enhancing the production of neutrophils. Filgrastim acts on hematopoietic cells by binding to specific cell surface receptors thereby stimulating proliferation, differentiation, commitment, and end cell functional activation. When tbo-filgrastim is administered to cancer patients, it took 3-5 days to reach maximum absolute neutrophil count (ANC). Levels of neutrophils returned to baseline by 21 days following completion of chemotherapy. In the healthy volunteer trials, doubling the tbo-filgrastim subcutaneous dose from 5 to 10 mcg/kg resulted in a 16-19% increase in the ANCmax and a 33-36% increase in the area under the effect curve for ANC.
Mode of Action:
Filgrastim binds to the G-CSF receptor and stimulates the production of neutrophils in the bone marrow. As a G-CSF analog, it controls proliferation of committed progenitor cells and influences their maturation into mature neutrophils. Filgrastim also stimulates the release of neutrophils from bone marrow storage pools and reduces their maturation time. Filgrastim acts to increase the phagocytic activity of mature neutrophils. In patients receiving cytotoxic chemotherapy, Filgrastim can accelerate neutrophil recovery, leading to a reduction in duration of the neutropenic phase
Metabolism:
Toxicity:
General Reference:
Wang B, Ludden TM, Cheung EN, Schwab GG, Roskos LK: Population pharmacokinetic-pharmacodynamic modeling of filgrastim (r-metHuG-CSF) in healthy volunteers. J Pharmacokinet Pharmacodyn. 2001 Aug;28(4):321-42. PubmedFDA label for Neupogen and tbo-filgrastim
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