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Filgrastim
Các tên gọi khác (3) :
  • G-CSF
  • Granulocyte Colony Stimulating Factor
  • Tbo-filgrastim
Thuốc tác dụng đối với máu
Thuốc Gốc
Biotech
CAS: 121181-53-1
ATC: L03AA02
ĐG : Amgen Inc. , http://www.amgen.com
CTHH: C845H1343N223O243S9
PTK: 18.8 kDa
Filgrastim is a recombinant, non-pegylated human granulocyte colony stimulating factor (G-CSF) analogue manufactured by recombinant DNA technology using a strain of E. coli. It is marketed as the brand name Neupogen by Amgen. Chemically, it consists of 175 amino acid residues. The protein has an amino acid sequence that is identical to the natural sequence predicted from human DNA sequence analysis, except for the addition of an N-terminal methionine necessary for expression in E coli. Tbo-filgrastim, which is marketed by Sicor Biotech and FDA approved on August 29, 2012, contains the same active ingredient as Neupogen and is biologically similar, but it is formulated to be short-acting.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C845H1343N223O243S9
Phân tử khối
18.8 kDa
Độ tan chảy
60 °C
Độ kỵ nước
0.209
Điểm đẳng điện tích
5.65
Dược Lực Học : 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.
Cơ Chế Tác Dụng : Filgrastim is a recombinant, non-pegylated human granulocyte colony stimulating factor (G-CSF) analogue manufactured by recombinant DNA technology using a strain of E. coli. It is marketed as the brand name Neupogen by Amgen. Chemically, it consists of 175 amino acid residues. The protein has an amino acid sequence that is identical to the natural sequence predicted from human DNA sequence analysis, except for the addition of an N-terminal methionine necessary for expression in E coli. Tbo-filgrastim, which is marketed by Sicor Biotech and FDA approved on August 29, 2012, contains the same active ingredient as Neupogen and is biologically similar, but it is formulated to be short-acting. 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
Dược Động Học :
▧ Absorption :
Absorption and clearance of Neupogen follows first-order pharmacokinetic modeling without apparent concentration dependence. When 3.45 mcg/kg and 11.5 mcg/kg of Neupogen is subcutaneously administered, the maximum serum concentration is 4 and 49 ng/mL‚ respectively‚ within 2 to 8 hours. Neupogen does not accumulate. It is estimated that when filgrastim is subcutaneously administered, the absolute bioavailability is approximately 62% and 71% for 375 mcg and 750 mcg doses respectively. When 5 mcg/kg tbo-filgrastim is subcutaneously administered, the absolute bioavailability is 33%. It takes 4-6 hours for tho-filgrastim to reach maximum concentration. Like Neupogen, accumulation was not observed.
▧ Volume of Distribution :
Vd, healthy subjects and cancer patients = 150 mL/kg
▧ Route of Elimination :
Filgrastim 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 endocytosis, and subsequent degradation inside the cells.
▧ Half Life :
Elimination half-life, healthy subjects and cancer patients, Neopogen = 3.5 hours; Elimination half-life, cancer patients, tbo-filgrastim = 3.2-3.8 hours
▧ Clearance :
0.5 - 0.7 mL/minute/kg (SC administration of 3.45 mcg/kg and 11.5 mcg/kg in both normal subjects and cancer patients, Neupogen)
Chỉ Định : 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.
Tương Tác Thuốc :
  • Bleomycin Monitor therapy due to enhanced adverse effects of bleomycin especially pulmonary toxicity.
  • Cyclophosphamide Monitor therapy due to adverse effects of cyclophosphamide, especially pulmonary toxicity.
  • Topotecan Filgrastim may increase the adverse effects of Topotecan. Increased risk of prolonged neutropenia. Filgrastim should be administered at least 24 hours following Topotecan therapy. Monitor for signs and symptoms of neutropenia.
Liều Lượng & Cách Dùng : Injection, solution - Intravenous - 300 mcg/mL; 480 mcg/1.6 mL; 300 mcg/0.5 mL; 480 mcg/0.8 mL
Injection, solution - Subcutaneous - 300 mcg/0.5 mL; 480 mcg/0.8 mL
Dữ Kiện Thương Mại
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Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00099
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D03235
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/55513-209-10
GenBank
http://www.ncbi.nlm.nih.gov/nuccore/X03438
PharmGKB
http://www.pharmgkb.org/drug/PA449626
Wikipedia
http://en.wikipedia.org/wiki/Filgrastim
RxList
http://www.rxlist.com/cgi/generic/filgrastim.htm
Drugs.com
http://www.drugs.com/cdi/filgrastim.html
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