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Các tên gọi khác (1) :
  • Envelope polyprotein GP160 precursor [Contains: Exterior membrane glycoprotein,GP120, Transmembrane glycoprotein,GP41]
hiv fusion inhibitors
Thuốc Gốc
CAS: 159519-65-0
ATC: J05AX07
ĐG : F Hoffmann La Roche Ltd. , http://www.roche.com
CTHH: C204H301N51O64
PTK: 4491.8760
36 residue synthetic peptide that inhibits HIV-1 fusion with CD4 cells. N-terminal acetylated, C-terminal amide.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
Độ kỵ nước
Điểm đẳng điện tích
Cơ Chế Tác Dụng : 36 residue synthetic peptide that inhibits HIV-1 fusion with CD4 cells. N-terminal acetylated, C-terminal amide. Enfuvirtide binds to the first heptad-repeat (HR1) in the gp41 subunit of the viral envelope glycoprotein and prevents the conformational changes required for the fusion of viral and cellular membranes. It works by disrupting the HIV-1 molecular machinery at the final stage of fusion with the target cell, preventing uninfected cells from becoming infected. Enfuvirtide is a biomimetic peptide that was rationally designed to mimic components of the HIV-1 fusion machinery and displace them, preventing normal fusion.
Dược Động Học :
▧ Absorption :
After a 90 mg single subcutaneous injection of Enfuvirtide into the abdomen in 12 HIV-1 infected subjects, the mean peak concentration is 4.59+/-1.5 ug/ml and the median time to peak concentration was 8 hours (ranged from 3 to12 hours).
▧ Volume of Distribution :
* 5.5 ± 1.1 L
▧ Protein binding :
▧ Metabolism :
Expected to undergo catabolism to its constituent amino acids, with subsequent recycling of the amino acids in the body pool.
▧ Half Life :
3.8 +/- 0.6 hrs
▧ Clearance :
* 24.8 +/- 4.1 mL/h/kg [HIV-1 infected adult and pediatric subjects following a 90-mg single SC dose of enfuvirtide] * 30.6 +/- 10.6 mL/h/kg [Following 90-mg twice daily dosing of FUZEON SC in combination with other antiretroviral agents in HIV-1 infected subjects] * 40 +/- 17 mL/h/kg [pediatric patients in the presence of concomitant medications including antiretroviral agents receiving the 2 mg/kg twice daily dose]
Chỉ Định : Enfuvirtide is an antiretroviral drug used in combination therapy for the treatment of HIV-1/AIDS.
Liều Lượng & Cách Dùng : Powder, for solution - Subcutaneous
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Fuzeon convenience kit
    Giá bán buôn : USD >3062.23
    Đơn vị tính : kit
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