Tìm theo
Pegaptanib
Các tên gọi khác (5 ) :
  • EYE 001
  • NX 1838
  • NX1838
  • Pegaptanib Octasodium
  • Pegaptanib sodium
Thuốc Gốc
Biotech
CAS: 222716-86-1
ATC: S01LA03
ĐG : Eyetech Inc. , http://www.eyetech.com
CTHH: C294H342F13N107Na28O188P28[C2H4O]2n
PTK: ~50 kDa
Pegaptanib is a polynucleotide aptamer. Pegaptanib specifically binds to VEGF 165, a protein that plays a critical role in angiogenesis (the formation of new blood vessels) and increased permeability (leakage from blood vessels), two of the primary pathological processes responsible for the vision loss associated with neovascular AMD. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C294H342F13N107Na28O188P28[C2H4O]2n
Phân tử khối
~50 kDa
Dược Lực Học : Pegaptanib is a selective vascular endothelial growth factor (VEGF) antagonist. VEGF is a secreted protein that selectively binds and activates its receptors located primarily on the surface of vascular endothelial cells. VEGF induces angiogenesis, and increases vascular permeability and inflammation, all of which are thought to contribute to the progression of the neovascular (wet) form of age-related macular degeneration (AMD), a leading cause of blindness. VEGF has been implicated in blood retinal barrier breakdown and pathological ocular neovascularization.
Cơ Chế Tác Dụng : Pegaptanib is a polynucleotide aptamer. Pegaptanib specifically binds to VEGF 165, a protein that plays a critical role in angiogenesis (the formation of new blood vessels) and increased permeability (leakage from blood vessels), two of the primary pathological processes responsible for the vision loss associated with neovascular AMD. [Wikipedia] Pegaptanib sodium is a pegylated aptamer, a modified oligonucleotide, which adopts a three- dimensional conformation that enables it to bind to extracellular VEGF with high affinity and selectivity. Pegaptanib sodium binds to the major pathological VEGF isoform, extracellular VEGF165, with high affinity (Kd = 200 pM) and specificity, thereby inhibiting VEGF165 binding to its VEGF receptors. In contrast virtually no binding of the non-pegylated aptamer to VEGF121 or the VEGF -related proteins VEGF-B, VEGF-C and placental growth factor (PlGF) was detected using invitro filter binding assays. Pegaptanib sodium does not bind significantly to VEGF121. In animal models, VEGF164 (the rodent counterpart of human VEGF165) was specifically upregulated in disease. The selective inhibition of VEGF164 with pegaptanib sodium proved as effective at suppressing pathological neovascularization as pan-VEGF inhibition7, however pegaptanib sodium spared the normal vasculature whereas pan-VEGF inhibition did not.
Dược Động Học :
▧ Absorption :
In animals, pegaptanib is slowly absorbed into the systemic circulation from the eye after intravitreous administration.
▧ Volume of Distribution :
It is distributed into vitreous fluid, retina, aqueous fluid, and kidneys. As well, it has been shown to cross the placenta in mice but whether or not it crosses the placenta in humans is unknown.
▧ Metabolism :
Based on preclinical data, pegaptanib is metabolized by endo- and exonucleases.
▧ Route of Elimination :
It is excreted primarily in urine as unchanged drug and also as metabolites. There is no dosage adjustment required for patients with renal impairment although it must be noted that not many studies have looked at patients with a creatinine clearance of 30mL/min.
▧ Half Life :
In humans, after a 3 mg monocular dose (10 times the recommended dose), the average (± standard deviation) apparent plasma half-life of pegaptanib is 10 (± 4) days.
Độc Tính : It is not known if pegaptanib is safe in pregnant women or if it is excreted in breast milk. Likewise, no studies have been done in the pediatric population. Most adverse events elated to the drug are ocular however non-ocular adverse events related to the drug or the injection procedure also occurred, among which headaches and rhinorrhoea appeared in more than 1% of patients. Pegaptanib is contraindicated when the patient has an ocular or periocular infection.
Chỉ Định : For the treatment of neovascular (wet) age-related macular degeneration.
Liều Lượng & Cách Dùng : Solution - Intravitreal
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Macugen 0.3 mg/0.09 ml
    Giá bán buôn : USD >1194.0
    Đơn vị tính : vial
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Macugen
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04895
PharmGKB
http://www.pharmgkb.org/drug/PA164771236
Wikipedia
http://en.wikipedia.org/wiki/Pegaptanib
RxList
http://www.rxlist.com/cgi/generic/macugen.htm
Drugs.com
http://www.drugs.com/cdi/pegaptanib.html
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