Tìm theo
Peginesatide
Các tên gọi khác (2) :
  • Erythropoiesis-Stimulating Agent (ESA)
  • Hematide
colony stimulating factors, hematopoietic agents
Thuốc Gốc
Small Molecule
CAS: 913976-27-9
ATC: B03XA04
CTHH: (C2H4O)n(C2H4O)nC229H344N62O58S6
Peginesatide is a synthetic peptide attached to polyethylene glycol for the treatment of anemia. The polyethylene glycol moiety helps make the drug less immunogenic and prolongs its plasma half-life. Chemically, peginesatide is designed to mimic the pharmacological activity of erythropoietin, but is not a replica of the structure itself. Peginesatide consists of two 21-amino acid chains that are covalently bonded by a linker derived from iminodiacetic acid and β-alanine. FDA approved March 27, 2012.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
(C2H4O)n(C2H4O)nC229H344N62O58S6
pKa
6.0 ± 0.3
Dược Lực Học : Peginesatide increases the reticulocyte count and levels of hemoglobin. It also increases RBC count, hematocrit, and soluble transferrin receptor protein in a dose-dependent manner.
Cơ Chế Tác Dụng : Peginesatide is a synthetic peptide attached to polyethylene glycol for the treatment of anemia. The polyethylene glycol moiety helps make the drug less immunogenic and prolongs its plasma half-life. Chemically, peginesatide is designed to mimic the pharmacological activity of erythropoietin, but is not a replica of the structure itself. Peginesatide consists of two 21-amino acid chains that are covalently bonded by a linker derived from iminodiacetic acid and β-alanine. FDA approved March 27, 2012. Peginesatide binds to and activates the human erythropoietin receptor and stimulates erythropoiesis in human red cell precursors in vitro.
Dược Động Học :
▧ Absorption :
Tmax, SubQ dose = 48 hours; Bioavailability, SubQ dose = 46%; Peginesatide does not accumulate when administered every 4 weeks following intravenous or subcutaneous administration.
▧ Volume of Distribution :
IV dose, dialysis patients = 34.9 ± 13.8 mL/kg;
▧ Protein binding :
Peginesatide does not bind to serum albumin or lipoprotein as demonstrated in in-vitro studies.
▧ Metabolism :
Preclinical radiolabeled peginesatide study indicated that peginesatide is not metabolized.
▧ Route of Elimination :
Peginesatide administered intravenously or subcutaneously is primarily excreted via urine. Most of the excreted dose is in the form of unchanged drug. Elimination from the plasma is biphasic and rapid from vascular compartments. In contrast, the drug is selectively retained in sites of erythropoiesis like the bone marrow.
▧ Half Life :
IV dose, healthy subjects = 25.0 ± 7.6 hours; SubQ, healthy subjects = 53.0 ± 17.7 hours; IV dose, dialysis patients = 47.9 ± 16.5 hours;
▧ Clearance :
Systemic clearance, IV dose, dialysis patients = 0.5 ± 0.2 mL/hr•kg
Độc Tính : The most common adverse events (≥10%) are dyspnea, diarrhea, nausea, cough, and arteriovenous fistula site complication.
Chỉ Định : Peginesatide is used for the treatment of anemia due to chronic kidney disease (CKD) in adult patients on dialysis
Liều Lượng & Cách Dùng : Solution - Intravenous - 10 mg/mL; 20 mg/2 mL
Dữ Kiện Thương Mại
Nhà Sản Xuất
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08894
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D09947
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/64764-620-20
Wikipedia
http://en.wikipedia.org/wiki/Peginesatide
RxList
http://www.rxlist.com/omontys-drug.htm
Drugs.com
http://www.drugs.com/cdi/peginesatide.html
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