Tìm theo
Romiplostim
Các tên gọi khác (5 ) :
  • Semaxanib
  • Semaxinib
  • SID49674962
  • SID50107014
  • SU-5416
colony stimulating factors, thrombopoietic agents
Thuốc Gốc
Biotech
CAS: 267639-76-9
ATC: B02BX04
CTHH: C2634H4086N722O790S18
PTK: 59 kDa
Romiplostim is a thrombopoiesis stimulating dimer Fc-peptide fusion protein (peptibody) to increase platelet production through activation of the thrombopoietin receptor. The peptibody molecule has two identical single-chain subunits, each one is made up of 269 amino acid residues. Each subunit consists of an IgG1 Fc carrier domain that is covalently attached to a polypeptide sequence that contains two binding domains to interact with thrombopoietin receptor c-Mpl. Each domain consists of 14 amino acids. Interestingly, romiplostim's amino acid sequence is not similar to that of endogenous thrombopoietin. Romiplostim is produced by recombinant DNA technology in Escherichia coli. FDA approved on August 22, 2008.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C2634H4086N722O790S18
Phân tử khối
59 kDa
Dược Lực Học : Responses to platelet increase varies between patients thus indicating a need for individualization of dose. However, a dose dependent-increase in platelet counts have been observed in clinical trials. Does not affect platelet destruction.
Cơ Chế Tác Dụng : Romiplostim is a thrombopoiesis stimulating dimer Fc-peptide fusion protein (peptibody) to increase platelet production through activation of the thrombopoietin receptor. The peptibody molecule has two identical single-chain subunits, each one is made up of 269 amino acid residues. Each subunit consists of an IgG1 Fc carrier domain that is covalently attached to a polypeptide sequence that contains two binding domains to interact with thrombopoietin receptor c-Mpl. Each domain consists of 14 amino acids. Interestingly, romiplostim's amino acid sequence is not similar to that of endogenous thrombopoietin. Romiplostim is produced by recombinant DNA technology in Escherichia coli. FDA approved on August 22, 2008. Romiplostim is a thrombopoietin receptor agonist that activates intracellular transcriptional pathways via c-Mpl to increase production of platelets. It also works similarly to thrombopoietin (TPO), an endogenous glycoprotein hormone that regulates the production of platelets in the bone marrow.
Dược Động Học :
▧ Absorption :
Cmax, healthy volunteers, subQ = 24-36 hours; Cmax, immune thrombocytopenia patients, subQ = 7-50 hours (median = 14 hours). Not affected by age, weight, or gender. Accumulation does not occur after six weekly doses of 3 mcg/kg romiplostim.
▧ Volume of Distribution :
In healthy volunteers, non-linear decrease in Vd with increase IV dose of romiplostim which indicates saturation of c-Mpl receptors. Vd, 0.3 μg/kg = 122 mL/kg Vd, 10 μg/kg = 48.2 mL/kg
▧ Route of Elimination :
Renal clearance (more dominant mode of clearance as dose increases) and binding to c-Mpl receptors (dominant mode of clearance at low doses)
▧ Half Life :
Immune thrombocytopenia patients, subQ = 3.5 days (median) (range 1-34 days)
Độc Tính : The most common adverse reactions (≥ 5% higher patient incidence in Nplate versus placebo) are arthralgia, dizziness, insomnia, myalgia, pain in extremity, abdominal pain, shoulder pain, dyspepsia, and paresthesia. Headache was the most commonly reported adverse reaction that did not occur at ≥ 5% higher patient incidence in Nplate versus placebo. LD50 = 980 mg/kg.
Chỉ Định : Treatment of chronic immune thrombocytopenic purpura.
Liều Lượng & Cách Dùng : Injection, powder, for solution - Subcutaneous - 250 mcg
Injection, powder, for solution - Subcutaneous - 500 mcg
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Amgen
    Sản phẩm biệt dược : Nplate
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB05332
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D08990
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/55513-221-01
Wikipedia
http://en.wikipedia.org/wiki/Romiplostim
RxList
http://www.rxlist.com/nplate-drug.htm
Drugs.com
http://www.drugs.com/monograph/romiplostim.html
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