Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Điểm đẳng điện tích
Dược Lực Học :
Oprelvekin is indicated for the prevention of severe thrombocytopenia and the reduction of the need for platelet transfusions following myelosuppressive chemotherapy in adult patients with nonmyeloid malignancies who are at high risk of severe thrombocytopenia. The primary hematopoietic activity of Oprelvekin is stimulation of megakaryocytopoiesis and thrombopoiesis. Oprelvekin has shown potent thrombopoietic activity in individuals with compromised hematopoiesis
Cơ Chế Tác Dụng :
Oprelvekin, the active ingredient in Neumega® is recombinant Interleukin eleven, which is produced in Escherichia coli (E. coli) by recombinant DNA technology. The protein has a molecular mass of approximately 19,000 daltons, and is non-glycosylated. The polypeptide is 177 amino acids in length (the natural IL-11 has 178). This alteration has not resulted in measurable differences in bioactivity either in vitro or in vivo.
The primary hematopoietic activity of Neumega® is stimulation of megakaryocytopoiesis and thrombopoiesis. In mice and nonhuman primate studies Neumega® has shown potent thrombopoietic activity in compromised hematopoiesis, including moderately to severely myelosuppressed animals. In these studies, Neumega® improved platelet nadirs and accelerated platelet recoveries compared to controls.
In animal studies Oprelvekin also has non-hematopoetic activities. This includes the regulation of intestinal epithelium growth (enhanced healing of gastrointestinal lesions), the inhibition of adipogenesis, the induction of acute phase protein synthesis (e.g., fibrinogen), and inhibition of macrophageal released pro-inflammatory cytokines.
Oprelvekin binds to the interleukin 11 receptor which leads to a cascade of signal transduction events. IL-11 is a thrombopoietic growth factor that directly stimulates the proliferation of hematopoietic stem cells and megakaryocyte progenitor cells and induces megakaryocyte maturation resulting in increased platelet production.
Dược Động Học :
▧ Absorption :
Absolute bioavailability is over 80%.
▧ Route of Elimination :
The kidney is the primary route of elimination. The amount of intact Neumega in urine was low, indicating that the molecule was metabolized before excretion.
▧ Half Life :
6.9 +/- 1.7 hrs
Chỉ Định :
Increases reduced platelet levels due to chemotherapy
Tương Tác Thuốc :
May increase the serum levels of opioid analgesics. It is recommended to monitor therapy for the signs and symptoms of respiratory depression and enhanced sedation.
Liều Lượng & Cách Dùng :
Injection, powder, lyophilized, for solution - Subcutaneous
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